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GR-127935: Difference between revisions

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Revision as of 22:24, 18 September 2011 editCheMoBot (talk | contribs)Bots141,565 edits Updating {{drugbox}} (no changed fields - added verified revid - updated 'ChemSpiderID_Ref', 'DrugBank_Ref', 'UNII_Ref', 'ChEMBL_Ref', 'ChEBI_Ref', 'KEGG_Ref', 'StdInChI_Ref', 'StdInChIKey_Ref', 'DrugBank_Ref', 'ChEBI_Ref') per [[WP:CHEMVALID|Chem/Dr← Previous edit Latest revision as of 12:59, 5 August 2024 edit undoJWBE (talk | contribs)Extended confirmed users10,129 edits removed Category:Piperazines; added Category:4-Methylpiperazin-1-yl compounds using HotCat 
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{{Short description|Drug}}
{{Drugbox {{Drugbox
| Verifiedfields = changed
| verifiedrevid = 407826266 | verifiedrevid = 451223322
| IUPAC_name = ''N''--2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1-1'-biphenyl-4-carboxamide | IUPAC_name = ''N''--2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1-1'-biphenyl-4-carboxamide
| image = GR-127,935_structure.png | image = GR-127,935_structure.png
| width = 250


<!--Clinical data--> <!--Clinical data-->
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| pregnancy_category = | pregnancy_category =
| legal_status = | legal_status =
| routes_of_administration = | routes_of_administration =


<!--Pharmacokinetic data--> <!--Pharmacokinetic data-->
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| metabolism = | metabolism =
| elimination_half-life = | elimination_half-life =
| excretion = | excretion =


<!--Identifiers--> <!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 148672-13-3 | CAS_number = 148672-13-3
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 2LLH6CEB40
| ATC_prefix = none | ATC_prefix = none
| ATC_suffix = | ATC_suffix =
| PubChem = 107780 | PubChem = 107780
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 15928
| IUPHAR_ligand = 14 | IUPHAR_ligand = 14
| ChemSpiderID = 96935
| ChEBI = 64114


<!--Chemical data--> <!--Chemical data-->
| C=29 | H=31 | N=5 | O=3 | C=29 | H=31 | N=5 | O=3
| molecular_weight = 497.587 g/mol
| smiles = n5oc(C)nc5-c(cc2C)ccc2-c(cc3)ccc3C(=O)Nc(ccc1OC)cc1N4CCN(C)CC4 | smiles = n5oc(C)nc5-c(cc2C)ccc2-c(cc3)ccc3C(=O)Nc(ccc1OC)cc1N4CCN(C)CC4
| StdInChI = 1S/C29H31N5O3/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34/h5-12,17-18H,13-16H2,1-4H3,(H,31,35)
| StdInChIKey = YDBCEBYHYKAFRX-UHFFFAOYSA-N
}} }}


'''GR-127,935''' is a ] which acts as a ] ] at the ] ]s ] and ].<ref name="pmid8788495">{{cite journal |author=Skingle M, Beattie DT, Scopes DI, Starkey SJ, Connor HE, Feniuk W, Tyers MB |title=GR127935: a potent and selective 5-HT1D receptor antagonist |journal=Behavioural Brain Research |volume=73 |issue=1-2 |pages=157–61 |year=1996 |pmid=8788495 |doi= 10.1016/0166-4328(96)00089-7|url=}}</ref> It has little effect when given by itself but blocks the ] effect of 5-HT<sub>1B</sub> agonists,<ref name="pmid17440711">{{cite journal |author=Bannai M, Fish EW, Faccidomo S, Miczek KA |title=Anti-aggressive effects of agonists at 5-HT1B receptors in the dorsal raphe nucleus of mice |journal=Psychopharmacology |volume=193 |issue=2 |pages=295–304 |year=2007 |month=August |pmid=17440711 |doi=10.1007/s00213-007-0780-5 |url=}}</ref> and alters release of serotonin in the brain,<ref name="pmid17888505">{{cite journal |author=Rex A, Voigt JP, Wicke KM, Fink H |title=In vivo/ex vivo and behavioural study on central effects of 5-HT1B/1D and 5-HT1A antagonists in guinea pigs |journal=Pharmacology, Biochemistry, and Behavior |volume=88 |issue=3 |pages=196–204 |year=2008 |month=January |pmid=17888505 |doi=10.1016/j.pbb.2007.07.016 |url=}}</ref> as well as reducing drug-seeking behaviour in cocaine addicted rats.<ref name="pmid19211971">{{cite journal |author=Przegaliński E, Gołda A, Filip M |title=Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats |journal=Pharmacological Reports : PR |volume=60 |issue=6 |pages=798–810 |year=2008 |pmid=19211971 |doi= |url=}}</ref> '''GR-127935''' is a ] which acts as a ] ] at the ] ]s ] and ].<ref name="pmid8788495">{{cite journal |vauthors=Skingle M, Beattie DT, Scopes DI, Starkey SJ, Connor HE, Feniuk W, Tyers MB |title=GR127935: a potent and selective 5-HT1D receptor antagonist |journal=Behavioural Brain Research |volume=73 |issue=1–2 |pages=157–61 |year=1996 |pmid=8788495 |doi= 10.1016/0166-4328(96)00089-7|s2cid=34394584 }}</ref> It has little effect when given by itself but blocks the ] effect of 5-HT<sub>1B</sub> agonists,<ref name="pmid17440711">{{cite journal |vauthors=Bannai M, Fish EW, Faccidomo S, Miczek KA |title=Anti-aggressive effects of agonists at 5-HT1B receptors in the dorsal raphe nucleus of mice |journal=Psychopharmacology |volume=193 |issue=2 |pages=295–304 |date=August 2007 |pmid=17440711 |doi=10.1007/s00213-007-0780-5 |s2cid=6766784 }}</ref> and alters release of serotonin in the brain,<ref name="pmid17888505">{{cite journal |vauthors=Rex A, Voigt JP, Wicke KM, Fink H |title=In vivo/ex vivo and behavioural study on central effects of 5-HT1B/1D and 5-HT1A antagonists in guinea pigs |journal=Pharmacology Biochemistry and Behavior |volume=88 |issue=3 |pages=196–204 |date=January 2008 |pmid=17888505 |doi=10.1016/j.pbb.2007.07.016 |s2cid=26577695 }}</ref> as well as reducing drug-seeking behaviour in cocaine addicted rats.<ref name="pmid19211971">{{cite journal |vauthors=Przegaliński E, Gołda A, Filip M |title=Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats |journal=Pharmacological Reports |volume=60 |issue=6 |pages=798–810 |year=2008 |pmid=19211971 }}</ref>


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


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


{{Dependence treatment}}

{{Antiaddictives}}
{{Serotonergics}} {{Serotonergics}}


] ]
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{{nervous-system-drug-stub}}
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