Journal ArticleDOI
ICI 174864: A highly selective antagonist for the opioid Δ-receptor
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This article is published in European Journal of Pharmacology.The article was published on 1984-01-27. It has received 357 citations till now. The article focuses on the topics: Competitive antagonist & Narcotic antagonist.read more
Citations
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D1 dopamine receptor--the search for a function: a critical evaluation of the D1/D2 dopamine receptor classification and its functional implications.
David Clark,Francis J. White +1 more
TL;DR: A variety of biochemical, behavioral, and electrophysiological evidence is presented which supports the view that D1 and D2 DA receptors can interact in both an opposing and synergistic fashion.
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Naltrindole, a highly selective and potent non-peptide δ opioid receptor antagonist
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Binaltorphimine and nor-binaltorphimine, potent and selective k-opioid receptor antagonists
TL;DR: BNI and nor-BNI represent the first highly selective kappa opioids receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with kappa opioid receptors in vitro and in vivo.
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Opioid Peptides and Opioid Receptors in Cells of the Immune System
N. E. S. Sibinga,A. Goldstein +1 more
TL;DR: A large number of binding sites were found in subjects treated with either a Jl-selective or a nonselective mode of administration of the pro-enkephalin gene, and the number of sites affected by either method was small.
Journal ArticleDOI
Opioid receptors and their ligands.
TL;DR: The main focus is on the structure-activity relationship studies of peptide ligands for three main opioid receptor types (micro, delta, kappa), their selectivities and pharmacological activities in vitro, and chemical modifications that led to obtaining potent and selective agonists and antagonists for these receptors.
References
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Journal ArticleDOI
The binding spectrum of narcotic analgesic drugs with different agonist and antagonist properties
TL;DR: Since each of the four groups of compounds, whether pure agonists, agonist-antagonists, ketazocine-like drugs or pure antagonists, shows independent varittions in the affinities to the μ- and ϰ-binding sites, their different pharmacological behaviour cannot be solely due to difference in the binding spectra.
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Selective antagonists at the opiate delta-receptor.
TL;DR: Using two in vitro models, two novel peptide antagonists are identified which selectively and competitively reverse the effects of opiates at the delta-receptor, with little or no activity at either mu or kappa receptors.
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A model for the interaction of competitive antagonists with two receptor-subtypes characterized by a Schild-plot with apparent slope unity. Agonist-dependent enantiomeric affinity ratios for bupranolol in tracheae but not in right atria of guinea pigs.
Horst Lemoine,Alberto J. Kaumann +1 more
TL;DR: In this paper, the double log relationship between the agonist concentration ratio (t-1) against antagonist concentration for the case of two receptor subtypes mediating the same qualitative effect of an agonist and interacting with both agonists and antagonist was presented.
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Differences in the inhibitory effects of normorphine and opioid peptides on the responses of the vasa deferentia of two strains of mice.
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Divergent structure activity relationships in series of enkephalin agonists and cognate antagonists.
P. Belton,Ronald Cotton,M.B. Giles,James J. Gormley,L. Miller,J.S. Shaw,D. Timms,A. Wilkinson +7 more
TL;DR: The diallyl congeners of a larger range of potent mu-and delta- selective enkephalin agonists have been prepared and were found to be weak, non-selective antagonists as assessed by their ability to antagonise the effects of normorphine and [Leu]enkephaline on the field-stimulated mouse vas deferens.