Arylacetamides as peripherally restricted kappa opioid receptor agonists

Analogues of the kappa (κ) opioid receptor agonist, ICI 199441, were prepared. K i values for these analogues at the cloned human κ opioid receptor ranged from 0.058 to 25 nM. Trifluoromethylaryl derivatives were potent analgesics when administered subcutaneously in the rat and were more peripherall...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-11, Vol.10 (22), p.2567-2570
Main Authors: Kumar, Virendra, Marella, Michael A., Cortes-Burgos, Luz, Chang, An-Chih, Cassel, Joel A., Daubert, Jeffrey D., DeHaven, Robert N., DeHaven-Hudkins, Diane L., Gottshall, Susan L., Mansson, Erik, Maycock, Alan L.
Format: Article
Language:English
Subjects:
Acetamides - chemistry
Acetamides - pharmacology
Analgesics
Analgesics, Opioid - chemistry
Analgesics, Opioid - pharmacology
Animals
Biological and medical sciences
Medical sciences
Molecular Structure
Neuropharmacology
Pharmacology. Drug treatments
Pyrrolidines - chemistry
Pyrrolidines - pharmacology
Rats
Receptors, Opioid, kappa - agonists
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Summary:Analogues of the kappa (κ) opioid receptor agonist, ICI 199441, were prepared. K i values for these analogues at the cloned human κ opioid receptor ranged from 0.058 to 25 nM. Trifluoromethylaryl derivatives were potent analgesics when administered subcutaneously in the rat and were more peripherally restricted than the parent compound, ICI 199441.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00519-9