Altanserin: Difference between revisions

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			{{Short description\|Chemical compound}}
	{{drugbox
			{{Drugbox
	\| Verifiedfields = changed
	\| ~~UNII_Ref~~ = ~~{{fdacite\|~~changed~~\|FDA}}~~		\| Watchedfields = changed
			\| verifiedrevid = 438043109
	\| UNII = 5015H744JQ
			\| IUPAC_name = 3-ethyl]-2-sulfanylidene-1''H''-quinazolin-4-one
	\| verifiedrevid = 407661180
			\| image = Altanserin.svg
	\| IUPAC_name = 3-ethyl]-2-sulfanylidene-1''H''-quinazolin-4-one
			<!--Clinical data-->
	\| image = Altanserin.png
			\| tradename =
			\| pregnancy_category =
			\| legal_status =
			\| routes_of_administration =
			<!--Pharmacokinetic data-->
			\| bioavailability =
			\| protein_bound =
			\| metabolism =
			\| elimination_half-life =
			\| excretion =
			<!--Identifiers-->
			\| CAS_number_Ref = {{cascite\|correct\|??}}
			\| CAS_number = 76330-71-7
			\| ATC_prefix = none
			\| ATC_suffix =
			\| PubChem = 3033677
			\| DrugBank_Ref = {{drugbankcite\|correct\|drugbank}}
			\| DrugBank =
	\| ChemSpiderID_Ref = {{chemspidercite\|correct\|chemspider}}		\| ChemSpiderID_Ref = {{chemspidercite\|correct\|chemspider}}
	\| ChemSpiderID = 2298299		\| ChemSpiderID = 2298299
			\| UNII_Ref = {{fdacite\|correct\|FDA}}
	\| InChI = 1/C22H22FN3O2S/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)
			\| UNII = 5015H744JQ
	\| smiles = Fc1ccc(cc1)C(=O)C4CCN(CCN3C(=O)c2ccccc2NC3=S)CC4
	\| InChIKey = SMYALUSCZJXWHG-UHFFFAOYAG
	\| ChEMBL_Ref = {{ebicite\|correct\|EBI}}		\| ChEMBL_Ref = {{ebicite\|correct\|EBI}}
	\| ChEMBL = 62919		\| ChEMBL = 62919
			<!--Chemical data-->
			\| C=22 \| H=22 \| F=1 \| N=3 \| O=2 \| S=1
			\| SMILES = Fc1ccc(cc1)C(=O)C4CCN(CCN3C(=O)c2ccccc2NC3=S)CC4
	\| StdInChI_Ref = {{stdinchicite\|correct\|chemspider}}		\| StdInChI_Ref = {{stdinchicite\|correct\|chemspider}}
	\| StdInChI = 1S/C22H22FN3O2S/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)		\| StdInChI = 1S/C22H22FN3O2S/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)
	\| StdInChIKey_Ref = {{stdinchicite\|correct\|chemspider}}		\| StdInChIKey_Ref = {{stdinchicite\|correct\|chemspider}}
	\| StdInChIKey = SMYALUSCZJXWHG-UHFFFAOYSA-N		\| StdInChIKey = SMYALUSCZJXWHG-UHFFFAOYSA-N
	\| CAS_number = 76330-71-7
	\| ATC_prefix = none
	\| ATC_suffix =
	\| PubChem = 3033677
	\| DrugBank =
	\| C=22\|H=22\|F=1\|N=3\|O=2\|S=1
	\| molecular_weight = 411.49<ref name="ABX">ABX, , Radeberg, Germany.</ref>
	\| bioavailability =
	\| protein_bound =
	\| metabolism =
	\| elimination_half-life =
	\| excretion =
	\| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
	\| pregnancy_US = <!-- A / B / C / D / X -->
	\| pregnancy_category=
	\| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
	\| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII -->
	\| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C -->
	\| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
	\| legal_status =
	\| routes_of_administration =
	}}		}}

			'''Altanserin''' is a compound that ] to the ] (5-Hydroxytryptamine (]) 2A receptor). Labeled with the ] ] it is used as a ] in ] (PET) studies of the ], i.e., studies of the 5-HT<sub>2A</sub> ]s. Besides human ] studies altanserin has also been used in the study of ]s.<ref name="pmid1744713">{{cite journal \| vauthors = Lemaire C, Cantineau R, Guillaume M, Plenevaux A, Christiaens L \| title = Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats \| journal = Journal of Nuclear Medicine \| volume = 32 \| issue = 12 \| pages = 2266–2272 \| date = December 1991 \| pmid = 1744713 }}</ref><ref name="pmid9257335">{{cite journal \| vauthors = Biver F, Lotstra F, Monclus M, Dethy S, Damhaut P, Wikler D, Luxen A, Goldman S \| display-authors = 6 \| title = In vivo binding of altanserin to rat brain 5HT2 receptors: a film and electronic autoradiographic study \| journal = Nuclear Medicine and Biology \| volume = 24 \| issue = 4 \| pages = 357–360 \| date = May 1997 \| pmid = 9257335 \| doi = 10.1016/s0969-8051(97)00054-1 \| hdl = 2268/144404 \| hdl-access = free }}</ref>
	'''Altanserin''' is a compound that ] to the ] (] 2A receptor).
	It is a yellowish solid.<ref name="ABX"/>
	Labeled with the ] ] it is used as a ] in ] (PET) studies of the ], i.e., studies of the serotonin-2A ]s.
	Besides human ] studies altanserin has also been used in the study of ]s.<ref>{{Cite journal
	\| author = ], R. Cantineau, M. Guillaume, A. Plenevaux, ]
	\| title = Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats
	\| journal = ]
	\| volume = 32
	\| pages = 2266–2277
	\| pmid = 1744713
	\| url = http://jnm.snmjournals.org/cgi/reprint/32/12/2266
	\| issue = 12
	\| date = December 1, 1991 }}</ref><ref>{{Cite journal
	\| author = F. Biver, F. Lotstra, M. Monclus, S. Dethy, P. Damhaut, D. Wikler, A. Luxen and S. Goldman
	\| title = ''In vivo'' binding of altanserin to rat brain 5HT<sub>2</sub> receptors: A film and electronic autoradiographic study
	\| journal = ]
	\| volume = 24
	\| issue = 4
	\| month = May
	\| year = 1997
	\| pages = 357–360
	\| doi = 10.1016/S0969-8051(97)00054-1
	\| pmid = 9257335
	}}</ref>

	An alternative for PET imaging the 5-HT<sub>2A</sub> receptor is the		An alternative for PET imaging the 5-HT<sub>2A</sub> receptor is the
	[]]~~MDL~~ 100,907 radioligand.		[]]] (MDL-100,907) radioligand.
			<sup>18</sup>F-altanserin and ]-volinanserin have shown very comparable binding.<ref name="pmid16206185">{{cite journal \| vauthors = Kristiansen H, Elfving B, Plenge P, Pinborg LH, Gillings N, Knudsen GM \| title = Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907 \| journal = Synapse \| volume = 58 \| issue = 4 \| pages = 249–257 \| date = December 2005 \| pmid = 16206185 \| doi = 10.1002/syn.20205 \| s2cid = 19110277 }}</ref>
	Fluorine-18-altanserin and ]-MDL 100,907 have shown very comparable binding.<ref name="KristiansenH2005Binding">{{Cite journal
			Both altanserin and MDL 100,907 are 5-HT<sub>2A</sub> receptor ]s.<ref name="pmid16206185"/>
	\| author = Heidi Kristiansen, Bettina Elfving, Per Plenge, Lars H. Pinborg, Nic Gillings & Gitte Moos Knudsen
	\| title = Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907
	\| journal = ]
	\| year = 2005
	\| month = December
	\| volume = 58
	\| issue = 4
	\| pages = 249–257
	\| url = http://www3.interscience.wiley.com/cgi-bin/abstract/112098314/ABSTRACT
	\| doi = 10.1002/syn.20205
	\| pmid = 16206185
	}}</ref>
	Both altanserin and MDL 100,907 are 5-HT<sub>2A</sub> receptor ]s.<ref name="KristiansenH2005Binding"/>
	-] can also be used in PET.		-] can also be used in PET.

