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阿扑吗啡对大鼠胃分泌的作用机制。

Mechanism of action of apomorphine on rat gastric secretion.

作者信息

Costall B, Naylor R J, Tan C C

出版信息

Eur J Pharmacol. 1985 Oct 22;116(3):279-85. doi: 10.1016/0014-2999(85)90163-3.

Abstract

The effects of apomorphine on the volume of gastric secretion and its content of H+, K+, Na+ and Cl- were determined in conscious rats having gastric cannulas. Apomorphine dose-dependently (0.25-0.5 mg/kg s.c.) decreased the volume of gastric secretion, its acid concentration and, at the highest dose, Cl- concentration. However, Na+ and K+ concentrations were unchanged. The alpha 1- and alpha 2-adrenoceptor antagonists prazosin (0.25-0.5 mg/kg i.p.) and yohimbine (5-10 mg/kg i.p.), the beta 1- and beta 2-adrenoceptor antagonist propranolol (5 mg/kg i.p.), the beta 2-adrenoceptor antagonist ICI 118551 (1 mg/kg i.p.) and the dopamine receptor antagonists haloperidol (0.25-2.5 mg/kg i.p.), metoclopramide (2.5-10 mg/kg i.p.) or domperidone (2.5 mg/kg i.p.), administered alone, had little or no effect on the volume, H+, Na+ or Cl- concentrations of gastric secretion. Propranolol prevented the action of apomorphine to reduce the volume of gastric secretion but failed to modify the reductions in H+ and Cl- concentrations. The action of propranolol was mimicked by ICI 118551 but not by the beta 1-adrenoceptor antagonist atenolol. Yohimbine, prazosin or domperidone had little or no effect on the actions of apomorphine. Haloperidol (0.5 mg/kg i.p.) and metoclopramide (10 mg/kg i.p.) antagonised apomorphine's action to reduce H+ and Cl- concentrations but significantly enhanced the action of apomorphine to reduce the volume of gastric secretion. The results suggest that the ability of apomorphine to reduce the volume of gastric secretion is mediated via beta 2-adrenoceptors whilst acid concentration is reduced via an action on neuroleptic sensitive receptors.

摘要

在有胃插管的清醒大鼠中,测定了阿扑吗啡对胃分泌量及其H⁺、K⁺、Na⁺和Cl⁻含量的影响。阿扑吗啡剂量依赖性地(皮下注射0.25 - 0.5mg/kg)减少胃分泌量、胃酸浓度,且在最高剂量时降低Cl⁻浓度。然而,Na⁺和K⁺浓度未发生变化。α₁和α₂肾上腺素能受体拮抗剂哌唑嗪(腹腔注射0.25 - 0.5mg/kg)和育亨宾(腹腔注射5 - 10mg/kg)、β₁和β₂肾上腺素能受体拮抗剂普萘洛尔(腹腔注射5mg/kg)、β₂肾上腺素能受体拮抗剂ICI 118551(腹腔注射1mg/kg)以及多巴胺受体拮抗剂氟哌啶醇(腹腔注射0.25 - 2.5mg/kg)、甲氧氯普胺(腹腔注射2.5 - 10mg/kg)或多潘立酮(腹腔注射2.5mg/kg)单独给药时,对胃分泌量、H⁺、Na⁺或Cl⁻浓度几乎没有影响。普萘洛尔可阻止阿扑吗啡减少胃分泌量的作用,但未能改变H⁺和Cl⁻浓度的降低。ICI 118551可模拟普萘洛尔的作用,但β₁肾上腺素能受体拮抗剂阿替洛尔则不能。育亨宾、哌唑嗪或多潘立酮对阿扑吗啡的作用几乎没有影响。氟哌啶醇(腹腔注射0.5mg/kg)和甲氧氯普胺(腹腔注射10mg/kg)可拮抗阿扑吗啡降低H⁺和Cl⁻浓度的作用,但显著增强了阿扑吗啡减少胃分泌量的作用。结果表明,阿扑吗啡减少胃分泌量的能力是通过β₂肾上腺素能受体介导的,而胃酸浓度的降低是通过作用于抗精神病药物敏感受体实现的。

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