Misplaced Pages

Terguride: Difference between revisions

Article snapshot taken from Wikipedia with creative commons attribution-sharealike license. Give it a read and then ask your questions in the chat. We can research this topic together.
Browse history interactively
Page 1
Page 2
← Previous editContent deleted Content addedVisualWikitext
Revision as of 23:19, 30 June 2011 editCheMoBot (talk | contribs)Bots141,565 edits Updating {{drugbox}} (changes to verified fields - updated 'ChemSpiderID_Ref', 'StdInChI_Ref', 'StdInChIKey_Ref', 'ChEMBL_Ref') per Chem/Drugbox validation (report [[Misplaced Pages talk:WikiProject_Ph← Previous edit Latest revision as of 14:46, 25 August 2023 edit undoCitation bot (talk | contribs)Bots5,428,799 edits Add: s2cid. | Use this bot. Report bugs. | Suggested by Headbomb | Linked from Misplaced Pages:WikiProject_Academic_Journals/Journals_cited_by_Wikipedia/Sandbox2 | #UCB_webform_linked 1791/1971 
(39 intermediate revisions by 21 users not shown)
Line 1: Line 1:
{{Short description|Chemical compound}}
{{drugbox
{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 437134889
| UNII_Ref = {{fdacite|changed|FDA}}
| IUPAC_name = 3-quinolin-9-yl]-1,1-diethylurea
| UNII = 21OJT43Q88
| image = Terguride.png
| verifiedrevid = 408925505
| width =
| IUPAC_name = ''N'',''N''-diethyl-''N'''-urea

| image = Terguride.png
<!--Clinical data-->
| CAS_number = 37686-84-3
| tradename = Teluron
| ATC_prefix = G02
| Drugs.com = {{drugs.com|international|terguride}}
| ATC_suffix = CB06
| pregnancy_category =
| PubChem = 443951
| legal_status = Rx-only
| routes_of_administration = ]

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

<!--Identifiers-->
| CAS_number = 37686-84-3
| ATC_prefix = G02
| ATC_suffix = CB06
| PubChem = 443951
| ChemSpiderID = 392004
| IUPHAR_ligand = 56 | IUPHAR_ligand = 56
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| DrugBank = DB13399
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 21OJT43Q88
| KEGG_Ref = {{keggcite|correct|kegg}} | KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D01348 | KEGG = D01348
| synonyms = Dironyl; Mysalfon; ''trans''-Dihydrolisuride; Transdihydrolisuride; TDHL; SH-406; VUFB-6638; ZK-31224; ''N'',''N''-Diethyl-''N<nowiki>'</nowiki>''-urea
| C = 20 | H = 28 | N = 4 | O = 1

| molecular_weight = 340.46 g/mol
<!--Chemical data-->
| smiles = CCN(CC)C(=O)N1C2(CC3=CNC4=CC=CC2=C34)N(C1)C
| C=20 | H=28 | N=4 | O=1
| bioavailability =
| StdInChI = 1S/C20H28N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,11,14,16,18,21H,4-5,9-10,12H2,1-3H3,(H,22,25)/t14-,16+,18+/m0/s1
| metabolism =
| StdInChIKey = JOAHPSVPXZTVEP-YXJHDRRASA-N
| elimination_half-life =
| SMILES = CCN(CC)C(=O)N1C2(CC3=CNC4=CC=CC2=C34)N(C1)C
| excretion =
| pregnancy_category=
| legal_status = Rx-only
| routes_of_administration = Oral
}} }}


'''Terguride''' ({{Abbrlink|INN|International Nonproprietary Name}}, {{Abbrlink|JAN|Japanese Accepted Name}}), sold under the brand name '''Teluron''', is a ] ] and ] ] of the ] family. It is approved for and used as a ] in the treatment of ] (high prolactin levels) in ].<ref name="Drugs.com">{{Cite web|url=http://drugs.com/international/terguride.html|archive-url = https://web.archive.org/web/20160303211431/http://drugs.com/international/terguride.html|archive-date = 2016-03-03|title = List of 5HT3 receptor antagonists (5hydroxytryptamine receptor antagonists)}}</ref><ref name="AdisInsight">{{Cite web|url=https://adisinsight.springer.com/drugs/800000563|title=Terguride - AdisInsight}}</ref> Terguride is taken ].{{Citation needed|date=April 2021}}
'''Terguride''' (]) is a ] ]. It is used for the treatment of hyperprolactinemia.


==Pharmacology==
In May 2008, terguride was granted ] status for the treatment of ].<ref></ref>
In May 2010 ] purchased world-wide rights for the drug.<ref></ref>


===Pharmacodynamics===
Terguride acts as an ] of the ] ] and as an ] of the ] ] and ]s, among other actions.{{Citation needed|date=April 2021}}


As an antagonist of the 5-HT<sub>2B</sub> receptor, terguride is not associated with ].<ref name="pmid25712664">{{cite journal | vauthors = Zajdel P, Bednarski M, Sapa J, Nowak G | title = Ergotamine and nicergoline - facts and myths | journal = Pharmacol Rep | volume = 67 | issue = 2 | pages = 360–3 | date = April 2015 | pmid = 25712664 | doi = 10.1016/j.pharep.2014.10.010 | s2cid = 22768662 | url = }}</ref>
== References ==
{{Reflist}}


