Literature DB >> 22579422

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

Hassan Pajouhesh1, Zhong-Ping Feng, Lingyun Zhang, Hossein Pajouhesh, Xinpo Jiang, Adam Hendricson, Haiheng Dong, Elizabeth Tringham, Yanbing Ding, Todd W Vanderah, Frank Porreca, Francesco Belardetti, Gerald W Zamponi, Lester A Mitscher, Terrance P Snutch.   

Abstract

We 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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22579422     DOI： 10.1016/j.bmcl.2012.04.054

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

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Review 2.  Voltage-dependent CaV3.2 and CaV2.2 channels in nociceptive pathways.

Authors:  Lucia Hoppanova; Lubica Lacinova
Journal:  Pflugers Arch       Date:  2022-01-18       Impact factor: 3.657

3.  Inhibition of N-type calcium channels by fluorophenoxyanilide derivatives.

Authors:  Ellen C Gleeson; Janease E Graham; Sandro Spiller; Irina Vetter; Richard J Lewis; Peter J Duggan; Kellie L Tuck
Journal:  Mar Drugs       Date:  2015-04-13       Impact factor: 5.118

4.  Pharmacological Inhibition of Voltage-gated Ca(2+) Channels for Chronic Pain Relief.

Authors:  Seungkyu Lee
Journal:  Curr Neuropharmacol       Date:  2013-12       Impact factor: 7.363

5.  Synthesis and characterization of a disubstituted piperazine derivative with T-type channel blocking action and analgesic properties.

Authors:  Zubaidha Pudukulatham; Fang-Xiong Zhang; Vinicius M Gadotti; Said M'Dahoma; Prabhuling Swami; Yasinalli Tamboli; Gerald W Zamponi
Journal:  Mol Pain       Date:  2016-04-06       Impact factor: 3.395

6.  Novel charged sodium and calcium channel inhibitor active against neurogenic inflammation.

Authors:  Seungkyu Lee; Sooyeon Jo; Sébastien Talbot; Han-Xiong Bear Zhang; Masakazu Kotoda; Nick A Andrews; Michelino Puopolo; Pin W Liu; Thomas Jacquemont; Maud Pascal; Laurel M Heckman; Aakanksha Jain; Jinbo Lee; Clifford J Woolf; Bruce P Bean
Journal:  Elife       Date:  2019-11-25       Impact factor: 8.140

Review 7.  The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential.

Authors:  Gerald W Zamponi; Joerg Striessnig; Alexandra Koschak; Annette C Dolphin
Journal:  Pharmacol Rev       Date:  2015-10       Impact factor: 25.468

8.  ω-Conotoxin GVIA mimetics that bind and inhibit neuronal Ca(v)2.2 ion channels.

Authors:  Charlotte Elisabet Tranberg; Aijun Yang; Irina Vetter; Jeffrey R McArthur; Jonathan B Baell; Richard J Lewis; Kellie L Tuck; Peter J Duggan
Journal:  Mar Drugs       Date:  2012-10-22       Impact factor: 6.085
  8 in total

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