新型吲哚-2-羧酰胺大麻素 CB1 拮抗剂的药代动力学优化。
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.
机构信息
Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):2034-9. doi: 10.1016/j.bmcl.2011.02.019. Epub 2011 Feb 19.
PMID:21334892
Abstract
The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB(1) antagonist with high predicted human oral bioavailability.
摘要
本发明揭示了一系列新型吲哚-2-甲酰胺类大麻素 CB1 受体拮抗剂的基于药代动力学的优化。研究发现化合物 24 是一种具有高活性和选择性的大麻素 CB1 拮抗剂，具有较高的预测人体口服生物利用度。
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