	An alternative ] radioligand is the -] receptor antagonist.<ref name="~~AudenaertK2003Decreased~~">{{~~Cite~~ journal		An alternative ] radioligand is the -] receptor antagonist.<ref name="pmid12571204">{{cite journal \| vauthors = Audenaert K, Van Laere K, Dumont F, Vervaet M, Goethals I, Slegers G, Mertens J, van Heeringen C, Dierckx RA \| display-authors = 6 \| title = Decreased 5-HT2a receptor binding in patients with anorexia nervosa \| journal = Journal of Nuclear Medicine \| volume = 44 \| issue = 2 \| pages = 163–169 \| date = February 2003 \| pmid = 12571204 }}</ref>
	\| author = Kurt Audenaert, Koen Van Laere, Filip Dumont, Miriam Vervaet, Ingeborg Goethals, Guido Slegers, John Mertens, Cees van Heeringen, Rudi A. Dierckx
	\| title = Decreased 5-HT<sub>2A</sub> Receptor Binding in Patients with Anorexia Nervosa
	\| journal = ]
	\| volume = 44
	\| pages = 163–169
	\| pmid = 12571204
	}}</ref>

	A rapid chemical synthesis of fluorine-18 and ] dual-labeled altanserin has been described.<ref>{{~~Cite~~ journal		A rapid chemical synthesis of fluorine-18 and ] dual-labeled altanserin has been described.<ref name="TanBaldwin1999">{{cite journal\| vauthors = Tan PZ, Baldwin RM, Fu T, Charney DS, Innis RB \|title=Rapid synthesis of F-18 and H-2 dual-labeled altanserin, a metabolically resistant PET ligand for 5-HT2a receptors\|journal=Journal of Labelled Compounds and Radiopharmaceuticals\|volume=42\|issue=5\|year=1999\|pages=457–467\|issn=0362-4803\|doi=10.1002/(SICI)1099-1344(199905)42:5<457::AID-JLCR206>3.0.CO;2-0}}</ref>
	\| author = Ping-Zhong Tan, Ronald M. Baldwin, Tao Fu, Dennis S. Charney, ]
	\| title = Rapid synthesis of F-18 and H-2 dual-labeled altanserin, a metabolically resistant PET ligand for 5-HT<sub>2a</sub> receptors
	\| journal = ]
	\| volume = 42
	\| issue = 5
	\| pages = 457–467
	\| year = 1999
	\| month = May
	\| doi = 10.1002/(SICI)1099-1344(199905)42:5<457::AID-JLCR206>3.0.CO;2-0
	}}</ref>

	Other ligands for other parts of the serotonin system used in PET studies are, e.g., ], ] and ].		Other ligands for other parts of the serotonin system used in PET studies are, e.g., ], ], and ].

	== Human brain mapping studies with altanserin ==		== Human brain mapping studies with altanserin ==
	]. Human experiments with fluorine-18 altanserin are performed in these types of brain scanners.]]		]. Human experiments with fluorine-18 altanserin are performed in these types of brain scanners.]]
	{{As of\|2007}} altanserin is probably not used in clinical routine.		{{As of\|2007}} altanserin is probably not used in clinical routine.
			However, there have been performed several research-based ] studies with the compound in humans since the 1990s.<ref>{{cite journal \| vauthors = Biver F, Goldman S, Luxen A, Monclus M, Forestini M, Mendlewicz J, Lotstra F \| title = Multicompartmental study of fluorine-18 altanserin binding to brain 5HT2 receptors in humans using positron emission tomography \| journal = European Journal of Nuclear Medicine \| volume = 21 \| issue = 9 \| pages = 937–946 \| date = September 1994 \| pmid = 7995287 \| doi = 10.1007/BF00238117 \| s2cid = 20200751 }}</ref><ref>{{cite journal \| vauthors = Sadzot B, Lemaire C, Maquet P, Salmon E, Plenevaux A, Degueldre C, Hermanne JP, Guillaume M, Cantineau R, Comar D \| display-authors = 6 \| title = Serotonin 5HT2 receptor imaging in the human brain using positron emission tomography and a new radioligand, altanserin: results in young normal controls \| journal = Journal of Cerebral Blood Flow and Metabolism \| volume = 15 \| issue = 5 \| pages = 787–797 \| date = September 1995 \| pmid = 7673371 \| doi = 10.1038/jcbfm.1995.99 \| s2cid = 36870327 \| doi-access = free }}</ref>
	However, there have been performed several research-based ] studies with the compound in humans since the 1990s.<ref>{{Cite journal
			Some of these studies have considered methodogical issues such as the ] of the method<ref>{{cite journal \| vauthors = Smith GS, Price JC, Lopresti BJ, Huang Y, Simpson N, Holt D, Mason NS, Meltzer CC, Sweet RA, Nichols T, Sashin D, Mathis CA \| display-authors = 6 \| title = Test-retest variability of serotonin 5-HT2A receptor binding measured with positron emission tomography and altanserin in the human brain \| journal = Synapse \| volume = 30 \| issue = 4 \| pages = 380–392 \| date = December 1998 \| pmid = 9826230 \| doi = 10.1002/(SICI)1098-2396(199812)30:4<380::AID-SYN5>3.0.CO;2-U \| s2cid = 1297178 }}</ref><ref>{{cite journal \| vauthors = Haugbøl S, Pinborg LH, Arfan HM, Frøkjaer VM, Madsen J, Dyrby TB, Svarer C, Knudsen GM \| display-authors = 6 \| title = Reproducibility of 5-HT2A receptor measurements and sample size estimations with altanserin PET using a bolus/infusion approach \| journal = European Journal of Nuclear Medicine and Molecular Imaging \| volume = 34 \| issue = 6 \| pages = 910–915 \| date = June 2007 \| pmid = 17195073 \| doi = 10.1007/s00259-006-0296-y \| s2cid = 1828118 }}</ref>
	\| author = Frangoise Biver, Serge Goldman, André Luxen, Michel Monclus, Manuel Forestini, Julien Mendlewicz and Françoise Lotstra
			or whether to use constant infusion<ref>{{cite journal \| vauthors = van Dyck CH, Tan PZ, Baldwin RM, Amici LA, Garg PK, Ng CK, Soufer R, Charney DS, Innis RB \| display-authors = 6 \| title = PET quantification of 5-HT2A receptors in the human brain: a constant infusion paradigm with altanserin \| journal = Journal of Nuclear Medicine \| volume = 41 \| issue = 2 \| pages = 234–241 \| date = February 2000 \| pmid = 10688105 \| url = http://jnm.snmjournals.org/cgi/content/abstract/41/2/234 \| author-link1 = Christopher H. van Dyck }}</ref> or bolus-infusion<ref>{{cite journal \| vauthors = Pinborg LH, Adams KH, Svarer C, Holm S, Hasselbalch SG, Haugbøl S, Madsen J, Knudsen GM \| display-authors = 6 \| title = Quantification of 5-HT2A receptors in the human brain using altanserin-PET and the bolus/infusion approach \| journal = Journal of Cerebral Blood Flow and Metabolism \| volume = 23 \| issue = 8 \| pages = 985–996 \| date = August 2003 \| pmid = 12902843 \| doi = 10.1097/01.WCB.0000074092.59115.23 \| s2cid = 6262998 \| doi-access = free }}</ref> delivery of altanserin.
	\| title = Multicompartmental study of fluorine-18 altanserin binding to brain 5HT2 receptors in humans using positron emission tomography
	\| journal = ]
	\| volume = 21
	\| issue = 9
	\| month = September
	\| year = 1994
	\| doi = 10.1007/BF00238117
	\| pages = 937–946
	\| url = http://www.springerlink.com/content/j063h72754286373/
	}}</ref><ref>{{Cite journal
	\| author = Sadzot B, Lemaire C, Maquet P, Salmon E, Plenevaux A, Degueldre C, Hermanne JP, Guillaume M, Cantineau R, Comar D, et al.
	\| title = Serotonin 5HT2 receptor imaging in the human brain using positron emission tomography and a new radioligand, altanserin: results in young normal controls
	\| journal = ]
	\| year = 1995
	\| month = September
	\| volume = 15
	\| issue = 5
	\| pages = 787–797
	\| pmid = 7673371
	}}</ref>
	Some of these studies have considered methodogical issues such as the ] of the method<ref>{{Cite journal
	\| author = Gwenn S. Smith, Julie C. Price, Brian J. Lopresti, Yiyun Huang, Norman Simpson, Daniel Holt, N. Scott Mason, Carolyn Cidis Meltzer, Robert A. Sweet, Thomas Nichols, Donald Sashin, Chester A. Mathis
	\| title = Test-retest variability of serotonin 5-HT<sub>2A</sub> receptor binding measured with positron emission tomography and altanserin in the human brain
	\| journal = ]
	\| year = 1998
	\| volume = 30
	\| issue = 4
	\| pages = 380–392
	\| doi = 10.1002/(SICI)1098-2396(199812)30:4<380::AID-SYN5>3.0.CO;2-U
	}}</ref><ref>{{Cite journal
	\| author = Steven Haugbøl, Lars H. Pinborg, Haroon M. Arfan, Vibe Frøkjær, Jacob Madsen, Tim B. Dyrby, Claus Svarer and Gitte M. Knudsen
	\| title = Reproducibility of 5-HT<sub>2A</sub> receptor measurements and sample size estimations with altanserin PET using a bolus/infusion approach
	\| journal = ]
	\| volume = 34
	\| issue = 6
	\| month = June
	\| year = 2007
	\| pages = 910–915
	\| doi = 10.1007/s00259-006-0296-y
	\| pmid = 17195073
	}}</ref>
	or whether to use constant infusion<ref>{{Cite journal
	\| author = Christopher H. van Dyck, Ping-Zhong Tan, Ronald M. Baldwin, Louis A. Amici, Pradeep K. Garg, Chin K. Ng, Robert Soufer, Dennis S. Charney and Robert B. Innis
	\| title = PET Quantification of 5-HT<sub>2A</sub> Receptors in the Human Brain: A Constant Infusion Paradigm with Altanserin
	\| journal = ]
	\| volume = 41
	\| issue = 2
	\| pages = 234–241
	\| url = http://jnm.snmjournals.org/cgi/content/abstract/41/2/234
	\| pmid = 10688105
	\| date = February 1, 2000 }}</ref> or bolus-infusion<ref>{{Cite journal
	\| author = Lars H Pinborg, Karen H Adams, Claus Svarer, Søren Holm*, Steen G Hasselbalch, Steven Haugbøl, Jacob Madsen and Gitte M Knudsen
	\| title = Quantification of 5-HT<sub>2A</sub> Receptors in the Human Brain Using [<sup>18</sup>F]Altanserin-PET and the Bolus/Infusion Approach
	\| journal = ]
	\| year = 2003
	\| volume = 23
	\| pages = 985–996
	\| doi = 10.1097/01.WCB.0000074092.59115.23
	\| url = http://www.nature.com/jcbfm/journal/v23/n8/abs/9591447a.html
	\| pmid = 12902843
	\| issue = 8
	}}</ref> delivery of altanserin.
	Other studies have compared altanserin ] to subject variables such as ], ] and ].		Other studies have compared altanserin ] to subject variables such as ], ] and ].

