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某些β-肾上腺素能受体激动剂对利血平诱导的小鼠体温过低的拮抗作用。

Antagonism of reserpine-induced hypothermia in mice by some beta-adrenoceptor agonists.

作者信息

Ross S B

出版信息

Acta Pharmacol Toxicol (Copenh). 1980 Nov;47(5):347-50. doi: 10.1111/j.1600-0773.1980.tb01570.x.

Abstract

The reversal of reserpine-induced hypothermia in mice be three beta-adrenoceptor agonists, terbutaline, salbutamol and clenbuterol, was examined. Terbutaline, 5 and 20 mg/kg intraperitoneally, caused a slight reversal of the hypothermia. Salbutamol, 5 mg/kg intraperitoneally, produced a pronounced and 1 mg/kg a slight reversal. Clenbuterol was very potent in reversing the hypothermic effect of reserpine with significant effect at 0.02 mg/kg intraperitoneally. Propranolol, 2.5 mg/kg intraperitoneally, and the selective beta 2-receptor antagonist IPS 339, 5 mg/kg intraperitoneally, almost completely antagonized the effect of clenbuterol, 1 mg/kg intraperitoneally. The beta-receptor antagonist metoprolol at 5 and 25 mg/kg intraperitoneally only partially antagonized the effect of clenbuterol. Since clenbuterol is much more lipophilic than salbutamol and terbutaline, it is suggested that the reserpine reversal produced by clenbuterol is at least partially of central origin and possibly mediated by stimulation of noradrenergic beta 2-receptors.

摘要

研究了三种β-肾上腺素受体激动剂特布他林、沙丁胺醇和克伦特罗对利血平诱导的小鼠体温过低的逆转作用。腹腔注射5毫克/千克和20毫克/千克的特布他林可使体温过低略有逆转。腹腔注射5毫克/千克的沙丁胺醇可产生明显的逆转作用,而1毫克/千克则产生轻微的逆转作用。克伦特罗在逆转利血平的体温过低作用方面非常有效,腹腔注射0.02毫克/千克时就有显著效果。腹腔注射2.5毫克/千克的普萘洛尔和5毫克/千克的选择性β2受体拮抗剂IPS 339几乎完全拮抗了腹腔注射1毫克/千克克伦特罗的作用。腹腔注射5毫克/千克和25毫克/千克的β受体拮抗剂美托洛尔仅部分拮抗了克伦特罗的作用。由于克伦特罗比沙丁胺醇和特布他林的亲脂性强得多,因此提示克伦特罗产生的利血平逆转作用至少部分源于中枢,可能是通过刺激去甲肾上腺素能β2受体介导的。

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