Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors

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dc.contributor.authorPajouhesh, Hassan
dc.contributor.authorDing, Yanbing
dc.contributor.authorZhang, Lingyun
dc.contributor.authorPajouhesh, Hossein
dc.contributor.authorBelardetti, Francesco
dc.contributor.authorSimonson, Eric
dc.contributor.authorPorreca, Frank
dc.contributor.authorMitscher, Lester A
dc.contributor.authorSnutch, Terrance P
dc.contributor.authorFeng, Zhong Ping
dc.contributor.authorMorrison, Jerrie Lynn
dc.contributor.authorTringham, Elizabeth W.
dc.contributor.authorVanderah, Todd W.
dc.contributor.authorZamponi, Gerald W.
dc.date.accessioned2018-05-25T17:53:13Z
dc.date.available2018-05-25T17:53:13Z
dc.date.issued2010-02-15
dc.description.abstractA 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.en_US
dc.identifier.citationPajouhesh, H., Feng, Z. P., Ding, Y., Zhang, L., Pajouhesh, H., Morrison, J. L., … Snutch, T. P. (2010). Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(4), 1378–1383. https://doi.org/10.1016/j.bmcl.2010.01.008en_US
dc.identifier.doihttp://dx.doi.org/10.1016/j.bmcl.2010.01.008en_US
dc.identifier.urihttp://hdl.handle.net/1880/106672
dc.language.isoenen_US
dc.publisherElsevier Ltd.en_US
dc.publisher.departmentPhysiology & Pharmacologyen_US
dc.publisher.facultyCumming School of Medicineen_US
dc.publisher.institutionUniversity of Calgaryen_US
dc.rights.urihttps://creativecommons.org/licenses/by/4.0en_US
dc.titleStructure-activity relationships of diphenylpiperazine N-type calcium channel inhibitorsen_US
dc.typeunknown
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