	The altanserin PET scan shows high binding in ].		The altanserin PET scan shows high binding in ].
	The ] is often regarded as a region with no specific 5-HT<sub>2A</sub> binding and the brain region is used as a reference in some studies, even though an ] study has found nonnegligible levels of 5-HT<sub>2A</sub> binding in the human cerebellum,<ref>{{~~Cite~~ journal		The ] is often regarded as a region with no specific 5-HT<sub>2A</sub> binding and the brain region is used as a reference in some studies, even though an ] study has found nonnegligible levels of 5-HT<sub>2A</sub> binding in the human cerebellum,<ref>{{cite journal \| vauthors = Eastwood SL, Burnet PW, Gittins R, Baker K, Harrison PJ \| title = Expression of serotonin 5-HT(2A) receptors in the human cerebellum and alterations in schizophrenia \| journal = Synapse \| volume = 42 \| issue = 2 \| pages = 104–114 \| date = November 2001 \| pmid = 11574947 \| doi = 10.1002/syn.1106 \| s2cid = 40304220 }}</ref>
			and another type of study have observed strong ] against 5-HT<sub>2A</sub> receptor protein in rat ]s.<ref>{{cite journal \| vauthors = Maeshima T, Shutoh F, Hamada S, Senzaki K, Hamaguchi-Hamada K, Ito R, Okado N \| title = Serotonin2A receptor-like immunoreactivity in rat cerebellar Purkinje cells \| journal = Neuroscience Letters \| volume = 252 \| issue = 1 \| pages = 72–74 \| date = August 1998 \| pmid = 9756362 \| doi = 10.1016/S0304-3940(98)00546-1 \| s2cid = 28549709 \| author-link1 = Toru Maeshima }}</ref>
	\| author = Sharon L. Eastwood, Philip W. J. Burnet, Rebecca Gittins, Kate Baker, Paul J. Harrison
	\| title = Expression of serotonin 5-HT<sub>2A</sub> receptors in the human cerebellum and alterations in schizophrenia
	\| journal = ]
	\| volume = 42
	\| issue = 2
	\| pages = 104–114
	\| month = November
	\| year = 2001
	\| doi = 10.1002/syn.1106
	\| pmid = 11574947
	}}</ref>
	and another type of study have observed strong ] against 5-HT<sub>2A</sub> receptor protein in rat ]s.<ref>{{Cite journal
	\| author = ], Fumihiro Shutoh, Shun Hamada, Kouji Senzaki, Kayoko Hamaguchi-Hamada, Ryuzo Ito, Nobuo Okado
	\| title = Serotonin2A receptor-like immunoreactivity in rat cerebellar Purkinje cells
	\| journal = ]
	\| year = 1998
	\| month = August
	\| volume = 252
	\| number = 1
	\| pages = 72–74
	\| pmid = 9756362
	\| doi = 10.1016/S0304-3940(98)00546-1
	\| issue = 1
	}}</ref>

	In the table below is an overview of the results of altanserin binding seen in human PET-studies.		In the table below is an overview of the results of altanserin binding seen in human PET-studies.
	A consistent finding across altanserin studies has been that the binding decreases with ].		A consistent finding across altanserin studies has been that the binding decreases with ].
	This is in line with '']'' studies of the 5-HT<sub>2A</sub> receptor,<ref>{{~~Cite~~ journal		This is in line with '']'' studies of the 5-HT<sub>2A</sub> receptor,<ref>{{cite journal \| vauthors = Marcusson JO, Morgan DG, Winblad B, Finch CE \| title = Serotonin-2 binding sites in human frontal cortex and hippocampus. Selective loss of S-2A sites with age \| journal = Brain Research \| volume = 311 \| issue = 1 \| pages = 51–56 \| date = October 1984 \| pmid = 6488044 \| doi = 10.1016/0006-8993(84)91397-0 \| s2cid = 1203974 }}</ref>
			as well as PET studies with other radioligands that binds to the receptor.<ref>{{cite journal \| vauthors = Wong DF, Wagner HN, Dannals RF, Links JM, Frost JJ, Ravert HT, Wilson AA, Rosenbaum AE, Gjedde A, Douglass KH \| display-authors = 6 \| title = Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain \| journal = Science \| volume = 226 \| issue = 4681 \| pages = 1393–1396 \| date = December 1984 \| pmid = 6334363 \| doi = 10.1126/science.6334363 \| s2cid = 24278577 \| bibcode = 1984Sci...226.1393W \| author-link9 = Albert Gjedde }}</ref>
	\| author = Jan O. Marcusson, David G. Morgan, ], Caleb E. Finch
	\| title = Serotonin-2 binding sites in human frontal cortex and hippocampus. Selective loss of S-2A sites with age
	\| journal = ]
	\| year = 1984
	\| month = October
	\| volume = 311
	\| issue = 1
	\| pages = 51–56
	\| pmid = 6488044
	\| doi = 10.1016/0006-8993(84)91397-0
	}}</ref>
	as well as PET studies with other radioligands that binds to the receptor.<ref>{{Cite journal
	\| author = D. F. Wong, H. N. Wagner Jr, R. F. Dannals, J. M. Links, J. J. Frost, H. T. Ravert, A. A. Wilson, A. E. Rosenbaum, ], K. H. Douglass, ''et al.''
	\| title = Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain
	\| journal = ]
	\| month = December
	\| year = 1984
	\| volume = 226
	\| issue = 4681
	\| pages = 1393–1396
	\| doi = 10.1126/science.6334363
	\| pmid = 6334363
	\| url = http://www.sciencemag.org/cgi/content/abstract/226/4681/1393
	}}</ref>

			The result for recovered ]-type ]<ref name="pmid15054474">{{cite journal \| vauthors = Bailer UF, Price JC, Meltzer CC, Mathis CA, Frank GK, Weissfeld L, McConaha CW, Henry SE, Brooks-Achenbach S, Barbarich NC, Kaye WH \| display-authors = 6 \| title = Altered 5-HT(2A) receptor binding after recovery from bulimia-type anorexia nervosa: relationships to harm avoidance and drive for thinness \| journal = Neuropsychopharmacology \| volume = 29 \| issue = 6 \| pages = 1143–1155 \| date = June 2004 \| pmid = 15054474 \| pmc = 4301578 \| doi = 10.1038/sj.npp.1300430 }}</ref>
	The result for recovered ]-type ]<ref name="BailerU2004Altered">{{Cite journal
			is in line with a SPECT study of anorexia nervosa patients, that found a decrease in frontal, occipital and parietal cortices.<ref name="pmid12571204" />
	\| author = Ursula F. Bailer, Julie C. Price, Carolyn C. Meltzer, Chester A. Mathis, Guido K. Frank, Lisa Weissfeld, Claire W. McConaha, Shannan E. Henry, Sarah Brooks-Achenbach, Nicole C. Barbarich, and ]
			The results of PET studies of the 5-HT<sub>2A</sub> in ] has been mixed.<ref name="pmid11063976">{{cite journal \| vauthors = Fujita M, Charney DS, Innis RB \| title = Imaging serotonergic neurotransmission in depression: hippocampal pathophysiology may mirror global brain alterations \| journal = Biological Psychiatry \| volume = 48 \| issue = 8 \| pages = 801–812 \| date = October 2000 \| pmid = 11063976 \| doi = 10.1016/s0006-3223(00)00960-4 \| s2cid = 10348049 }}</ref>
	\| title = Altered 5-HT<sub>2A</sub> receptor binding after recovery from bulimia-type anorexia nervosa: Relationships to harm avoidance and drive for thinness.
	\| journal = ]
	\| year = 2004
	\| volume = 29
	\| pages = 1143–1155
	\| url = http://www.medical-tribune.at/mm/Bailer_NPP20046.pdf
	\|format=PDF\| doi = 10.1038/sj.npp.1300430
	\| pmid = 15054474
	\| issue = 6
	}}</ref>
	is in line with a SPECT study of anorexia nervosa patients, that found a decrease in frontal, occipital and parietal cortices.<ref name="AudenaertK2003Decreased"/>
	The results of PET studies of the 5-HT<sub>2A</sub> in ] has been mixed.<ref>{{Cite journal
	\| author = Masahiro Fujita, Dennis S. Charneya, c and Robert B. Innis
	\| title = Imaging serotonergic neurotransmission in depression: hippocampal pathophysiology may mirror global brain alterations
	\| journal = ]
	\| volume = 48
	\| issue = 8
	\| month = October
	\| year = 2000
	\| pages = 801–812
	\| doi = 10.1016/S0006-3223(00)00960-4
	\| pmid = 11063976
	}}</ref>

