cheminform abstract: optimization of a novel series of selective cns penetrant cb2 agonists
TRANSCRIPT
Receptor binding activityX 0280 DOI: 10.1002/chin.201148208
Optimization of a Novel Series of Selective CNS Penetrant CB2 Agonists. — The compound (Ia) shows excellent selectivity as CB2 agonist (EC50 2.7 nM) over the CB1 receptor and demonstrates a good central nervous system (CNS) penetration in rat. The compound (Ib) shows improved selectivity over hERG and also excellent CNS pene-tration in rat. — (WATSON*, C.; et al.; Bioorg. Med. Chem. Lett. 21 (2011) 14, 4284-4287, http://dx.doi.org/10.1016/j.bmcl.2011.05.063 ; Pfizer Global Res. Dev., Sandwich, Kent CT13 9NJ, UK; Eng.) — C. Gebhardt
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ChemInform 2011, 42, issue 48 © 2011 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim