Neurochemical Investigation on the Effects of a New Diphenylpiperazine Calcium Antagonist, KB-2796, on the Central Dopaminergic System of Rats.
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概要
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The effects of KB-2796, a new diphenylpiperazine calcium antagonist, on the striatal dopaminergic system of rats were investigated in comparison with various calcium antagonists and the dopamine antagonist chlorpromazine. The inhibiting effect of KB-2796 on [<SUP>3</SUP>H]spiperone binding to striatal membranes in vitro was weaker than those of chlorpromazine and the other diphenylpiperazine analogues, flunarizine and cinnarizine, and more potent than those of verapamil and nicardipine. Diltiazem and nifedipine were inactive. KB-2796 (30, 100 mg/kg, p.o.) had no effect on K<SUB>d</SUB> and B<SUB>max</SUB> values of in vitro [<SUP>3</SUP>H]spiperone specific binding to striatal membranes obtained from the rat at 36 hr and 7 days after repeated administration for 18 days, whereas flunarizine (30 mg/kg, p.o.) and chlorpromazine (3 mg/kg, p.o.) increased B<SUB>max</SUB> values by 47% and 31%, respectively, at 36 hr, but not at 7 days after the final administration. At 1 hr after the single administration, KB-2796 (30, 100 mg/kg, p.o.) had no effect on the content of dopamine and its metabolites in the striatum, whereas flunarizine (30 mg/kg, p.o.) and chlorpromazine (3 mg/kg, p.o.) increased the level of homovanillic acid. These results indicate that flunarizine may affect dopaminergic neurotransmission by partially blocking dopamine D<SUB>2</SUB> receptors, while KB-2796 has negligible in vivo effect on the dopaminergic system.
- 公益社団法人 日本薬理学会の論文
著者
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YAMASHITA Akira
New Drug Research Laboratories, Kanebo, Ltd.
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Yamashita Akira
New Drug Research Laboratories Kanebo Ltd.
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SUKAMOTO Takayuki
New Drug Discovery Research Laboratory, Kanebo Ltd.
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Hara Hideaki
New Drug Research Laboratories, Kanebo, Ltd.
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Ito Keizo
New Drug Research Laboratories, Kanebo, Ltd.
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Ikegami Akira
New Drug Research Laboratories, Kanebo, Ltd.
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Ozaki Akio
New Drug Research Laboratories, Kanebo, Ltd.
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