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Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.

Abstract：

:The synthesis and structure-activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. L-Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC(50) 0.63 microM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat formalin-induced pain model by intrathecal and oral administration.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Seko T,Kato M,Kohno H,Ono S,Hashimura K,Takimizu H,Nakai K,Maegawa H,Katsube N,Toda M

doi

10.1016/s0960-894x(01)00414-0

subject

Has Abstract

pub_date

2001-08-20 00:00:00

pages

2067-70

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960894X01004140

journal_volume

11

pub_type

杂志文章

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