Structure-activity relationships of trimethoxybenzyl piperazine N-type calcium channel inhibitors

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dc.contributor.authorPajouhesh, Hassan
dc.contributor.authorFeng, Zhong-Ping
dc.contributor.authorZhang, Lingyun
dc.contributor.authorPajouhesh, Hossein
dc.contributor.authorJiang, Xinpo
dc.contributor.authorDong, Haiheng
dc.contributor.authorDing, Yanbing
dc.contributor.authorPorreca, Frank
dc.contributor.authorBelardetti, Francesco
dc.contributor.authorHendricson, Adam W.
dc.contributor.authorTringham, Elizabeth W.
dc.contributor.authorVanderah, Todd W.
dc.contributor.authorZamponi, Gerald W.
dc.contributor.authorMitscher, Lester A.
dc.contributor.authorSnutch, Terrance Preston
dc.date.accessioned2018-05-29T14:58:19Z
dc.date.available2018-05-29T14:58:19Z
dc.date.issued2012-04-19
dc.description.abstractWe previously reported the small organic N-type calcium channel blocker NP078585 that while efficacious in animal models for pain, exhibited modest L-type calcium channel selectivity and substantial off-target inhibition against the hERG potassium channel. Structure-activity studies to optimize NP078585 preclinical properties resulted in compound 16, which maintained high potency for N-type calcium channel blockade, and possessed excellent selectivity over the hERG (~120-fold) and L-type (~3600-fold) channels. Compound 16 shows significant anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain and is also efficacious in the rat formalin model of inflammatory pain.en_US
dc.identifier.citationPajouhesh, H., Feng, Z. P., Zhang, L., Pajouhesh, H., Jiang, X., Hendricson, A., … Snutch, T. P. (2012). Structure-activity relationships of trimethoxybenzyl piperazine N-type calcium channel inhibitors. Bioorganic and Medicinal Chemistry Letters, 22(12), 4153–4158. https://doi.org/10.1016/j.bmcl.2012.04.054en_US
dc.identifier.doihttp://dx.doi.org/10.1016/j.bmcl.2012.04.054en_US
dc.identifier.urihttp://hdl.handle.net/1880/106697
dc.identifier.urihttps://doi.org/10.11575/PRISM/43761
dc.language.isoenen_US
dc.publisherElsevieren_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 trimethoxybenzyl piperazine N-type calcium channel inhibitorsen_US
dc.typejournal articleen_US
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