Relaxing Effect of Vesnarinone (OPC-8212) on the Tracheal Muscle Strips Isolated from Guinea Pigs.
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概要
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The effect of vesnarinone (OPC-8212), an orally active positive inotropic agent was studied in tracheal muscle isolated from guinea pigs, and the mechanism of its action was analyzed. Vesnarinone (10<SUP>-6</SUP> -10<SUP>-4</SUP> M) caused a concentration-dependent relaxation of tracheal muscle pre-contracted by 10<SUP>-4</SUP> M histamine. The potency of the relaxing effect of vesnarinone was greater than that of theophylline; the pD<SUB>2</SUB> values for vesnarinone and theophylline were 4.9 and 4.5, respectively. Vesnarinone reduced the high-K<SUP>+</SUP>-induced contracture of depolarized tracheal muscle non-competitively (pD''<SUB>2</SUB>=3.7). Vesnarinone at the low concentration of 3 × 10<SUP>-6</SUP> M shifted the concentration-response curve for isoproterenol in a parallel fashion to the left. Vesnarinone additively acted on the relaxing effect of isobutyl methyl xanthine. Propranolol (10<SUP>-5</SUP> M) and reserpine pre-treatment (5 mg/kg, i.p., 24 hr) had no effect on the relaxing effect of vesnarinone. These results suggested that vesnarinone elevated the intracellular cyclic AMP level via phosphodiesterase inhibition, resulting in the tracheal muscle relaxation.
- 公益社団法人 日本薬理学会の論文
著者
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Takeya Kazumi
Department Of Pharmacology Aichi Medical University
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YAJIMA Michio
Department of Pharmacology, Aichi Medical University
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Ando Hiroaki
Department Of Advanced Materials Chemistry Graduate School Of Engineering Yokohama National Universi
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ANDO Hiroaki
Department of Pharmacology, Aichi Medical University
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Ando Sawako
Department of Pharmacology, Aichi Medical University
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Nomura Hirohiko
Department of Pharmacology, Aichi Medical University
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