Carratù M R, De Serio A, Lagioia R, Conte-Camerino D, Ferrari E, Mitolo-Chieppa D
Istituto di Farmacologia, Università di Bari.
Boll Soc Ital Biol Sper. 1990 Jan;66(1):35-42.
Transdihydrolisuride (terguride), a 9,10-dihydrogenated analogue of the ergot dopamine agonist lisuride, is characterized as partial dopamine receptor agonist at CNS level. This compound was investigated for its effects on peripheral neurotransmission in the attempt to delineate its pharmacological profile. The contractile responses of field-stimulated mouse vas deferens were slightly inhibited by terguride at very high concentrations (10(-5)-10(-2) M); the selective antagonists for alpha 2-adrenergic and dopamine receptors failed to counteract this effect. Terguride was very effective in blocking the inhibitory effects of LY 171555 (selective DA2 agonist), SK&F 38393 (selective DA1 agonist) and clonidine (selective alpha 2 agonist). In no case the antagonism was competitive: the control dose-response curves were not shifted in a parallel and dose-dependent manner. Therefore terguride displays a mixed DA1, DA2 and alpha 2 antagonistic activity.
反式二氢麦角乙脲（替古瑞肽）是麦角多巴胺激动剂麦角乙脲的9,10-二氢化类似物，在中枢神经系统水平上被表征为部分多巴胺受体激动剂。对该化合物对外周神经传递的影响进行了研究，以描绘其药理学特征。在非常高的浓度（10⁻⁵ - 10⁻² M）下，替古瑞肽对电场刺激的小鼠输精管的收缩反应有轻微抑制作用；α₂-肾上腺素能受体和多巴胺受体的选择性拮抗剂未能抵消这种作用。替古瑞肽在阻断LY 171555（选择性DA₂激动剂）、SK&F 38393（选择性DA₁激动剂）和可乐定（选择性α₂激动剂）的抑制作用方面非常有效。在任何情况下，拮抗作用都不是竞争性的：对照剂量-反应曲线没有以平行且剂量依赖性的方式移动。因此，替古瑞肽表现出混合的DA₁、DA₂和α₂拮抗活性。