	Altanserin binding has also been examine in ], where one study showed higher correlation between monozygotic twin pairs than between dizygotic twin pairs, giving evidence that the binding is "strongly genetically determined".<ref>{{~~Cite~~ journal		Altanserin binding has also been examine in ], where one study showed higher correlation between monozygotic twin pairs than between dizygotic twin pairs, giving evidence that the binding is "strongly genetically determined".<ref>{{cite journal \| vauthors = Pinborg LH, Arfan H, Haugbol S, Kyvik KO, Hjelmborg JV, Svarer C, Frokjaer VG, Paulson OB, Holm S, Knudsen GM \| display-authors = 6 \| title = The 5-HT2A receptor binding pattern in the human brain is strongly genetically determined \| journal = NeuroImage \| volume = 40 \| issue = 3 \| pages = 1175–1180 \| date = April 2008 \| pmid = 18291676 \| doi = 10.1016/j.neuroimage.2007.09.019 \| s2cid = 9105318 \| author-link1 = Lars H. Pinborg }}</ref>
	\| author = ], ], ], ], ], ], ], ], ] & ]
	\| title = The 5-HT2A receptor binding pattern in the human brain is strongly genetically determined
	\| journal = ]
	\| volume = 40
	\| issue = 3
	\| pages = 1175–1170
	\| year = 2008
	\| month = April
	\| doi = 10.1016/j.neuroimage.2007.09.019
	\| pmid = 18291676
	}}</ref>

