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在离体豚鼠心脏中,布立马胺对可乐定在心脏收缩性、磷酸化酶激活及环磷酸腺苷方面作用的阻断。

Blockade by burimamide of the effects of clonidine on cardiac contractility phosphorylase activation and cyclic adenosine monophosphate in isolated guinea pig heart.

作者信息

Verma S C, McNeill J H

出版信息

Indian J Physiol Pharmacol. 1980 Apr-Jun;24(2):77-83.

PMID:6247271
Abstract

Clonidine in a dose-range of 2.5 microgram to 80 microgram caused positive inotropic effect, which was accompanied by increase in the cyclic AMP levels and phosphorylase-activation of the isolated perfused guinea pig heart. Clonidine-induced biochemical and mechanical effects were blocked by burimamide, an H2-receptor antagonist Propranolol (1 x 10(-6)M), phentolamine (1 x 10(-6)M) or reserpine pretreatment, did not affect the clonidine responses on the perfused guinea pig heart. Clonidine reduced the 4-methyl-histamine (H2-agonist) responses of guinea pig heart. Our data suggest that the cardiac effects of clonidine may be due to stimulation of H2-type of receptors.

摘要

剂量范围为2.5微克至80微克的可乐定可产生正性肌力作用,同时伴有离体灌注豚鼠心脏中环磷酸腺苷水平升高和磷酸化酶激活。H2受体拮抗剂布立马胺可阻断可乐定诱导的生化和机械效应。普萘洛尔(1×10⁻⁶M)、酚妥拉明(1×10⁻⁶M)或利血平预处理不影响可乐定对灌注豚鼠心脏的反应。可乐定可降低豚鼠心脏对4-甲基组胺(H2激动剂)的反应。我们的数据表明,可乐定的心脏效应可能是由于刺激了H2型受体。

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