Opiate Receptor Subtypes

1985 ◽  
Author(s):  
John W. Holaday
Keyword(s):  
Opiate Receptor ◽  
Receptor Subtypes

scholarly journals Opiate Modulation of Gastrointestinal Motility and the Actions of Trimebutine

1991 ◽  
Vol 5 (5) ◽  
pp. 185-193 ◽  
Author(s):  
Stephen M Collins ◽  
Edwin E Daniel
Keyword(s):  
Postoperative Ileus ◽  
Opiate Receptors ◽  
Opiate Receptor ◽  
Receptor Subtypes ◽  
Control Mechanisms ◽  
Therapeutic Approaches ◽  
Esophageal Sphincter ◽  
Irritable Bowel ◽  
Κ Receptor ◽  
Inhibitory Control Mechanisms

Trimebutine is an opiate ligand that interacts with the μ, σ and κ receptor subclasses with approximately equal affinity. Since opiate receptors are widely distributed in the gut, and because opiate receptor subtypes may be involved in excitatory or inhibitory control mechanisms, trimebutine has an unusual profile of action that cannot be predicted on the basis of experience with other synthetic opiates such as codeine, morphine or loperamide. Trimebutine influences motility throughout the gastrointestinal tract. The effect of trimcbutine on the lower esophageal sphincter raises the possibility of a beneficial role in the treatment of gastroesophageal reflex disease. The ability of trimebutine to promote propulsive activity in the fasting and postprandial small intestine offers novel therapeutic approaches to the treatment of motility disorders, including postoperative ileus and pseudo-obstruction. Finally, the effect of the drug on the colon supports the use of trimcbutine in irritable bowel syndrome patients who have constipation due to colonic inertia.

scholarly journals Comparison of [11C]Diprenorphine and [11C]Carfentanil Binding to Opiate Receptors in Humans by Positron Emission Tomography

1990 ◽  
Vol 10 (4) ◽  
pp. 484-492 ◽  
Author(s):  
J. James Frost ◽  
Helen S. Mayberg ◽  
Bernard Sadzot ◽  
Robert F. Dannals ◽  
John R. Lever ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Specific Binding ◽  
Regional Distribution ◽  
Opiate Receptors ◽  
Opiate Receptor ◽  
Total Radioactivity ◽  
Emission Tomography ◽  
Receptor Subtypes ◽  
Positron Emission ◽  
Kinetics Of

The kinetics and regional distribution of [11C]carfentanil, a μ-selective opiate receptor agonist, and [11C]diprenorphine, a nonselective opiate receptor antagonist, were compared using paired positron emission tomography studies in two normal volunteers. Kinetics of total radioactivity (counts/mCi/pixel) was greater for [11C]diprenorphine than [11C]carfentanil in all regions. [11C]Carfentanil binding (expressed as the total/nonspecific ratio) reached near equilibrium at ∼40 min, whereas [11C]diprenorphine showed a linear increase until ∼60 min. Kinetics of specific binding demonstrated significant dissociation of [11C]carfentanil from opiate receptors, whereas little dissociation of [11C]diprenorphine was observed during the 90-min scan session. Regional distributions of [11C]carfentanil and [11C]diprenorphine were qualitatively and quantitatively different: Relative to the thalamus (a region with known predominance of μ-receptors), [11C]diprenorphine displayed greater binding in the striatum and cingulate and frontal cortex compared to [11C]carfentanil, consistent with labeling of additional, non-μ sites by [11C]diprenorphine. We conclude from these studies that [11C]diprenorphine labels other opiate receptor subtypes in addition to the μ sites selectively labeled by [11C]carfentanil. The nonselective nature of diprenorphine potentially limits its usefulness in defining abnormalities of specific opiate receptor subtypes in various diseases. Development of selective tracers for the δ- and κ-opiate receptor sites, or alternatively use of unlabeled inhibitors to differentially displace μ, δ, and κ subtypes, will help offset these limitations.

Distribution of opiate receptor subtypes and enkephalin and dynorphin immunoreactivity in the hippocampus of squirrel, guinea pig, rat, and hamster

1987 ◽  
Vol 255 (4) ◽  
pp. 497-510 ◽  
Author(s):  
Stafford McLean ◽  
Richard B. Rothman ◽  
Arthur E. Jacobson ◽  
Kenner C. Rice ◽  
Miles Herkenham
Keyword(s):  
Guinea Pig ◽  
Opiate Receptor ◽  
Receptor Subtypes

Effects of traumatic brain injury in rats on binding to forebrain opiate receptor subtypes

1992 ◽  
Vol 16 (1-2) ◽  
pp. 95-107 ◽  
Author(s):  
David C. Perry ◽  
Bruce G. Lyeth ◽  
Leonard P. Miller ◽  
Rena L. Getz ◽  
Larry W. Jenkins ◽  
...  
Keyword(s):  
Traumatic Brain Injury ◽  
Brain Injury ◽  
Opiate Receptor ◽  
Receptor Subtypes
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