"目录号: HY-14782
GPCR/G ProteinNeuronal Signaling-
Adoprazine是5-HT1A受体的完全激动剂和D2/3受体的拮抗剂。
5-HT ReceptorDopamine Receptor
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生物活性
Description
Adoprazine, a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.IC50 Value: N/ATarget: Dopamine Receptor; 5-HT ReceptorAdoprazine is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia.
Clinical Trial
NCT00581243
Wyeth is now a wholly owned subsidiary of Pfizer-Solvay Pharmaceuticals
Healthy
January 2008
Phase 1
NCT00620568
Wyeth is now a wholly owned subsidiary of Pfizer-Solvay Pharmaceuticals
Healthy
February 2008
Phase 1
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References
[1].Auclair AL, Kleven MS, Barret-Grévoz C, Barreto M, Newman-Tancredi A, Depoortère R. Differences among conventional, atypical and novel putative D(2)/5-HT(1A) antipsychotics on catalepsy-associated behaviour in cynomolgus monkeys. Behav Brain Res. 2009 N
[2].Lange JH, Reinders JH, Tolboom JT, Glennon JC, Coolen HK, Kruse CG.Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. J Med Chem. 2007 Oct 18;50(21):5103-8.
[3].McCreary AC, Glennon JC, Ashby CR Jr, Meltzer HY, Li Z, Reinders JH, Hesselink MB, Long SK, Herremans AH, van Stuivenberg H, Feenstra RW, Kruse CG. SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monoh
[4].Feenstra RW, van den Hoogenband A, Stroomer CN, van Stuivenberg HH, Tulp MT, Long SK, van der Heyden JA, Kruse CG. SAR study of 1-aryl-4-(phenylarylmethyl)piperazines as ligands for both dopamine D2 and serotonin 5-HT1A receptors showing varying degrees
[5].Cosi C, Carilla-Durand E, Assié MB, Ormiere AM, Maraval M, Leduc N, Newman-Tancredi A. Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Eur J Ph