Itoh Y, Beaulieu M, Kebabian J W
Eur J Pharmacol. 1984 Apr 13;100(1):119-22. doi: 10.1016/0014-2999(84)90324-8.
SCH 23390 (R(+)-7-chloro-8-hydroxy-2,3,4,5-tetrahydro-3-methyl-1-phenyl-1H-3 -benzazepine) is a potent, relatively selective antagonist of the D-1 dopamine receptor ( Iorio et al., J. Pharmacol. Exp. Ther. 226, 462). Because SKF 75670, the 7-OH analogue of SCH 23390, is a partial D-1 agonist, we conclude that the 7-Cl substituent of SCH 23390 contributes to its D-1 antagonist activity. Because SKF 83509, the desmethyl analogue of SCH 23390, is a selective D-1 antagonist, we conclude that the N-methyl substituent of SCH 23390 is not essential for its D-1 antagonist activity.
SCH 23390（R(+)-7-氯-8-羟基-2,3,4,5-四氢-3-甲基-1-苯基-1H-3-苯并氮杂䓬）是一种强效、相对选择性的D-1多巴胺受体拮抗剂（伊奥里奥等人，《药理学与实验治疗学杂志》226, 462）。由于SCH 23390的7-OH类似物SKF 75670是一种部分D-1激动剂，我们得出结论，SCH 23390的7-氯取代基有助于其D-1拮抗剂活性。由于SCH 23390的去甲基类似物SKF 83509是一种选择性D-1拮抗剂，我们得出结论，SCH 23390的N-甲基取代基对其D-1拮抗剂活性并非必不可少。
