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(+)-[3H]SK&F 10,047 binding sites in rat liver.
N N Samovilova1, L V Nagornaya, V A Vinogradov
1Laboratory of Peptide Biochemistry and Pharmacology, Institute of Experimental Cardiology, Cardiology Research Center of the USSR, Moscow.
European Journal of Pharmacology
|March 1, 1988
Summary
Researchers found stereospecific binding sites for (+)-[3H]SKF 10,047 in rat liver, identifying them as sigma-type opioid receptors. These findings suggest a novel
Area of Science:
- Pharmacology
- Neuroscience
- Biochemistry
Background:
- Opioid receptors are crucial in the central nervous system.
- Sigma receptors are a distinct class of opioid receptors.
- The role of sigma receptors in peripheral organs like the liver is less understood.
Purpose of the Study:
- To investigate the presence and characteristics of (+)-[3H]SKF 10,047 binding sites in rat liver.
- To determine if these sites represent sigma-type opioid receptors.
- To explore the potential physiological significance of these receptors in the liver.
Main Methods:
- Radioligand binding assays using (+)-[3H]SKF 10,047.
- Characterization of binding properties: reversibility, saturability, stereospecificity.
- Assessment of the influence of ions and various pharmacological agents on binding.
Main Results:
- Stereospecific binding sites for (+)-[3H]SKF 10,047 were identified in rat liver homogenates.
- Binding characteristics were consistent with sigma-type opioid receptors.
- Ions and drugs modulated the binding in a manner typical for sigma receptors.
Conclusions:
- Rat liver possesses stereospecific binding sites for (+)-[3H]SKF 10,047, identified as sigma-type opioid receptors.
- These findings suggest a potential role for sigma receptors in liver function.
- The study proposes these liver and brain binding sites form a novel 'sigmergic' regulatory system.