Kohli J D, Glock D, Goldberg L I
Eur J Pharmacol. 1983 Apr 22;89(1-2):137-41. doi: 10.1016/0014-2999(83)90618-0.
Relative activity of domperidone as an antagonist of the two peripheral dopamine (DA) receptors, DA1 and DA2, was studied in pentobarbital-anesthetized dogs. Renal vasodilation produced by intra-arterial injection of DA into the phenoxybenzamine-pretreated renal vascular bed was the DA1-mediated response, while femoral vasodilation induced by dipropyl dopamine injected into the femoral artery with intact nerve supply was the DA2-mediated response. Domperidone, 0.5-5 micrograms/kg intravenously, inhibited the DA2 response by 15-75%. In contrast, doses up to 5 mg/kg had no effect on DA1-mediated or bradykinin-induced renal vasodilation. Domperidone has thus proved to be more selective than other DA2 antagonists, differentiating between the two peripheral DA receptors by a margin of greater than 10(4). Furthermore, domperidone was found to be selective as a DA2 versus alpha 2-adrenergic antagonist as studied on the dog cardioaccelerator nerve, thus, enhancing its value as a selective DA2 antagonist.
在戊巴比妥麻醉的犬中研究了多潘立酮作为两种外周多巴胺（DA）受体DA1和DA2拮抗剂的相对活性。在经酚苄明预处理的肾血管床内动脉注射DA所产生的肾血管舒张是DA1介导的反应，而在神经供应完整的情况下向股动脉注射二丙基多巴胺所诱导的股血管舒张是DA2介导的反应。静脉注射0.5 - 5微克/千克的多潘立酮可使DA2反应抑制15% - 75%。相比之下，高达5毫克/千克的剂量对DA1介导的或缓激肽诱导的肾血管舒张没有影响。因此，已证明多潘立酮比其他DA2拮抗剂更具选择性，区分两种外周DA受体的能力超过10⁴倍。此外，如在犬心加速神经上所研究的，发现多潘立酮作为DA2拮抗剂相对于α2 - 肾上腺素能拮抗剂具有选择性，因此，增强了其作为选择性DA2拮抗剂的价值。
