Hilditch A, Drew G M
Eur J Pharmacol. 1985 Oct 8;116(1-2):171-4. doi: 10.1016/0014-2999(85)90199-2.
The antagonist potencies of SCH 23390 and domperidone have been determined at vascular and neuronal dopamine receptors in the rabbit isolated splenic artery and rectococcygeus muscle, respectively. SCH 23390 was a potent, competitive antagonist at vascular (pA2 = 10.65) but not neuronal (pA2 less than 6.0) receptors. Domperidone was a potent, competitive antagonist at neuronal (pA2 = 7.9) but not vascular (pA2 less than 4.0) receptors. SCH 23390 and domperidone are, therefore, highly selective vascular and neuronal dopamine receptor antagonists respectively.
已分别测定了SCH 23390和多潘立酮在兔离体脾动脉血管多巴胺受体及直肠尾骨肌神经多巴胺受体上的拮抗效价。SCH 23390是血管多巴胺受体的强效竞争性拮抗剂(pA2 = 10.65),但不是神经多巴胺受体的拮抗剂(pA2小于6.0)。多潘立酮是神经多巴胺受体的强效竞争性拮抗剂(pA2 = 7.9),但不是血管多巴胺受体的拮抗剂(pA2小于4.0)。因此,SCH 23390和多潘立酮分别是高度选择性的血管和神经多巴胺受体拮抗剂。