Relation of Diltiazem Binding Sites to Opioid Receptor Subtypes in the Guinea-pig Brain

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概要

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• Interactions between diltiazem and opioids in guinea-pig brain membrane preparations were examined. Diltiazem did not inhibit bindings of ^3H-dihydromorphine (^3H-DHM), ^3H-ethylketocyclazocine (^3H-EKCZ) and ^3H-naloxone (^3H-NOX) but inhibited binding of ^3H-[D-Ala^2, D-Leu^5]-enkephalin (^3H-DADLE). In ^3H-DADLE binding, diltiazem decreased the reciprocal indices of affinity (Kd values) of ^3H-DADLE without changing on the maximal saturable binding (B. max) in guinea-pig brain membranes. These effects of diltiazem on the binding of ^3H-DADLE were enhanced by 2.5mM CaCl_2. Morphine, EKCZ, naloxone and even DADLE did not change the binding of ^3H-diltiazem. These results suggest that the current of information concerning diltiazem and DADLE binding sites is one-way only so that no interaction exists.

• 東海大学の論文

著者

• Oka Tetsuo

  Department Of Pharmacology School Of Medicine Tokai University

• ISHIZUKA Yoshihisa

  Department of Pharmacology, School of Medicine, Tokai University

• Ishizuka Yoshihisa

  Department Of Pharmacology School Of Medicine Tokai University

• OKA Tetsuo

  Department of Clinical Pharmacology, School of Medicine, Tokai University

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