	{\| class="wikitable"		{\| class="wikitable"
Line 274:		Line 81:
	! What !! Result !! Reference		! What !! Result !! Reference
	\|-		\|-
	\| ]		\| ]
	\| Higher binding in men		\| Higher binding in men
			\| <ref>{{cite journal \| vauthors = Biver F, Lotstra F, Monclus M, Wikler D, Damhaut P, Mendlewicz J, Goldman S \| title = Sex difference in 5HT2 receptor in the living human brain \| journal = Neuroscience Letters \| volume = 204 \| issue = 1–2 \| pages = 25–28 \| date = February 1996 \| pmid = 8929969 \| doi = 10.1016/0304-3940(96)12307-7 \| s2cid = 43416706 }}</ref>
	\| <ref>{{Cite journal
	\| author = Françoise Biver, Françoise Lotstra, Michel Monclus, David Wikler, Philippe Damhaut, Julien Mendlewicz and Serge Goldman
	\| title = Sex difference in 5HT<sub>2</sub> receptor in the living human brain
	\| journal = ]
	\| volume = 204
	\| issues = 1-2
	\| month = February
	\| year = 1996
	\| pages = 25–28
	\| doi = 10.1016/0304-3940(96)12307-7
	\| pmid = 8929969
	\| issue = 1-2
	}}</ref>
	\|-		\|-
	\| ]		\| ]
	\| Correlation in cortex		\| Correlation in cortex
			\| <ref>{{cite journal \| vauthors = Erritzoe D, Frokjaer VG, Haugbol S, Marner L, Svarer C, Holst K, Baaré WF, Rasmussen PM, Madsen J, Paulson OB, Knudsen GM \| display-authors = 6 \| title = Brain serotonin 2A receptor binding: relations to body mass index, tobacco and alcohol use \| journal = NeuroImage \| volume = 46 \| issue = 1 \| pages = 23–30 \| date = May 2009 \| pmid = 19457377 \| doi = 10.1016/j.neuroimage.2009.01.050 \| author-link10 = Gitte Moos Knudsen \| s2cid = 26525667 }}</ref>
	\| <ref>{{Cite journal
	\| title = Brain serotonin 2A receptor binding: Relations to body mass index, tobacco and alcohol use
	\| author1 = D. Erritzoe
	\| author2 = V.G. Frokjaer
	\| author3 = S. Haugbol
	\| author4 = L. Marner
	\| author5 = C. Svarer
	\| author6 = K. Holst
	\| author7 = W.F.C. Baaré
	\| author8 = P.M. Rasmussen
	\| author9 = J. Madsen
	\| author11 = ]
	\| journal = NeuroImage
	\| volume = 46
	\| issue = 1
	\| month = May
	\| pages = 23–30
	\| doi = 10.1016/j.neuroimage.2009.01.050
	\| pmid = 19457377
	\| year = 2009
	}}</ref>
	\|-		\|-
			\| ] (]) \|\| Increase in frontolimbic region \|\| <ref>{{cite journal \| vauthors = Frokjaer VG, Mortensen EL, Nielsen FA, Haugbol S, Pinborg LH, Adams KH, Svarer C, Hasselbalch SG, Holm S, Paulson OB, Knudsen GM \| display-authors = 6 \| title = Frontolimbic serotonin 2A receptor binding in healthy subjects is associated with personality risk factors for affective disorder \| journal = Biological Psychiatry \| volume = 63 \| issue = 6 \| pages = 569–576 \| date = March 2008 \| pmid = 17884017 \| doi = 10.1016/j.biopsych.2007.07.009 \| s2cid = 25979780 }}</ref>
	\| ] (]) \|\| Increase in frontolimbic region \|\| <ref>{{Cite journal
	\| title = Frontolimbic Serotonin 2A Receptor Binding in Healthy Subjects Is Associated with Personality Risk Factors for Affective Disorder
	\| author = Vibe G. Frøkjær, Erik Lykke Mortensen, Finn Årup Nielsen, Steven Haugbøl, Lars H Pinborg, Karen H. Adams, Claus Svarer, Steen G. Hasselbalch, Søren Holm, ], Gitte Moos Knudsen
	\| journal = ]
	\| doi = 10.1016/j.biopsych.2007.07.009
	\| pmid = 17884017
	\| year = 2008
	\| volume = 63
	\| pages = 569–76
	\| issue = 6
	}}</ref>
	\|-		\|-
			\| ] \|\| Increase \|\| <ref>{{cite journal \| vauthors = Haugbøl S, Pinborg LH, Regeur L, Hansen ES, Bolwig TG, Nielsen FA, Svarer C, Skovgaard LT, Knudsen GM \| display-authors = 6 \| title = Cerebral 5-HT2A receptor binding is increased in patients with Tourette's syndrome \| journal = The International Journal of Neuropsychopharmacology \| volume = 10 \| issue = 2 \| pages = 245–252 \| date = April 2007 \| pmid = 16945163 \| doi = 10.1017/S1461145706006559 \| name-list-style = vanc \| doi-access = free }}</ref>
	\| ] \|\| Increase \|\| <ref>{{Cite journal
	\| author = Steven Haugbøl, Lars H. Pinborg, Lisbeth Regeur, Elsebet S. Hansen, ], Finn Årup Nielsen, Claus Svarer, Lene T. Skovgaardand ]
	\| title = Cerebral 5-HT<sub>2A</sub> receptor binding is increased in patients with Tourette's syndrome
	\| journal = ]
	\| doi = 10.1017/S1461145706006559
	\| year = 2008
	\| volume = 63
	\| pages = 569
	\| pmid = 16945163
	\| issue = 2
	}}</ref>
	\|-		\|-
			\| ] \|\| Increase in ] \|\| <ref>{{cite journal \| vauthors = Adams KH, Hansen ES, Pinborg LH, Hasselbalch SG, Svarer C, Holm S, Bolwig TG, Knudsen GM \| display-authors = 6 \| title = Patients with obsessive-compulsive disorder have increased 5-HT2A receptor binding in the caudate nuclei \| journal = The International Journal of Neuropsychopharmacology \| volume = 8 \| issue = 3 \| pages = 391–401 \| date = September 2005 \| pmid = 15801987 \| doi = 10.1017/S1461145705005055 \| doi-access = free }}</ref>
	\| ] \|\| Increase in ] \|\| <ref>{{Cite journal
	\| author = K. H. Adams, E. S. Hansen, L. H. Pinborg, S. G. Hasselbalch, C. Svarer, S. Holm, ] & ]
	\| title = Patients with obsessive-compulsive disorder have increased 5-HT<sub>2A</sub> receptor binding in the caudate nuclei
	\| journal = ]
	\| year = 2005
	\| month = September
	\| volume = 8
	\| issue = 3
	\| pages = 391–401
	\| pmid = 15801987
	\| doi = 10.1017/S1461145705005055
	}}</ref>
	\|-		\|-
	\| (Recovered) ]-type ]		\| (Recovered) ]-type ]
	\| Decrease in left ], left ] and right ]		\| Decrease in left ], left ] and right ]
	\| <ref name="~~BailerU2004Altered~~"/>		\| <ref name="pmid15054474" />
	\|-		\|-
	\| ]		\| ]
	\| Decrease in a region in right hemisphere (posterolateral ] and the anterior ])		\| Decrease in a region in right hemisphere (posterolateral ] and the anterior ])
			\| <ref>{{cite journal \| vauthors = Biver F, Wikler D, Lotstra F, Damhaut P, Goldman S, Mendlewicz J \| title = Serotonin 5-HT2 receptor imaging in major depression: focal changes in orbito-insular cortex \| journal = The British Journal of Psychiatry \| volume = 171 \| issue = 5 \| pages = 444–448 \| date = November 1997 \| pmid = 9463603 \| doi = 10.1192/bjp.171.5.444 \| s2cid = 38577128 }}</ref>
	\| <ref>{{Cite journal
	\| author = F. Biver, D. Wikler, F. Lotstra, P. Damhaut, S. Goldman, J. Mendlewicz
	\| title = Serotonin 5-HT2 receptor imaging in major depression: focal changes in orbito-insular cortex
	\| journal = ]
	\| year = 1997
	\| month = November
	\| volume = 171
	\| pages = 444–448
	\| pmid = 9463603
	\| doi = 10.1192/bjp.171.5.444
	}}</ref>
	\|-		\|-
	\| ]		\| ]
	\| Decrease in ]		\| Decrease in ]
			\| <ref>{{cite journal \| vauthors = Mintun MA, Sheline YI, Moerlein SM, Vlassenko AG, Huang Y, Snyder AZ \| title = Decreased hippocampal 5-HT2A receptor binding in major depressive disorder: in vivo measurement with altanserin positron emission tomography \| journal = Biological Psychiatry \| volume = 55 \| issue = 3 \| pages = 217–224 \| date = February 2004 \| pmid = 14744461 \| doi = 10.1016/j.biopsych.2003.08.015 \| s2cid = 24849671 \| author-link5 = Abraham Z. Snyder \| author-link1 = Mark A. Mintun }}</ref>
	\| <ref>{{Cite journal
	\| author = ], Yvette I. Sheline, Stephen M. Moerlein, Andrei G. Vlassenko, Yiyun Huang and ]
	\| title = Decreased hippocampal 5-HT2A receptor binding in major depressive disorder: in vivo measurement with altanserin positron emission tomography
	\| journal = ]
	\| volume = 55
	\| issue = 3
	\| month = February
	\| year = 2004
	\| pages = 217–224
	\| doi = 10.1016/j.biopsych.2003.08.015
	\| pmid=14744461
	}}</ref>
	\|-		\|-
	\| Older depressed patients		\| Older depressed patients
	\| Decrease in ]		\| Decrease in ]
			\| <ref>{{cite journal \| vauthors = Sheline YI, Mintun MA, Barch DM, Wilkins C, Snyder AZ, Moerlein SM \| title = Decreased hippocampal 5-HT(2A) receptor binding in older depressed patients using altanserin positron emission tomography \| journal = Neuropsychopharmacology \| volume = 29 \| issue = 12 \| pages = 2235–2241 \| date = December 2004 \| pmid = 15367923 \| doi = 10.1038/sj.npp.1300555 \| s2cid = 1727523 \| doi-access = free }}</ref>
	\| <ref>{{Cite journal
	\| author = Yvette I. Sheline, ], Deanna M. Barch, Consuelo Wilkins, Abraham Z. Snyder & Stephen M. Moerlein
	\| title = Decreased hippocampal 5-HT<sub>2A</sub> receptor binding in older depressed patients using altanserin positron emission tomography
	\| journal = ]
	\| year = 2004
	\| month = December
	\| volume = 29
	\| issue = 12
	\| pages = 2235–2241
	\| url = http://www.nature.com/npp/journal/v29/n12/abs/1300555a.html
	\| doi = 10.1038/sj.npp.1300555
	\| pmid = 15367923
	}}</ref>
	\|-		\|-
	\| ] \|\| Increase in ]		\| ] \|\| Increase in ]
			\| <ref>{{cite journal \| vauthors = Soloff PH, Price JC, Meltzer CC, Fabio A, Frank GK, Kaye WH \| title = 5HT2A receptor binding is increased in borderline personality disorder \| journal = Biological Psychiatry \| volume = 62 \| issue = 6 \| pages = 580–587 \| date = September 2007 \| pmid = 17448449 \| doi = 10.1016/j.biopsych.2006.10.022 \| s2cid = 12109806 }}</ref>
	\| <ref>{{Cite journal
	\| title = 5HT2A Receptor Binding is Increased in Borderline Personality Disorder
	\| author = P. Soloff, J. Price, C. Meltzer, A. Fabio, G. Frank, W. Kaye
	\| journal = ]
	\| volume = 62
	\| issue = 6
	\| pages = 580–587
	\| doi = 10.1016/j.biopsych.2006.10.022
	\| year = 2007
	\| pmid = 17448449
	}}</ref>
	\|-		\|-
	\| ]		\| ]
	\| No significant cortical difference, higher binding in ]		\| No significant cortical difference, higher binding in ]
			\| <ref>{{cite journal \| vauthors = Erritzoe D, Rasmussen H, Kristiansen KT, Frokjaer VG, Haugbol S, Pinborg L, Baaré W, Svarer C, Madsen J, Lublin H, Knudsen GM, Glenthoj BY \| display-authors = 6 \| title = Cortical and subcortical 5-HT2A receptor binding in neuroleptic-naive first-episode schizophrenic patients \| journal = Neuropsychopharmacology \| volume = 33 \| issue = 10 \| pages = 2435–2441 \| date = September 2008 \| pmid = 18288096 \| doi = 10.1038/sj.npp.1301656 \| s2cid = 7596368 \| doi-access = free }} Electronic publication ahead of print</ref>
	\| <ref>{{Cite journal
	\| author = David Erritzoe, Hans Rasmussen, Klaus T. Kristiansen, Vibe G. Frøkjær, Steven Haugbøl, Lars Pinborg, William Baaré, Claus Svarer, Jacob Madsen, Henrik Lublin, ] & Birte Y. Glenthøj
	\| title = Cortical and Subcortical 5-HT<sub>2A</sub> Receptor Binding in Neuroleptic-Naive First-Episode Schizophrenic Patients
	\| journal = ]
	\| year = 2008
	\| month = February
	\| doi = 10.1038/sj.npp.1301656
	\| pmid = 18288096
	\| volume = 62
	\| pages = 580
	\| issue = 10
	}} Electronic publication ahead of print</ref>
	\|-		\|-
	\| ]		\| ]
	\| Decrease		\| Decrease
			\| <ref>{{cite journal \| vauthors = Hurlemann R, Matusch A, Kuhn KU, Berning J, Elmenhorst D, Winz O, Kolsch H, Zilles K, Wagner M, Maier W, Bauer A \| display-authors = 6 \| title = 5-HT2A receptor density is decreased in the at-risk mental state \| journal = Psychopharmacology \| volume = 195 \| issue = 4 \| pages = 579–590 \| date = January 2008 \| pmid = 17899021 \| doi = 10.1007/s00213-007-0921-x \| s2cid = 7784253 \| author-link8 = Karl Zilles }}</ref> See also <ref>{{cite journal \| vauthors = Hurlemann R, Boy C, Meyer PT, Scherk H, Wagner M, Herzog H, Coenen HH, Vogeley K, Falkai P, Zilles K, Maier W, Bauer A \| display-authors = 6 \| title = Decreased prefrontal 5-HT2A receptor binding in subjects at enhanced risk for schizophrenia \| journal = Anatomy and Embryology \| volume = 210 \| issue = 5–6 \| pages = 519–523 \| date = December 2005 \| pmid = 16187138 \| doi = 10.1007/s00429-005-0036-2 \| author-link10 = Karl Zilles \| s2cid = 4113675 }}</ref>
	\| <ref>{{Cite journal
	\| author = René Hurlemann, Andreas Matusch, Kai-Uwe Kuhn, Julia Berning, David Elmenhorst, Oliver Winz, Heike Kolsch, ], Michael Wagner, Wolfgang Maier and Andreas Bauer
	\| title = 5-HT<sub>2A</sub> receptor density is decreased in the at-risk mental state
	\| journal = ]
	\| year = 2008
	\| month = January
	\| volume = 195
	\| issue = 4
	\| pages = 579–590
	\| pmid = 17899021
	\| doi = 10.1007/s00213-007-0921-x
	}}</ref> See also <ref>{{Cite journal
	\| author = René Hurlemann, Christian Boy, Philipp T. Meyer, Harald Scherk, Michael Wagner, Hans Herzog, Heinz H. Coenen, Kai Vogeley, Peter Falkai, ], Wolfgang Maier and Andreas Bauer
	\| title = Decreased prefrontal 5-HT2A receptor binding in subjects at enhanced risk for schizophrenia
	\| journal = ]
	\| year = 2005
	\| month = December
	\| volume = 210
	\| issue = 5-6
	\| pages = 519–523
	\| pmid = 16187138
	\| url = http://www.springerlink.com/content/p283r20161447148/
	\| doi = 10.1007/s00429-005-0036-2
	}}</ref>
	\|-		\|-
	\| ] \|\| Decrease		\| ] \|\| Decrease
			\| <ref>{{cite journal \| vauthors = Rosier A, Dupont P, Peuskens J, Bormans G, Vandenberghe R, Maes M, de Groot T, Schiepers C, Verbruggen A, Mortelmans L \| display-authors = 6 \| title = Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using altanserin and positron emission tomographic imaging \| journal = Psychiatry Research \| volume = 68 \| issue = 1 \| pages = 11–22 \| date = November 1996 \| pmid = 9027929 \| doi = 10.1016/S0925-4927(96)02806-5 \| s2cid = 32317795 }}</ref>
	\| <ref>{{Cite journal
	\| author = A. Rosier, P. Dupont, J. Peuskens, G. Bormans, R. Vandenberghe, M. Maes, T. de Groot, C. Schiepers, A. Verbruggen, L. Mortelmans
	\| title = Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using altanserin and positron emission tomographic imaging
	\| journal = ]
	\| year = 1996
	\| month = November
	\| volume = 68
	\| issue = 1
	\| pages = 11–22
	\| pmid = 9027929
	\| doi = 10.1016/S0925-4927(96)02806-5
	}}</ref>
	\|-		\|-
	\| ]		\| ]
	\| Decrease		\| Decrease
			\| <ref>{{cite journal \| vauthors = Meltzer CC, Smith G, Price JC, Reynolds CF, Mathis CA, Greer P, Lopresti B, Mintun MA, Pollock BG, Ben-Eliezer D, Cantwell MN, Kaye W, DeKosky ST \| display-authors = 6 \| title = Reduced binding of altanserin to serotonin type 2A receptors in aging: persistence of effect after partial volume correction \| journal = Brain Research \| volume = 813 \| issue = 1 \| pages = 167–171 \| date = November 1998 \| pmid = 9824691 \| doi = 10.1016/S0006-8993(98)00909-3 \| author-link13 = Steven T. DeKosky \| s2cid = 21884218 \| author-link8 = Mark A. Mintun }}</ref>
	\| <ref>{{Cite journal
	\| author = Carolyn Cidis Meltzer, Gwenn Smith, Julie C. Price, Charles F. Reynolds III, Chester A. Mathis, , Phil Greer, Brian Lopresti, ], Bruce G. Pollock, Doron Ben-Eliezer, Michael N. Cantwell, Walter Kaye and ]
	\| title = Reduced binding of altanserin to serotonin type 2A receptors in aging: persistence of effect after partial volume correction
	\| journal = ]
	\| volume = 813
	\| issue = 1
	\| month = November
	\| year = 1998
	\| pages = 167–171
	\| doi = 10.1016/S0006-8993(98)00909-3
	\| pmid=9824691
	}}</ref>
	\|-		\|-
	\| ]		\| ]
	\| Decrease in ] regions (except ]), increase in ]		\| Decrease in ] regions (except ]), increase in ]
			\| <ref>{{cite journal \| vauthors = Adams KH, Pinborg LH, Svarer C, Hasselbalch SG, Holm S, Haugbøl S, Madsen K, Frøkjaer V, Martiny L, Paulson OB, Knudsen GM \| display-authors = 6 \| title = A database of -altanserin binding to 5-HT(2A) receptors in normal volunteers: normative data and relationship to physiological and demographic variables \| journal = NeuroImage \| volume = 21 \| issue = 3 \| pages = 1105–1113 \| date = March 2004 \| pmid = 15006678 \| doi = 10.1016/j.neuroimage.2003.10.046 \| s2cid = 24403109 }}</ref>
	\| <ref>{{Cite journal
	\| author = K. H. Adams, Lars H. Pinborg, Claus Svarer, S. G. Hasselbalch, Søren Holm, S. Haugbøl, K. Madsen, Vibe G. Frøkjaer, L. Martiny, ], ]
	\| title = A database of -altanserin binding to 5-HT<sub>2A</sub> receptors in normal volunteers: normative data and relationship to physiological and demographic variables
	\| journal = ]
	\| year = 2004
	\| month = March
	\| volume = 21
	\| issue = 3
	\| pages = 1105–1113
	\| pmid = 15006678
	\| doi = 10.1016/j.neuroimage.2003.10.046
	}}</ref>
	\|-		\|-
	\| ]		\| ]
	\| Decrease		\| Decrease
	\| <ref>{{~~Cite~~ journal \| ~~title= Reduced 5-HT<sub>2A</sub> receptor binding in patients with mild cognitive impairment\| author~~ = Hasselbalch SG, Madsen K, Svarer C, Pinborg LH, Holm S, ], Waldemar G, ~~Gitte~~ ~~Moos~~ ~~Knudsen~~ \| journal = ] \| ~~year~~ = ~~2007~~ \| pmid = 17544547 \| doi= 10.1016/j.neurobiolaging.2007.04.011 \| ~~volume=~~ ~~29 \| pages~~= ~~1830–8 \| issue= 12~~ }}</ref>		\| <ref>{{cite journal \| vauthors = Hasselbalch SG, Madsen K, Svarer C, Pinborg LH, Holm S, Paulson OB, Waldemar G, Knudsen GM \| display-authors = 6 \| title = Reduced 5-HT2A receptor binding in patients with mild cognitive impairment \| journal = Neurobiology of Aging \| volume = 29 \| issue = 12 \| pages = 1830–1838 \| date = December 2008 \| pmid = 17544547 \| doi = 10.1016/j.neurobiolaging.2007.04.011 \| s2cid = 23665678 }}</ref>
	\|-		\|-
	\| ]		\| ]
	\| Decrease in ]-] complex and cortical regions, such as ], ], ] and ]		\| Decrease in ]-] complex and cortical regions, such as ], ], ] and ]
			\| <ref>{{cite journal \| vauthors = Meltzer CC, Price JC, Mathis CA, Greer PJ, Cantwell MN, Houck PR, Mulsant BH, Ben-Eliezer D, Lopresti B, DeKosky ST, Reynolds CF \| display-authors = 6 \| title = PET imaging of serotonin type 2A receptors in late-life neuropsychiatric disorders \| journal = The American Journal of Psychiatry \| volume = 156 \| issue = 12 \| pages = 1871–1878 \| date = December 1999 \| pmid = 10588399 \| doi = 10.1176/ajp.156.12.1871 \| s2cid = 7678215 }}</ref>
	\| <ref>{{Cite journal
	\| author = Carolyn Cidis Meltzer, Julie C. Price, Chester A. Mathis, Phil J. Greer, Michael N. Cantwell, Patricia R. Houck, Benoit H. Mulsant, Doron Ben-Eliezer, Brian Lopresti, Steven T. DeKosky, and Charles F. Reynolds, III
	\| title = PET Imaging of Serotonin Type 2A Receptors in Late-Life Neuropsychiatric Disorders
	\| journal = ]
	\| volume = 156
	\| pages = 1871–1878
	\| url = http://ajp.psychiatryonline.org/cgi/content/abstract/156/12/1871
	\| pmid = 10588399
	\| issue = 12
	\| date = December 1, 1999 }}</ref>
	\|}		\|}