{| class="wikitable"
|+ {{Nowrap|Activities of terguride at various sites<ref name="pmid12388666">{{cite journal | vauthors = Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A | title = Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes | journal = J Pharmacol Exp Ther | volume = 303 | issue = 2 | pages = 791–804 | date = November 2002 | pmid = 12388666 | doi = 10.1124/jpet.102.039867 | s2cid = 6200455 | url = }}</ref><ref name="pmid12388667">{{cite journal | vauthors = Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ | title = Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor | journal = J Pharmacol Exp Ther | volume = 303 | issue = 2 | pages = 805–14 | date = November 2002 | pmid = 12388667 | doi = 10.1124/jpet.102.039875 | s2cid = 35238120 | url = }}</ref><ref name="pmid12388668">{{cite journal | vauthors = Newman-Tancredi A, Cussac D, Quentric Y, Touzard M, Verrièle L, Carpentier N, Millan MJ | title = Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes | journal = J Pharmacol Exp Ther | volume = 303 | issue = 2 | pages = 815–22 | date = November 2002 | pmid = 12388668 | doi = 10.1124/jpet.102.039883 | s2cid = 19260572 | url = }}</ref><ref name="PDSPKiDatabase">{{cite web |url=https://pdsp.unc.edu/databases/pdsp.php?testFreeRadio=testFreeRadio&testLigand=Terguride&doQuery=Submit+Query |title=PDSP Database - UNC |website=pdsp.unc.edu |access-date=15 January 2022 |archive-url=https://web.archive.org/web/20210413033753/https://pdsp.unc.edu/databases/pdsp.php?testFreeRadio=testFreeRadio&testLigand=Terguride&doQuery=Submit+Query |archive-date=13 April 2021 |url-status=dead}}</ref>}}
! Site
! Affinity (K<sub>i</sub> )
! Efficacy (E<sub>max</sub> )
! Action
|-
| ]
| 28
| ?
| ?
|-
| ]
| 0.81
| 39
| Partial agonist
|-
| ]
| 1.1
| 0
| Silent antagonist
|-
| ]
| 1.0
| 36
| Partial agonist
|-
| ]
| 8.1
| 0
| Silent antagonist
|-
| ]
| 23
| ?
| ?
|-
| ]
| 3.5
| 71
| Partial agonist
|-
| ]
| 257
| 37
| Partial agonist
|-
| ]
| 16
| 62
| Partial agonist
|-
| ]
| 4.8
| 49
| Partial agonist
|-
| ]
| 7.1
| 0
| Silent antagonist
|-
| ]
| 48
| 0
| Silent antagonist
|-
| ]
| 8–42
| ?
| ?
|-
| ]
| 3.5
| 0
| Silent antagonist
|-
| ]
| 35
| ?
| ?
|-
| ]
| 3.9
| ?
| ?
|-
| ]
| 0.30
| 0
| Silent antagonist
|-
| ]
| 0.45
| 0
| Silent antagonist
|-
| ]
| 0.76
| 0
| Silent antagonist
|-
| ]
| 1.5
| ?
| ?
|-
| ]
| 661
| ?
| ?
|-
| ]
| 20
| ?
| ?
|-
| ]
| 339
| ?
| ?
|-
| ]
| >10,000
| ?
| ?
|- class="sortbottom"
| colspan="4" style="width: 1px; background-color:#eaecf0; text-align: center;" | '''Notes:''' All receptors are human except α<sub>2D</sub>-adrenergic, which is rat (no human counterpart), and 5-HT<sub>7</sub>, which was ].<ref name="pmid12388666" /><ref name="PDSPKiDatabase" />
|}


==Research==
{{Other gynecologicals}}
] stimulates the proliferation of pulmonary artery smooth muscle cells, and induces fibrosis in the wall of pulmonary arteries. Together, this causes vascular remodeling and narrowing of the pulmonary arteries. These changes result in increased vascular resistance and PAH. Due to the potential anti-proliferative and anti-fibrotic activity of terguride, this potential medicine could offer the hope of achieving reversal of pulmonary artery vascular remodeling and attenuation of disease progression.<ref>{{cite journal | vauthors = Janssen W, Schymura Y, Novoyatleva T, Kojonazarov B, Boehm M, Wietelmann A, Luitel H, Murmann K, Krompiec DR, Tretyn A, Pullamsetti SS, Weissmann N, Seeger W, Ghofrani HA, Schermuly RT | display-authors = 6 | title = 5-HT2B receptor antagonists inhibit fibrosis and protect from RV heart failure | journal = BioMed Research International | year = 2015 | volume = 2015 | pages = 438403 | pmid = 25667920 | doi = 10.1155/2015/438403 | pmc = 4312574 | doi-access = free }}</ref> In May 2008, terguride was granted ] status for the treatment of ].<ref></ref>
{{Dopaminergics}}
In May 2010 ] purchased worldwide rights for the drug.<ref>{{Cite web |url=http://www.theday.com/article/20100513/BIZ02/305139376/1044 |title=TheDay.com 5/10/2010 |access-date=2010-05-21 |archive-date=2016-03-05 |archive-url=https://web.archive.org/web/20160305160006/http://www.theday.com/article/20100513/BIZ02/305139376/1044 |url-status=dead }}</ref> However, development was discontinued in 2011.


==References==
]
{{Reflist}}
]
]


{{Prolactin inhibitors and anti-inflammatory products for vaginal administration}}
{{Navboxes
| title = ]
| titlestyle = background:#ccccff
| list1 =
{{Adrenergic receptor modulators}}
{{Dopamine receptor modulators}}
{{Prolactin receptor modulators}}
{{Serotonin receptor modulators}}
}}
{{Ergolines}}


]
{{genito-urinary-drug-stub}}
]
]
]
]
]
]
]
]
]
]
]
]