基于 6-烷氧基异吲哚啉-1-酮的多巴胺 D2 部分激动剂作为潜在的抗精神病药物。
6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.
机构信息
Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, United States.
出版信息
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5666-9. doi: 10.1016/j.bmcl.2010.08.023. Epub 2010 Aug 8.
PMID:20801650
Abstract
A series of 6-alkoxyisoindolin-1-ones with a magic shotgun pharmacological profile are presented as potential antipsychotics. The in vitro pharmacological profile includes D(2) partial agonism (30-55%), 5-HT(1A) partial agonism (60-90%), and 5-HT(2A) antagonism. Selected compounds in this series displayed good in vivo activity and potency.
摘要
一系列具有神奇“猎枪”药理学特征的 6-烷氧基异吲哚啉-1-酮被呈现为有潜力的抗精神病药物。体外药理学特征包括 D2 部分激动剂（30-55%）、5-HT1A 部分激动剂（60-90%）和 5-HT2A 拮抗剂。该系列中的选定化合物表现出良好的体内活性和效力。
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