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超敏化的药理学研究。VII. 双苄胺对可卡因诱导的豚鼠离体输精管超敏反应的抑制作用。

Pharmacological studies on supersensitization. VII. Inhibitory effect of dibenamine on cocaine-induced supersensitivity of isolated vas deferens of guinea pig.

作者信息

Araki K, Muramatsu M, Kontani H, Gomi Y

出版信息

J Pharmacobiodyn. 1982 Oct;5(10):789-95. doi: 10.1248/bpb1978.5.789.

DOI:10.1248/bpb1978.5.789
PMID:7161706
Abstract

Effects of dibenamine on cocaine-induced supersensitivity of isolated vas deferens of guinea pig were examined. Dibenamine at 1.0 x 10(-7)-1.0 x 10(-5) M attenuated the degree of cocaine-induced increase in sensitivity to acetylcholine without any effect on acetylcholine-contraction. The degree of dibenamine-induced inhibition was dependent on the concentration of dibenamine and inversely related to the concentration of cocaine. Dibenamine at the concentration capable of inhibiting the contractile response to norepinephrine did not affect the degree of the increase in sensitivity to norepinephrine induced by cocaine. Dibenamine diminished the degree of cocaine-induced increase in sensitivity to potassium in standard Tyrode solution and that in maximum response to calcium in partially depolarized vas deferens. Dibenamine at the concentration of 3.2 x 10(-7) M did not affect acetylcholine-contractions and attenuated potassium-contractions of the preparations exposed 5 min to calcium-free Tyrode solution, but the degree of cocaine-induced potentiation of contractile response in calcium-free Tyrode solution was not affected by dibenamine. These results suggest that cocaine-induced increase in calcium influx from extracellular fluid is selectively inhibited by dibenamine.

摘要

研究了双苄胺对可卡因诱导的豚鼠离体输精管超敏反应的影响。1.0×10⁻⁷ - 1.0×10⁻⁵ M的双苄胺可减弱可卡因诱导的对乙酰胆碱敏感性增加的程度,而对乙酰胆碱收缩无任何影响。双苄胺诱导的抑制程度取决于双苄胺的浓度,且与可卡因的浓度呈负相关。能够抑制对去甲肾上腺素收缩反应的双苄胺浓度对可卡因诱导的对去甲肾上腺素敏感性增加的程度没有影响。双苄胺降低了标准台氏液中可卡因诱导的对钾敏感性增加的程度以及部分去极化输精管中对钙最大反应的程度。3.2×10⁻⁷ M浓度的双苄胺对暴露于无钙台氏液5分钟的制剂的乙酰胆碱收缩无影响,但减弱了钾收缩,然而双苄胺不影响无钙台氏液中可卡因诱导的收缩反应增强程度。这些结果表明,双苄胺可选择性抑制可卡因诱导的细胞外液钙内流增加。

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Pharmacological studies on supersensitization. VII. Inhibitory effect of dibenamine on cocaine-induced supersensitivity of isolated vas deferens of guinea pig.超敏化的药理学研究。VII. 双苄胺对可卡因诱导的豚鼠离体输精管超敏反应的抑制作用。
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