Arylacetamides as peripherally restricted kappa opioid receptor agonists

Authors
Kumar, V Marella, MA Cortes-Burgos, L Chang, AC Cassel, JA Daubert, JD DeHaven, RN DeHaven-Hudkins, DL Gottshall, SL Mansson, E Maycock, AL
Citation
V. Kumar et al., Arylacetamides as peripherally restricted kappa opioid receptor agonists, BIOORG MED, 10(22), 2000, pp. 2567-2570
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
22
Year of publication
2000
Pages
2567 - 2570
Database
ISI
SICI code
0960-894X(20001120)10:22<2567:AAPRKO>2.0.ZU;2-T
Abstract
Analogues of the kappa (kappa) opioid receptor agonist, ICI 199441, were pr epared. K-i values for these analogues at the cloned human kappa opioid rec eptor ranged from 0.058 to 25 nM. Trifluoromethylaryl derivatives were pote nt analgesics when administered subcutaneously in the rat and were more per ipherally restricted than the parent compound, ICI 199441. (C) 2000 Elsevie r Science Ltd. All rights reserved.