SCH 23390和SK&F 83566是血管多巴胺和5-羟色胺受体的拮抗剂。
SCH 23390 and SK&F 83566 are antagonists at vascular dopamine and serotonin receptors.
作者信息
Ohlstein E H, Berkowitz B A
出版信息
Eur J Pharmacol. 1985 Jan 22;108(2):205-8. doi: 10.1016/0014-2999(85)90728-9.
SCH 23390 and SK&F 83566 have been utilized as selective antagonists at postjunctional dopamine receptors. However, in the isolated rabbit thoracic aorta evidence for competitive antagonism of serotonin was obtained. The KB values were 11 and 34 nM for SK&F R-83566 and SCH 23390, respectively. The S-enantiomer of SK&F 83566 was a weaker antagonist at the vascular serotonin receptor (KB = 1.5 microM). Thus, these results indicate that SCH 23390 and SK&F 83566 are not totally specific for the dopamine DA-1 receptor because they can also be potent antagonists at the vascular serotonin receptor.
SCH 23390和SK&F 83566已被用作节后多巴胺受体的选择性拮抗剂。然而，在离体兔胸主动脉中，获得了5-羟色胺竞争性拮抗的证据。SK&F R-83566和SCH 23390的KB值分别为11和34 nM。SK&F 83566的S-对映体是血管5-羟色胺受体的较弱拮抗剂（KB = 1.5 microM）。因此，这些结果表明SCH 23390和SK&F 83566对多巴胺DA-1受体并非完全特异，因为它们也可以是血管5-羟色胺受体的强效拮抗剂。
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