烷基黄嘌呤的正性肌力作用并非由于腺苷受体阻断的证据。
Evidence that the positive inotropic effects of the alkylxanthines are not due to adenosine receptor blockade.
作者信息
Collis M G, Keddie J R, Torr S R
出版信息
Br J Pharmacol. 1984 Feb;81(2):401-7. doi: 10.1111/j.1476-5381.1984.tb10092.x.
Abstract
We investigated the possibility that the positive inotropic effects of the alkylxanthines are due to adenosine receptor blockade. The potency of 8-phenyltheophylline, theophylline and enprofylline as adenosine antagonists was assessed in vitro, using the guinea-pig isolated atrium, and in vivo, using the anaesthetized dog. The order of potency of the alkylxanthines as antagonists of the negative inotropic response to 2-chloroadenosine in vitro, and of the hypotensive response to adenosine in vivo was 8-phenyltheophylline greater than theophylline greater than enprofylline. The order of potency of the alkylxanthines as positive inotropic and chronotropic agents in the anaesthetized dog was enprofylline greater than theophylline greater than 8-phenyltheophylline. The results of this study indicate that the inotropic effects of the alkylxanthines in the anaesthetized dog are not due to adenosine receptor blockade.
摘要
我们研究了烷基黄嘌呤的正性肌力作用是否归因于腺苷受体阻断的可能性。使用豚鼠离体心房在体外以及使用麻醉犬在体内评估了8-苯基茶碱、茶碱和恩丙茶碱作为腺苷拮抗剂的效力。烷基黄嘌呤作为对体外2-氯腺苷负性肌力反应的拮抗剂以及对体内腺苷降压反应的拮抗剂，其效力顺序为8-苯基茶碱＞茶碱＞恩丙茶碱。烷基黄嘌呤作为麻醉犬正性肌力和变时性药物的效力顺序为恩丙茶碱＞茶碱＞8-苯基茶碱。本研究结果表明，麻醉犬中烷基黄嘌呤的肌力作用并非由于腺苷受体阻断。
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