κ-阿片受体激动剂加μ-阿片受体拮抗剂协同抑制结肠氯离子分泌的阿片类药物作用
Synergistic opioid inhibition of colonic Cl- secretion by kappa-opioid receptor agonism plus mu-opioid receptor antagonism.
作者信息
Kromer W
机构信息
Department of Pharmacology, Byk Gulden Pharmaceuticals, Konstanz, Germany.
出版信息
Eur J Pharmacol. 1993 Jan 12;230(2):235-7. doi: 10.1016/0014-2999(93)90808-u.
On the basis of the novel concept of a dual prosecretory/antisecretory intestinal opioid system, a voltage-clamp experiment was performed with guinea-pig colonic mucosa, and net anion (Cl-) secretion was measured after stimulation with prostaglandin E1 (PGE1) plus theophylline. Synergism between kappa-opioid receptor agonism by U69593 and mu-opioid receptor antagonism by CTOP-NH2 (D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2) was observed.
基于双分泌/抗分泌肠道阿片系统这一新概念，对豚鼠结肠黏膜进行了电压钳实验，并在用前列腺素E1（PGE1）加茶碱刺激后测量净阴离子（Cl-）分泌。观察到U69593对κ-阿片受体的激动作用与CTOP-NH2（D-苯丙氨酸-半胱氨酸-酪氨酸-D-色氨酸-鸟氨酸-苏氨酸-青霉胺-苏氨酸-NH2）对μ-阿片受体的拮抗作用之间存在协同作用。
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