Velasco M, Luchsinger A
Clinical Pharmacology Unit, José M. Vargas Medical School, Universidad Central de Venezuela, Caracas, Venezuela.
Am J Ther. 1998 Jan;5(1):37-43.
Dopamine is a biogenic amine synthesized in the hypothalamus, in the arcuate nucleus, the caudad, and various areas of the central and peripheral nervous system. It has been widely established that dopamine and its agonists play an important role in cardiovascular, renal, hormonal, and central nervous system regulation through stimulation of alpha and beta adrenergic and dopaminergic receptors. There are several agonists of dopamine-2 (DA 2 ) dopaminergic receptors, such as bromocriptine, pergolide, lisuride, quinpirole, and carmoxirole, which inhibit norepinephrine release and produce a decrease in arterial blood pressure; in some cases, bromocriptine and pergolide also reduce heart rate. From a therapeutic point of view, the above-mentioned agonists are used for treating Parkinson's disease, acting over DA 2 dopaminergic receptors of the nigrostriatal system. Bromocriptine and the other dopaminergic agonists mentioned act over DA 2 receptors of the tuberoinfundibular system, inhibiting prolactin release and decreasing hyperprolactinemia and tumor size. Among DA 1 receptor agonists, we can mention fenoldopam, piribedil, ibopamine, SKF 3893, and apomorphine (nonspecific). Activation of these receptors decreases peripheral resistance, inducing lowering of arterial blood pressure and increases in heart rate, sympathetic tone, and activity of the renin aldosterone system. Among DA 2 receptor antagonists, we can mention metoclopramide, domperidone, sulpiride, and haloperidol. From a therapeutic point of view, metoclopramide and domperidone are used in gastric motility disorders, and haloperidol is used in psychotic alterations. Antagonists of DA 1 receptors are SCH23390 and clozapine. Clozapine is used for treating schizophrenia.
多巴胺是一种在下丘脑、弓状核、尾状核以及中枢和外周神经系统的各个区域合成的生物胺。多巴胺及其激动剂通过刺激α和β肾上腺素能受体以及多巴胺能受体,在心血管、肾脏、激素和中枢神经系统调节中发挥重要作用,这一点已得到广泛证实。有几种多巴胺 -2(DA 2)多巴胺能受体激动剂,如溴隐亭、培高利特、利苏力特、喹吡罗和卡莫西罗,它们抑制去甲肾上腺素释放并导致动脉血压下降;在某些情况下,溴隐亭和培高利特还会降低心率。从治疗角度来看,上述激动剂用于治疗帕金森病,作用于黑质纹状体系统的DA 2多巴胺能受体。溴隐亭和提到的其他多巴胺能激动剂作用于结节漏斗系统的DA 2受体,抑制催乳素释放并降低高催乳素血症和肿瘤大小。在DA 1受体激动剂中,我们可以提到非诺多泮、匹莫齐特、异波帕胺、SKF 3893和阿扑吗啡(非特异性)。这些受体的激活会降低外周阻力,导致动脉血压下降,并使心率、交感神经张力和肾素 - 醛固酮系统的活性增加。在DA 2受体拮抗剂中,我们可以提到甲氧氯普胺、多潘立酮、舒必利和氟哌啶醇。从治疗角度来看,甲氧氯普胺和多潘立酮用于治疗胃动力障碍,氟哌啶醇用于治疗精神障碍。DA 1受体拮抗剂是SCH23390和氯氮平。氯氮平用于治疗精神分裂症。