Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.
第一作者:
R Ian,Storer
第一单位:
Discovery Chemistry, ‡Discovery Biology, and §Pharmacokinetics, Dynamics and Metabolism, Sandwich Laboratories, Pfizer Global Research and Development , Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom.
作者:
医学主题词
动物(Animals);吖庚因类(Azepines);血脑屏障(Blood-Brain Barrier);CHO细胞(CHO Cells);中枢神经系统药物(Central Nervous System Agents);仓鼠属(Cricetulus);狗(Dogs);药物设计(Drug Design);人类(Humans);通透性(Permeability);嘧啶类(Pyrimidines);受体, 血清素, 5-HT2A(Receptor, Serotonin, 5-HT2A);受体, 血清素, 5-HT2B(Receptor, Serotonin, 5-HT2B);受体, 血清素, 5-HT2C(Receptor, Serotonin, 5-HT2C);血清素5-HT2受体激动剂(Serotonin 5-HT2 Receptor Agonists);构效关系(Structure-Activity Relationship);尿失禁, 压力性(Urinary Incontinence, Stress)
DOI
10.1021/jm5003292
PMID
24878222
发布时间
2021-10-21
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