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豚鼠心脏突触前抑制性阿片受体对强啡肽-(1-13)的敏感性。

Sensitivity to dynorphin-(1-13) of the presynaptic inhibitory opiate receptors of the guinea-pig heart.

作者信息

Ledda F, Mantelli L, Corti V

出版信息

Eur J Pharmacol. 1985 Nov 19;117(3):377-80. doi: 10.1016/0014-2999(85)90013-5.

Abstract

Dynorphin-(1-13) at the concentrations of 1-10 microM, produced a dose-dependent inhibition of the cardiac response to field stimulation of the adrenergic nerve terminals in guinea-pig atria pretreated with peptidase inhibitors. This inhibitory effect was competitively antagonized in a dose-dependent manner by 5 and 10 microM naloxone. Since dynorphin-(1-13) did not modify the dose-inotropic effect curve of exogenous noradrenaline, it was concluded that the depressant effect of the opioid agonist was due to the stimulation of the presynaptic inhibitory opiate receptors belonging to the kappa subtype.

摘要

浓度为1 - 10微摩尔的强啡肽 -(1 - 13),对用肽酶抑制剂预处理的豚鼠心房肾上腺素能神经末梢的场刺激所引起的心脏反应产生剂量依赖性抑制作用。这种抑制作用被5和10微摩尔的纳洛酮以剂量依赖性方式竞争性拮抗。由于强啡肽 -(1 - 13)不改变外源性去甲肾上腺素的剂量 - 变力效应曲线,因此得出结论,阿片类激动剂的抑制作用是由于刺激了属于κ亚型的突触前抑制性阿片受体。

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