Literature DB >> 10206559

N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.

L Y Hu1, T R Ryder, M F Rafferty, W L Cody, S M Lotarski, G P Miljanich, E Millerman, D M Rock, Y Song, S J Stoehr, C P Taylor, M L Weber, B G Szoke, M G Vartanian.   

Abstract

Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.

Entities:  

Mesh:

Substances:

Year:  1999        PMID: 10206559     DOI: 10.1016/s0960-894x(99)00100-6

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


  3 in total

Review 1.  Calcium channel blockers and pain therapy.

Authors:  B Cox
Journal:  Curr Rev Pain       Date:  2000

2.  Molecular modelling and QSAR analysis of some structurally diverse N-type calcium channel blockers.

Authors:  Jignesh Mungalpara; Ashish Pandey; Vaibhav Jain; C Gopi Mohan
Journal:  J Mol Model       Date:  2009-10-04       Impact factor: 1.810

Review 3.  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

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.