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泮库溴铵与阿库氯铵毒蕈碱拮抗作用的比较。

A comparison of the muscarinic antagonist actions of pancuronium and alcuronium.

作者信息

Dalton D W, Tyers M B

出版信息

J Auton Pharmacol. 1982 Dec;2(4):261-6. doi: 10.1111/j.1474-8673.1982.tb00518.x.

Abstract

1 In the pithed rat, muscarine (2.5-10 microgram/kg i.v.) normally produced bradycardias, but tachycardias were seen in the presence of pancuronium (0.1-1.0 mg/kg i.v.) and alcuronium (0.1-5.0 mg/kg i.v.). 2 The tachycardia was probably a result of muscarinic receptor stimulation, because it was antagonized by atropine (10 microgram/kg i.v.) and pirenzepine (10-30 microgram/kg i.v.). The location of these muscarinic receptors is probably within the sympathetic ganglia since the tachycardias were inhibited by pretreatment with propranolol (1 mg/kg i.v.) or reserpine (5 mg/kg i.p. 24 h prior to study). 3 In the rat isolated atria preparation, pancuronium was 86 times more potent as an antagonist of the effects of muscarine than in the rat isolated superior cervical ganglion. The mechanism of action in both tissues may be non-competitive. 4 Pancuronium selectivity antagonized atrial inhibitory muscarinic responses compared to excitatory muscarinic responses in sympathetic ganglia in the rat.

摘要
  1. 在脊髓被破坏的大鼠中,毒蕈碱(静脉注射2.5 - 10微克/千克)通常会引起心动过缓,但在泮库溴铵(静脉注射0.1 - 1.0毫克/千克)和阿库氯铵(静脉注射0.1 - 5.0毫克/千克)存在的情况下会出现心动过速。2. 心动过速可能是毒蕈碱受体受刺激的结果,因为它可被阿托品(静脉注射10微克/千克)和哌仑西平(静脉注射10 - 30微克/千克)拮抗。这些毒蕈碱受体的位置可能在交感神经节内,因为在研究前用普萘洛尔(静脉注射1毫克/千克)或利血平(腹腔注射5毫克/千克,提前24小时)预处理可抑制心动过速。3. 在大鼠离体心房制备中,泮库溴铵作为毒蕈碱作用拮抗剂的效力比在大鼠离体颈上神经节中高86倍。两种组织中的作用机制可能是非竞争性的。4. 与大鼠交感神经节中的兴奋性毒蕈碱反应相比,泮库溴铵选择性拮抗心房抑制性毒蕈碱反应。

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