			==Synthesis==
			altanserin for human PET imaging by a new work-up procedure \| journal = Applied Radiation and Isotopes \| volume = 67 \| issue = 11 \| pages = 2040–2043 \| date = November 2009 \| pmid = 19692252 \| doi = 10.1016/j.apradiso.2009.07.020 }}</ref><ref name="pmid14516599">{{cite journal \| vauthors = Monclus M, Van Naemen J, Mulleneers E, Damhaut P, Luxen A, Goldman S \| title = Automatic Synthesis of Altanserin, a Radiopharmaceutical for Positron Emission Tomographic Studies of the Serotonergic Type-2 Receptors \| journal = Clinical Positron Imaging \| volume = 1 \| issue = 2 \| pages = 111–116 \| date = March 1998 \| pmid = 14516599 \| doi = 10.1016/s1095-0397(98)00005-3 \| hdl = 2268/144402 \| hdl-access = free }}</ref><ref name="TanBaldwin1999" />]]

			The reaction of 4-(4-fluorobenzoyl)piperidine ('''1''') with 2-bromoethylamine gives -(4-fluorophenyl)methanone ('''2'''). The reaction of the terminal amino group with thiophosgene leads to the corresponding isothiocyanate derivative, 4-fluorophenyl 1-(2-isothiocyanatoethyl)piperidin-4-yl ketone ('''3'''). Upon reaction of this reactive intermediate with ethyl anthranilate ('''4'''), the transient addition product might be expected to be initially formed ('''5''''). An intramolecular lactamization to the heterocyclic ring then occurs giving altanserin ('''6''').

			== See also ==
			* ]
			* ]
			* ]

	== References ==		== References ==
	{{Reflist}}		{{Reflist\|2}}

			{{Serotonin receptor modulators}}
	{{Serotonergics}}

	]		]
	]		]
	]
	]		]
			]
			]
	]		]
	]		]
	]
	]		]

Latest revision as of 13:50, 5 September 2024

Chemical compound Pharmaceutical compound

Altanserin
Clinical data

ATC code	none
Identifiers
IUPAC name 3-ethyl]-2-sulfanylidene-1H-quinazolin-4-one
CAS Number	76330-71-7
PubChem CID	3033677
ChemSpider	2298299
UNII	5015H744JQ
ChEMBL	ChEMBL62919
CompTox Dashboard (EPA)	DTXSID5043891
ECHA InfoCard	100.071.272
Chemical and physical data
Formula	C₂₂H₂₂FN₃O₂S
Molar mass	411.50 g·mol
3D model (JSmol)	Interactive image
SMILES Fc1ccc(cc1)C(=O)C4CCN(CCN3C(=O)c2ccccc2NC3=S)CC4
InChI InChI=1S/C22H22FN3O2S/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29) Key:SMYALUSCZJXWHG-UHFFFAOYSA-N
(verify)

Altanserin is a compound that binds to the 5-HT_2A receptor (5-Hydroxytryptamine (serotonin) 2A receptor). Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain, i.e., studies of the 5-HT_2A neuroreceptors. Besides human neuroimaging studies altanserin has also been used in the study of rats.

An alternative for PET imaging the 5-HT_2A receptor is the [C]volinanserin (MDL-100,907) radioligand. F-altanserin and H-volinanserin have shown very comparable binding. Both altanserin and MDL 100,907 are 5-HT_2A receptor antagonists. -setoperone can also be used in PET.

An alternative SPECT radioligand is the -5-I-R91150 receptor antagonist.

A rapid chemical synthesis of fluorine-18 and H-2 dual-labeled altanserin has been described.

Other ligands for other parts of the serotonin system used in PET studies are, e.g., DASB, ketanserin, and WAY-100635.

Human brain mapping studies with altanserin

A PET scanner. Human experiments with fluorine-18 altanserin are performed in these types of brain scanners.

