Characteristics of the inhibition of ligand binding to serotonin receptors in rat brain membranes by verapamil.

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概要

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• Characteristics of the interaction of verapamil with serotonin receptors were studied in rat brain membranes using a radioligand binding technique. While verapamil competed for the [<SUP>3</SUP>H]ketanserin binding sites at low concentrations with the K<SUB>i</SUB> value of 0.41 μM, much higher concentrations were needed to inhibit the binding of [<SUP>3</SUP>H]serotonin to its binding sites, indicating higher affinity of verapamil binding for 5-HT<SUB>2</SUB> than 5-HT<SUB>1</SUB> receptors. The inhibitory action of verapamil on the [<SUP>3</SUP>H]ketanserin binding was stereoselective; the (-)isomer was about ten times more potent than the (+)isomer. The interaction of verapamil with [<SUP>3</SUP>H]ketanserin was competitive and reversible. While D600, a verapamil derivative, also competed for the [<SUP>3</SUP>H]ketanserin binding sites, nifedipine and nicardipine had practically no ability to inhibit the ligand binding to 5-HT<SUB>1</SUB> or 5-HT<SUB>2</SUB> receptors. Although diltiazem competed for 5-HT<SUB>2</SUB> receptors, the affinity was much less than verapamil and D600.

• 公益社団法人 日本薬理学会の論文

著者

• Adachi Hideyuki

  Department Of Cardiovascular Disease Research Eisai Tsukuba Research Laboratories

• Shoji Tadao

  Department of Applied Chemistry, Faculty of Engineering, Keio University

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