Journal ArticleDOI
Opiate receptor binding affected differentially by opiates and opioid peptides
TLDR
The potencies of various opiates in displacing several 3H-opiate ligands' binding to rat membranes vary depending on the nature of the ligand, and these agonists differ from the other opiate classes by possessing a relatively hydrophilic component in their C-ring moieties.About:
This article is published in European Journal of Pharmacology.The article was published on 1979-04-01. It has received 173 citations till now. The article focuses on the topics: Opioid peptide & Opiate.read more
Citations
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Journal ArticleDOI
Molecular mechanisms of opioid receptor-dependent signaling and behavior.
TL;DR: There is a continued need for more translational work on opioid receptors in vivo and the authors put into context how opioid receptor signaling leads to the modulation of behavior with the potential for therapeutic intervention.
Journal ArticleDOI
Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist
TL;DR: L-364,718 exhibited a very high selectivity for peripheral CCK receptors relative to brain CCK, gastrin, and various other peptide and nonpeptide receptors in both in vitro radioligand and isolated tissue assays.
Journal ArticleDOI
Uniform assessment and ranking of opioid Mu receptor binding constants for selected opioid drugs
Donna A. Volpe,Grainne A. McMahon Tobin,R. Daniel Mellon,Aspandiar G. Katki,Robert J. Parker,Thomas Colatsky,Timothy J. Kropp,S. Leigh Verbois +7 more
TL;DR: Experiments were conducted to obtain K(i)'s for 19 approved opioid drugs using a single binding assay in a cell membrane preparation expressing recombinant human MOR, adding to the understanding of the pharmacology of opioid drugs and support the development of a more consistent labeling policies regarding safe disposal.
Journal ArticleDOI
Morphiceptin (NH4-tyr-pro-phe-pro-COHN2): a potent and specific agonist for morphine (mu) receptors
TL;DR: The discovery of this specific morphine receptor ligand substantiates the hypothesis of multiple opiate receptors and may prove useful for further investigation of the functions of opiate receptor subtypes.
Journal ArticleDOI
Naloxone attenuates voluntary ethanol intake in rats selectively bred for high ethanol preference
TL;DR: Although naloxone may attenuate the positively reinforcing properties of both ethanol and water, ethanol drinking is a subset of consummatory behaviors that is particularly sensitive to opioid receptor blockade and activation of the endogenous opioid system may be an important mechanism which serves to maintain continued ethanol drinking.
References
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Journal ArticleDOI
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
Journal ArticleDOI
Identification of two related pentapeptides from the brain with potent opiate agonist activity
John J. Hughes,T. W. Smith,H. W. Kosterlitz,Linda A. Fothergill,B. A. Morgan,Howard R. Morris +5 more
TL;DR: The evidence is based on the determination of the amino acid sequence of natural enkephalin by the dansyl–Edman procedure and by mass spectrometry followed by synthesis and comparison of the natural and synthetic peptides.
Journal Article
The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
TL;DR: It has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists.
Journal ArticleDOI
Endogenous opioid peptides: multiple agonists and receptors
TL;DR: It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor.
Related Papers (5)
Endogenous opioid peptides: multiple agonists and receptors
Multiple opiate receptors. Enkephalins and morphine bind to receptors of different specificity.
K J Chang,P Cuatrecasas +1 more