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KMID : 0360419940300010001
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Korean Journal of Pharmacology
1994 Volume.30 No. 1 p.1 ~ p.9
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Regulation of Histamine Release by Kappa Opioid Receptor in Rat Cortical Slices
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Kim Kee-Won
Cho Kyu-Park
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Abstract
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It has been shown that there are several subtypes of opioid receptor. We examined ligand binding profiles and the effects of various opioid agonists on high potassium-stimulated release of histamine. We have evaluated the properties of binding of anonselective opioid antagonist, in rat cortex membranes. Binding sites was inhibited by the use of an excess of competing selective agonists (DAMGO, DPDPE) for these sites. (-) Ethylketocyclazocine (EKC), DIP and bremazocine inhibited DIP binding. However, arylacetamides (U69593 and U50488H) gave little inhibition Replacement of sodium by NMDG and the addition of guanine nucleotide influenced the inhibitory potency of (-) EKC, an agonist for site, but not of bremazocine. This result suggests that bremazocine can be an antagonist at this binding site. Also, we have examined the opioid modulation of release in rat frontal cortex slices labeled with . The release from cortex slices was inhibited by EKC in a concentration-dependent manner. However, the receptor selective agonists, DPDPE and deltorphine II, receptor agonists, DAMGO and TAPS, , U69593 and U50488H, and did not. The concentration-response curve of EKC was shifted to right in the presence of naloxone, nor-binaltorphimine and bremazocine, respectively. These results suggest that opioid receptor regulates histamine release in the fromtal cortex of the rat.
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KEYWORD
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Kappa, opioid, Receptor binding, Histamine Release, Rat, Cortex
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