| Literature DB >> 21669533 |
Christine Watson1, Dafydd R Owen, Denise Harding, Kana Kon-I, Mark L Lewis, Helen J Mason, Miyako Matsumizu, Takasuke Mukaiyama, Margarita Rodriguez-Lens, Akiko Shima, Mifune Takeuchi, Isabelle Tran, Tim Young.
Abstract
A series of benzimidazole CB(2) receptor agonists were prepared and their properties investigated. Optimisation of the three benzimidazole substituents led to the identification of compound 23, a potent CB(2) full agonist (EC(50) 2.7nM) with excellent selectivity over the CB(1) receptor (>3000-fold). Compound 23 demonstrated good CNS penetration in rat. Further optimisation led to the identification of compound 34 with improved selectivity over hERG and excellent CNS penetration in rat.Entities:
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Year: 2011 PMID： 21669533 DOI： 10.1016/j.bmcl.2011.05.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823