As of 2007 altanserin is probably not used in clinical routine. However, there have been performed several research-based neuroimaging studies with the compound in humans since the 1990s. Some of these studies have considered methodogical issues such as the reproducibility of the method or whether to use constant infusion or bolus-infusion delivery of altanserin. Other studies have compared altanserin binding to subject variables such as age, personality trait and neuropsychiatric disorder.

The altanserin PET scan shows high binding in neocortex. The cerebellum is often regarded as a region with no specific 5-HT_2A binding and the brain region is used as a reference in some studies, even though an autoradiography study has found nonnegligible levels of 5-HT_2A binding in the human cerebellum, and another type of study have observed strong immunoreaction against 5-HT_2A receptor protein in rat Purkinje cells.

In the table below is an overview of the results of altanserin binding seen in human PET-studies. A consistent finding across altanserin studies has been that the binding decreases with age. This is in line with in vitro studies of the 5-HT_2A receptor, as well as PET studies with other radioligands that binds to the receptor.

The result for recovered bulimia-type anorexia nervosa is in line with a SPECT study of anorexia nervosa patients, that found a decrease in frontal, occipital and parietal cortices. The results of PET studies of the 5-HT_2A in depression has been mixed.

Altanserin binding has also been examine in twins, where one study showed higher correlation between monozygotic twin pairs than between dizygotic twin pairs, giving evidence that the binding is "strongly genetically determined".

Altanserin neuroimaging studies
What	Result	Reference
Gender	Higher binding in men
Body mass index	Correlation in cortex
Neuroticism (NEO PI-R)	Increase in frontolimbic region
Tourette syndrome	Increase
Obsessive-compulsive disorder	Increase in caudate nuclei
(Recovered) bulimia-type anorexia nervosa	Decrease in left subgenual cingulate, left parietal cortex and right occipital cortex
Unipolar depression	Decrease in a region in right hemisphere (posterolateral orbitofrontal cortex and the anterior insular cortex)
Major depressive disorder	Decrease in hippocampus
Older depressed patients	Decrease in hippocampus
Borderline personality disorder	Increase in hippocampus
Schizophrenia	No significant cortical difference, higher binding in caudate
At-risk mental state	Decrease	See also
Age	Decrease
Age	Decrease
Age	Decrease in cortical regions (except occipital), increase in cerebellum
Mild cognitive impairment	Decrease
Alzheimer's disease	Decrease in amygdalo-hippocampal complex and cortical regions, such as anterior cingulate, lateral temporal cortex, prefrontal cortex and sensorimotor cortex

Synthesis

The reaction of 4-(4-fluorobenzoyl)piperidine (1) with 2-bromoethylamine gives -(4-fluorophenyl)methanone (2). The reaction of the terminal amino group with thiophosgene leads to the corresponding isothiocyanate derivative, 4-fluorophenyl 1-(2-isothiocyanatoethyl)piperidin-4-yl ketone (3). Upon reaction of this reactive intermediate with ethyl anthranilate (4), the transient addition product might be expected to be initially formed (5'). An intramolecular lactamization to the heterocyclic ring then occurs giving altanserin (6).

References

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Rosier A, Dupont P, Peuskens J, Bormans G, Vandenberghe R, Maes M, et al. (November 1996). "Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using altanserin and positron emission tomographic imaging". Psychiatry Research. 68 (1): 11–22. doi:10.1016/S0925-4927(96)02806-5. PMID 9027929. S2CID 32317795.
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EP0013612 idem Jan Vandenberk, Ludo Kennis, Marcel Van der Aa, Albert Van Heertum, U.S. patent 4,522,945 (1985 to Janssen Pharmaceutica N.V.).
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Serotonin receptor modulators

5-HT₁

5-HT_1A

Agonists: 8-OH-DPAT Adatanserin Amphetamine Antidepressants (e.g., etoperidone, hydroxynefazodone, nefazodone, trazodone, triazoledione, vilazodone, vortioxetine) Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, lurasidone, quetiapine, ziprasidone) Azapirones (e.g., buspirone, eptapirone, gepirone, perospirone, tandospirone) Bay R 1531 Befiradol BMY-14802 Cannabidiol Dimemebfe Dopamine Ebalzotan Eltoprazine Enciprazine Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, lisuride, LSD, methylergometrine (methylergonovine), methysergide, pergolide) F-11,461 F-12826 F-13714 F-14679 F-15063 F-15,599 Flesinoxan Flibanserin Flumexadol Hypidone Lesopitron LY-293284 LY-301317 mCPP MKC-242 Naluzotan NBUMP Osemozotan Oxaflozane Pardoprunox Piclozotan Rauwolscine Repinotan Roxindole RU-24,969 S-14,506 S-14671 S-15535 Sarizotan Serotonin (5-HT) SSR-181507 Sunepitron Tryptamines (e.g., 5-CT, 5-MeO-DMT, 5-MT, bufotenin, DMT, indorenate, N-Me-5-HT, psilocin, psilocybin) TGBA01AD U-92,016-A Urapidil Vilazodone Xaliproden Yohimbine
Antagonists: Atypical antipsychotics (e.g., iloperidone, risperidone, sertindole) AV965 Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, pindolol, propranolol, tertatolol) BMY-7,378 CSP-2503 Dotarizine Ergolines (e.g., metergoline) FCE-24379 Flopropione GR-46611 Isamoltane Lecozotan Mefway Metitepine (methiothepin) MIN-117 (WF-516) MPPF NAN-190 Robalzotan S-15535 SB-649,915 SDZ 216-525 Spiperone Spiramide Spiroxatrine UH-301 WAY-100135 WAY-100635 Xylamidine
Unknown/unsorted: Acetryptine Carvedilol Ergolines (e.g., ergometrine (ergonovine))

5-HT_1B

Agonists: Anpirtoline CGS-12066A CP-93129 CP-94253 CP-122,288 CP-135807 Eltoprazine Ergolines (e.g., bromocriptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide) mCPP RU-24,969 Serotonin (5-HT) Triptans (e.g., avitriptan, donitriptan, eletriptan, sumatriptan, zolmitriptan) TFMPP Tryptamines (e.g., 5-BT, 5-CT, 5-MT, DMT) Vortioxetine
Antagonists: AR-A000002 Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, tertatolol) Elzasonan Ergolines (e.g., metergoline) GR-127935 Isamoltane LY-393558 Metitepine (methiothepin) SB-216641 SB-224289 SB-236057 Yohimbine
Unknown/unsorted: Ergolines (e.g., cabergoline, ergometrine (ergonovine), lisuride)

5-HT_1D

Agonists: CP-122,288 CP-135807 CP-286601 Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, LSD, methysergide) GR-46611 L-694247 L-772405 mCPP PNU-109291 PNU-142633 Serotonin (5-HT) TGBA01AD Triptans (e.g., almotriptan, avitriptan, donitriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan) Tryptamines (e.g., 5-BT, 5-CT, 5-Et-DMT, 5-MT, 5-(nonyloxy)tryptamine, DMT)
Antagonists: Alniditan BRL-15,572 Elzasonan Ergolines (e.g., metergoline) GR-127935 Ketanserin LY-310762 LY-367642 LY-393558 LY-456219 LY-456220 Metitepine (methiothepin) Mianserin Ritanserin Yohimbine Ziprasidone
Unknown/unsorted: Acetryptine Ergolines (e.g., lisuride, lysergol, pergolide)

5-HT_1E

Agonists: BRL-54443 Ergolines (e.g., methysergide) Serotonin (5-HT) Triptans (e.g., eletriptan) Tryptamines (e.g., tryptamine)
Antagonists: Metitepine (methiothepin)
Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine), lysergol, methylergometrine (methylergonovine)

5-HT_1F

Agonists: BRL-54443 CP-122,288 Ergolines (e.g., bromocriptine, lysergol, methylergometrine (methylergonovine) methysergide) Lasmiditan LY-334370 Serotonin (5-HT) Triptans (e.g., eletriptan, naratriptan, sumatriptan) Tryptamines (e.g., 5-MT)
Antagonists: Metitepine (methiothepin) Mianserin

