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

Authors
Seko, T Kato, M Kohno, H Ono, S Hashimura, K Takimizu, H Nakai, K Maegawa, H Katsube, N Toda, M
Citation
T. Seko et al., Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers, BIOORG MED, 11(16), 2001, pp. 2067-2070
Citations number
14
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960-894X → ACNP
Volume
11
Issue
16
Year of publication
2001
Pages
2067 - 2070
Database
ISI
SICI code
0960-894X(20010820)11:16<2067:SSAAEO>2.0.ZU;2-#
Abstract
The synthesis and structure activity relationship (SAR) study of a novel se ries of N-type calcium channel blockers are described. L-Cysteine derivativ e 2a was found to be a potent and selective N-type calcium channel blocker with IC50 0.63 muM on IMR-32 assay. Compound 2a showed analgesic efficacy i n the rat formalin-induced pain model by intrathecal and oral administratio n. (C) 2001 Elsevier Science Ltd. All rights reserved.