Citation
S. Menzler et al., Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA, BIOORG MED, 10(4), 2000, pp. 345-347
Citations number
27
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X
→ ACNP
Volume
10
Issue
4
Year of publication
2000
Pages
345 - 347
Database
ISI
SICI code
0960-894X(20000221)10:4<345:DABEON>2.0.ZU;2-L
Abstract
Omega-conotoxin MVIIA, a highly potent antagonist of the N-type voltage sen
sitive calcium channel, has shown utility in several models of pain and isc
hemia. We report a series of three alkylphenyl ether based analogues which
mimic three key amino acids of the toxin. Two of the compounds have been fo
und to exhibit IC50 values of 2.7 and 3.3 mu M at the human N-type voltage
sensitive calcium channel. (C) 2000 Elsevier Science Ltd. All rights reserv
ed.