| Literature DB >> 20117000 |
Hassan Pajouhesh1, Zhong-Ping Feng, Yanbing Ding, Lingyun Zhang, Hossein Pajouhesh, Jerrie-Lynn Morrison, Francesco Belardetti, Elizabeth Tringham, Eric Simonson, Todd W Vanderah, Frank Porreca, Gerald W Zamponi, Lester A Mitscher, Terrance P Snutch.
Abstract
A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC(50) values in the range of 10-150 nM and selectivity over the L-type channels up to nearly 1200-fold. Orally administered compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20117000 DOI： 10.1016/j.bmcl.2010.01.008
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823