Interaction of p-nitrophenylalanine enkephalins with mu-, delta- and kappa-subtypes of the opiate receptor.

Details

Serval ID
serval:BIB_71C189524271
Type
Article: article from journal or magazin.
Collection
Publications
Title
Interaction of p-nitrophenylalanine enkephalins with mu-, delta- and kappa-subtypes of the opiate receptor.
Journal
European Journal of Pharmacology
Author(s)
Fauchère J.L., Do K.Q., Schwyzer R., Robson L.E., Gillan M.G., Paterson S.J., Kosterlitz H.W.
ISSN
0014-2999 (Print)
ISSN-L
0014-2999
Publication state
Published
Issued date
1982
Peer-reviewed
Oui
Volume
77
Number
4
Pages
339-342
Language
english
Notes
Publication types: In Vitro ; Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, P.H.S.Publication Status: ppublish
Abstract
Substitution of L-p-nitrophenylalanine for phenylalanine in position 4 of [D-Ala2, KLeu-NH2(5)]enkephalin analogues increased their affinity for mu-, delta- and kappa-binding sites in guinea-pig brain, increased their potency to inhibit electrically evoked contractions of the guinea-pig ileum and mouse vas deferens, and increased their analgesic potency in the mouse tail flick test, Introduction of L-adamantylalanine, but not of L-neopentylglycine, in position 5 resulted in a loss of activity.
Keywords
Animals, Binding, Competitive, Brain Chemistry, Endorphins/metabolism, Enkephalins/metabolism, Guinea Pigs, Male, Mice, Muscle Contraction/drug effects, Muscle, Smooth/drug effects, Receptors, Opioid/metabolism, Receptors, Opioid, delta, Receptors, Opioid, kappa, Receptors, Opioid, mu, Structure-Activity Relationship
Pubmed
Web of science
Create date
06/03/2014 15:57
Last modification date
20/08/2019 14:30
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