一类新型选择性人CB1反向激动剂的发现。
Discovery of a novel class of selective human CB1 inverse agonists.
作者信息
Foloppe Nicolas, Allen Nicola H, Bentley Carol H, Brooks Teresa D, Kennett Guy, Knight Antony R, Leonardi Stefania, Misra Anil, Monck Nathaniel J T, Sellwood Daniel M
机构信息
Vernalis (R&D) Ltd, Granta Park, Abington, Cambridge CB21 6GB, UK.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1199-206. doi: 10.1016/j.bmcl.2007.11.133. Epub 2007 Dec 7.
Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB(1), which are selective versus hCB(2). These CB(1) ligands present intriguing departures from a classical CB(1) antagonist pharmacophore. Elements of SAR are discussed in this context.
基于配体的虚拟筛选发现了一类新型的人大麻素受体1（hCB(1)）强效反向激动剂，它们对hCB(2)具有选择性。这些CB(1)配体与经典的CB(1)拮抗剂药效团存在有趣的差异。本文将在此背景下讨论构效关系的要素。
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