5-HT₂

5-HT_2A

Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN-NBOH, 2CBFly-NBOMe) 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) 2C-B-FLY 2CB-Ind 5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT) α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT) AL-34662 AL-37350A Bromo-DragonFLY Dimemebfe DMBMPP DOx (e.g., DOB, DOC, DOI, DOM) Efavirenz Ergolines (e.g., 1P-LSD, ALD-52, bromocriptine, cabergoline, ergine (LSA), ergometrine (ergonovine), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, methylergometrine (methylergonovine), pergolide) Flumexadol IHCH-7113 Jimscaline Lorcaserin MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA) O-4310 Oxaflozane PHA-57378 PNU-22394 PNU-181731 RH-34 SCHEMBL5334361 Phenethylamines (e.g., lophophine, mescaline) Piperazines (e.g., BZP, quipazine, TFMPP) Serotonin (5-HT) TCB-2 TFMFly Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)
Antagonists: 5-I-R91150 5-MeO-NBpBrT AC-90179 Adatanserin Altanserin Antihistamines (e.g., cyproheptadine, hydroxyzine, ketotifen, perlapine) AMDA Atypical antipsychotics (e.g., amperozide, aripiprazole, asenapine, blonanserin, brexpiprazole, carpipramine, clocapramine, clorotepine, clozapine, fluperlapine, gevotroline, iloperidone, lurasidone, melperone, mosapramine, ocaperidone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, zicronapine, ziprasidone, zotepine) Chlorprothixene Cinanserin CSP-2503 Deramciclane Dotarizine Eplivanserin Ergolines (e.g., amesergide, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole) Fananserin Flibanserin Glemanserin Irindalone Ketanserin KML-010 Landipirdine LY-393558 mCPP Medifoxamine Metitepine (methiothepin) MIN-117 (WF-516) Naftidrofuryl Nantenine Nelotanserin Opiranserin (VVZ-149) Pelanserin Phenoxybenzamine Pimavanserin Pirenperone Pizotifen Pruvanserin Rauwolscine Ritanserin Roluperidone S-14671 Sarpogrelate Serotonin antagonists and reuptake inhibitors (e.g., etoperidone, hydroxynefazodone, lubazodone, mepiprazole, nefazodone, triazoledione, trazodone) SR-46349B TGBA01AD Teniloxazine Temanogrel Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine) Tricyclic antidepressants (e.g., amitriptyline) Typical antipsychotics (e.g., chlorpromazine, fluphenazine, haloperidol, loxapine, perphenazine, pimozide, pipamperone, prochlorperazine, setoperone, spiperone, spiramide, thioridazine, thiothixene, trifluoperazine) Volinanserin Xylamidine Yohimbine
Unknown/unsorted: Ergolines (e.g., dihydroergotamine, nicergoline)

5-HT_2B

Agonists: 4-Methylaminorex Aminorex Amphetamines (e.g., chlorphentermine, cloforex, dexfenfluramine, fenfluramine, levofenfluramine, norfenfluramine) BW-723C86 DOx (e.g., DOB, DOC, DOI, DOM) Ergolines (e.g., cabergoline, dihydroergocryptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide) Lorcaserin MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA) Piperazines (e.g., TFMPP) PNU-22394 Ro60-0175 Serotonin (5-HT) Tryptamines (e.g., 5-BT, 5-CT, 5-MT, α-Me-5-HT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)
Antagonists: Agomelatine Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, N-desalkylquetiapine (norquetiapine), N-desmethylclozapine (norclozapine), olanzapine, pipamperone, quetiapine, risperidone, ziprasidone) Cyproheptadine EGIS-7625 Ergolines (e.g., amesergide, bromocriptine, lisuride, LY-53857, LY-272015, mesulergine) Ketanserin LY-393558 mCPP Metadoxine Metitepine (methiothepin) Pirenperone Pizotifen Propranolol PRX-08066 Rauwolscine Ritanserin RS-127445 Sarpogrelate SB-200646 SB-204741 SB-206553 SB-215505 SB-221284 SB-228357 SDZ SER-082 Tegaserod Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine) Trazodone Typical antipsychotics (e.g., chlorpromazine) TIK-301 Yohimbine
Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine))

5-HT_2C

Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) 5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT) α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT) A-372159 AL-38022A Alstonine CP-809101 Dimemebfe DOx (e.g., DOB, DOC, DOI, DOM) Ergolines (e.g., ALD-52, cabergoline, dihydroergotamine, ergine (LSA), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, pergolide) Flumexadol Lorcaserin MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA) MK-212 ORG-12962 ORG-37684 Oxaflozane PHA-57378 Phenethylamines (e.g., lophophine, mescaline) Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP) PNU-22394 PNU-181731 Ro60-0175 Ro60-0213 Serotonin (5-HT) Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine) Vabicaserin WAY-629 WAY-161503 YM-348
Antagonists: Adatanserin Agomelatine Atypical antipsychotics (e.g., asenapine, clorotepine, clozapine, fluperlapine, iloperidone, melperone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, ziprasidone, zotepine) Captodiame CEPC Cinanserin Cyproheptadine Deramciclane Desmetramadol Dotarizine Eltoprazine Ergolines (e.g., amesergide, bromocriptine, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole) Etoperidone Fluoxetine FR-260010 Irindalone Ketanserin Ketotifen Latrepirdine (dimebolin) Medifoxamine Metitepine (methiothepin) Nefazodone Pirenperone Pizotifen Propranolol Ritanserin RS-102221 S-14671 SB-200646 SB-206553 SB-221284 SB-228357 SB-242084 SB-243213 SDZ SER-082 Tedatioxetine Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine) TIK-301 Tramadol Trazodone Tricyclic antidepressants (e.g., amitriptyline, nortriptyline) Typical antipsychotics (e.g., chlorpromazine, loxapine, pimozide, pipamperone, thioridazine) Xylamidine
Unknown/unsorted: Efavirenz Ergolines (e.g., ergometrine (ergonovine), methylergometrine (methylergonovine))

5-HT₃_–7

5-HT₃

Agonists: Alcohols (e.g., butanol, ethanol (alcohol), trichloroethanol) m-CPBG Phenylbiguanide Piperazines (e.g., BZP, mCPP, quipazine) RS-56812 Serotonin (5-HT) SR-57227 SR-57227A Tryptamines (e.g., 2-Me-5-HT, 5-CT, bufotenidine (5-HTQ)) Volatiles/gases (e.g., halothane, isoflurane, toluene, trichloroethane) YM-31636
Antagonists: Alosetron Anpirtoline Arazasetron AS-8112 Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine) Azasetron Batanopride Bemesetron (MDL-72222) Bupropion Cilansetron CSP-2503 Dazopride Dolasetron Galanolactone Granisetron Hydroxybupropion Lerisetron Memantine Ondansetron Palonosetron Ramosetron Renzapride Ricasetron Tedatioxetine Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine) Thujone Tropanserin Tropisetron Typical antipsychotics (e.g., loxapine) Volatiles/gases (e.g., nitrous oxide, sevoflurane, xenon) Vortioxetine Zacopride Zatosetron
Unknown/unsorted: LY-53857 Piperazines (e.g., naphthylpiperazine)

5-HT₄

Agonists: 5-MT BIMU8 Capeserod Cinitapride Cisapride CJ-033466 Dazopride Metoclopramide Minesapride Mosapride Prucalopride PRX-03140 Renzapride RS-67,333 RS-67,506 Serotonin (5-HT) Tegaserod Usmarapride Velusetrag Zacopride
Antagonists: GR-113808 GR-125487 L-Lysine Piboserod RS-39604 RS-67532 SB-203186 SB-204070

5-HT_5A

Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD)
Serotonin (5-HT)
Tryptamines (e.g., 5-CT)
Valerenic acid

Unknown/unsorted: Ergolines (e.g., metergoline, methysergide)
Piperazines (e.g., naphthylpiperazine)

5-HT₆

Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, methysergide) Hypidone Serotonin (5-HT) Tryptamines (e.g., 2-Me-5-HT, 5-BT, 5-CT, 5-MT, Bufotenin, E-6801, E-6837, EMD-386088, EMDT, LY-586713, N-Me-5-HT, ST-1936, tryptamine) WAY-181187 WAY-208466
Antagonists: ABT-354 Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, iloperidone, olanzapine, tiospirone) AVN-101 AVN-211 AVN-322 AVN-397 BGC20-760 BVT-5182 BVT-74316 Cerlapirdine EGIS-12,233 GW-742457 Idalopirdine Ketanserin Landipirdine Latrepirdine (dimebolin) Masupirdine Metitepine (methiothepin) MS-245 PRX-07034 Ritanserin Ro 04-6790 Ro 63-0563 SB-258585 SB-271046 SB-357134 SB-399885 SB-742457 Tetracyclic antidepressants (e.g., amoxapine, mianserin) Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, nortriptyline) Typical antipsychotics (e.g., chlorpromazine, loxapine)
Unknown/unsorted: Ergolines (e.g., 2-Br-LSD (BOL-148), bromocriptine, lergotrile, pergolide) Piperazines (e.g., naphthylpiperazine)

5-HT₇

Agonists: 8-OH-DPAT AS-19 Bifeprunox E-55888 Ergolines (e.g., LSD) LP-12 LP-44 LP-211 RU-24,969 Sarizotan Serotonin (5-HT) Triptans (e.g., frovatriptan) Tryptamines (e.g., 5-CT, 5-MT, bufotenin, N-Me-5-HT)
Antagonists: Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, clorotepine, clozapine, fluperlapine, olanzapine, risperidone, sertindole, tiospirone, ziprasidone, zotepine) Butaclamol DR-4485 EGIS-12,233 Ergolines (e.g., 2-Br-LSD (BOL-148), amesergide, bromocriptine, cabergoline, dihydroergotamine, ergotamine, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole) JNJ-18038683 Ketanserin LY-215,840 Metitepine (methiothepin) Ritanserin SB-258719 SB-258741 SB-269970 SB-656104 SB-656104A SB-691673 SLV-313 SLV-314 Spiperone SSR-181507 Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine) Tricyclic antidepressants (e.g., amitriptyline, clomipramine, imipramine) Typical antipsychotics (e.g., acetophenazine, chlorpromazine, chlorprothixene, fluphenazine, loxapine, pimozide) Vortioxetine
Unknown/unsorted: Ergolines (e.g., lisuride, pergolide) Piperazines (e.g., naphthylpiperazine)

See also: Receptor/signaling modulators
Adrenergics
Dopaminergics
Melatonergics
Monoamine reuptake inhibitors and releasing agents
Monoamine metabolism modulators
Monoamine neurotoxins

Categories:

Latest revision as of 13:50, 5 September 2024

Human brain mapping studies with altanserin

Synthesis

See also

References