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Revision as of 06:13, 1 July 2011 editCheMoBot (talk | contribs)Bots141,565 edits Updating {{drugbox}} (changes to verified fields - added verified revid - updated 'ChemSpiderID_Ref', 'StdInChI_Ref', 'StdInChIKey_Ref', 'ChEMBL_Ref', 'KEGG_Ref') per Chem/Drugbox validation (rep← Previous edit Latest revision as of 16:36, 19 December 2023 edit undoJWBE (talk | contribs)Extended confirmed users10,129 edits added Category:Sec-Butyl compounds using HotCat 
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{{Short description|Chemical compound}}
{{drugbox
{{Drugbox
| Verifiedfields = changed | Verifiedfields = changed
| UNII_Ref = {{fdacite|changed|FDA}} | Watchedfields = changed
⚫ | verifiedrevid = 437186450
⚫ | UNII = LF1VBG4ZUK
⚫ | IUPAC_name = 8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-''N''-pyrazolo-1,3,5-triazin-4-amine
⚫ | verifiedrevid = 415900050
⚫ | image = Pexacerfont.svg
⚫ | IUPAC_name = 8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-''N''-pyrazolo-1,3,5-triazin-4-amine
| width = 250
⚫ | image = Pexacerfont.svg

⚫ | CAS_number = 459856-18-9
<!--Clinical data-->
⚫ | ATC_prefix = none
| tradename =
⚫ | ATC_suffix =
⚫ | pregnancy_category =
| PubChem = ?
⚫ | legal_status = Uncontrolled
⚫ | C = 18 | H = 24 | N = 6 | O = 1
| molecular_weight = 340.4 g/mol
⚫ | bioavailability =
⚫ | metabolism =
⚫ | elimination_half-life =
⚫ | excretion =
⚫ | pregnancy_category =
⚫ | legal_status = Uncontrolled
| routes_of_administration = Oral | routes_of_administration = Oral

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

<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
⚫ | CAS_number = 459856-18-9
⚫ | ATC_prefix = None
⚫ | ATC_suffix =
| PubChem = 9884366
| UNII_Ref = {{fdacite|correct|FDA}}
⚫ | UNII = LF1VBG4ZUK
| KEGG = D10022
| KEGG_Ref = {{keggcite|changed|kegg}}
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 8060040

<!--Chemical data-->
⚫ | C = 18 | H = 24 | N = 6 | O = 1
| smiles = CC(C)NC1=NC(=NC2=C(C(=NN21)C)C3=C(N=C(C=C3)OC)C)C
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 1S/C18H24N6O/c1-7-10(2)19-18-22-13(5)21-17-16(12(4)23-24(17)18)14-8-9-15(25-6)20-11(14)3/h8-10H,7H2,1-6H3,(H,19,21,22)/t10-/m1/s1
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = LBWQSAZEYIZZCE-SNVBAGLBSA-N
}} }}


'''Pexacerfont''' ('''BMS-562,086''') is a drug developed by ] which acts as a ] antagonist. '''Pexacerfont''' (],<ref>{{cite web|title=International Nonproprietary Names for Pharmaceutical Substances (INN). RECOMMENDED International Nonproprietary Names: List 59|url=https://www.who.int/medicines/publications/druginformation/innlists/RL59.pdf|publisher=World Health Organization|access-date=16 July 2016|page=60}}</ref> previously known as '''BMS-562,086''') is a drug developed by ] which acts as a ] antagonist.


Corticotropin releasing factor (CRF), also known as ], is an endogenous peptide hormone which is released in response to various triggers such as chronic stress. This then triggers the release of ] (ACTH), another hormone which is involved in the physiological response to stress. Chronic release of CRF and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive ] release, ], ], ], ], ], and development of ] and consequent cardiovascular problems.<ref>Zoumakis E, Rice KC, Gold PW, Chrousos GP. Potential uses of corticotropin-releasing hormone antagonists. ''Annals of the New York Academy of Sciences''. 2006 Nov;1083:239-51.</ref> Corticotropin-releasing factor (CRF), also known as ], is an endogenous peptide hormone which is released in response to various triggers such as ]. This then triggers the release of ] (ACTH), another hormone which is involved in the physiological response to stress. Chronic release of CRF and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive ] release, ], ], ]{{citation needed|date=July 2016}}, ], ], and development of ] and consequent cardiovascular problems.<ref>{{cite journal | vauthors = Zoumakis E, Rice KC, Gold PW, Chrousos GP | title = Potential uses of corticotropin-releasing hormone antagonists | journal = Annals of the New York Academy of Sciences | volume = 1083 | issue = 1 | pages = 239–51 | date = November 2006 | pmid = 17148743 | doi = 10.1196/annals.1367.021 | bibcode = 2006NYASA1083..239Z | s2cid = 7731338 }}</ref>


Pexacerfont is a recently developed CRF-1 antagonist which is currently in clinical trials for the treatment of anxiety disorders,<ref></ref> and has also been proposed to be useful for the treatment of depression and irritable bowel syndrome.<ref></ref> Pexacerfont is a recently developed CRF-1 antagonist which was in clinical trials for the treatment of ]s,<ref>{{ClinicalTrialsGov|NCT00481325|Study of Pexacerfont (BMS-562086) in the Treatment of Outpatients With Generalized Anxiety Disorder}}</ref> and has also been proposed to be useful for the treatment of ] and ].{{citation needed|date=July 2016}}


A recent multicenter, randomized, double-blind, placebo-controlled trial found that Pexacerfont (100 mg/day) did not separate from placebo on the primary outcome measure (the mean change from baseline to end point in the Hamilton Anxiety Scale score). <ref>Coric V, Feldman HH, Oren DA, Shekhar A, Pultz J, Dockens RC, Wu X, Gentile KA, Huang SP, Emison E, Delmonte T, D'Souza BB, Zimbroff DL, Grebb JA, Goddard AW, Stock EG (2010). Multicenter, randomized, double-blind, active comparator and placebo-controlled trial of a corticotropin-releasing factor receptor-1 antagonist in generalized anxiety disorder. Depress Anxiety. 27(5):417-25. PMID: 20455246.</ref> These results suggest that blockade of CRF-1 receptor may not be a feasible treatment for anxiety disorders in certain human populations. A recent multicenter, randomized, double-blind, placebo-controlled trial found that pexacerfont (100&nbsp;mg/day) did not separate from placebo on the primary outcome measure (the mean change from baseline to end point in the ] score).<ref>{{cite journal | vauthors = Coric V, Feldman HH, Oren DA, Shekhar A, Pultz J, Dockens RC, Wu X, Gentile KA, Huang SP, Emison E, Delmonte T, D'Souza BB, Zimbroff DL, Grebb JA, Goddard AW, Stock EG | display-authors = 6 | title = Multicenter, randomized, double-blind, active comparator and placebo-controlled trial of a corticotropin-releasing factor receptor-1 antagonist in generalized anxiety disorder | journal = Depression and Anxiety | volume = 27 | issue = 5 | pages = 417–25 | date = May 2010 | pmid = 20455246 | doi = 10.1002/da.20695 | s2cid = 5370614 | doi-access = free }}</ref> These results suggest that blockade of CRF<sub>1</sub> receptor may not be a feasible treatment for anxiety disorders in certain human populations.


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


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


{{Antidepressants}}
{{Anxiolytics}}
{{Neuropeptidergics}}


] ]
] ]
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