Feldman J M, Roche J, Plonk J W
J Clin Pharmacol. 1976 Feb-Mar;16(2-3):106-9. doi: 10.1002/j.1552-4604.1976.tb02390.x.
Cypro, a serotonin and histamine antagonist, has been shown to be a moderately potent reversible inhibitor of tissue monoamine oxidase (MAO) obtained from hamsters and rabbits. In the present study, Cypro inhibits MAO obtained from human platelets with the same potency as harmine (Ki = 5 x 10(-5) M). However, when ten normal volunteers received conventional therapeutic doses of Cypro (16 mg/day) for two days, there was no alteration in their urinary excretion of tryptamine, 5-hydroxyindoleacetic acid, 3-methoxy-4-hydroxymandelic acid, epinephrine, or norepinephrine. We conclude that, when used in conventional clinical doses, Cypro does not inhibit MAO in man.
赛庚啶是一种血清素和组胺拮抗剂,已被证明是从仓鼠和兔子获得的组织单胺氧化酶(MAO)的中度有效可逆抑制剂。在本研究中,赛庚啶抑制从人血小板获得的MAO的效力与 harmine 相同(Ki = 5 x 10(-5) M)。然而,当十名正常志愿者连续两天接受常规治疗剂量的赛庚啶(16 毫克/天)时,他们尿中色胺、5-羟吲哚乙酸、3-甲氧基-4-羟基扁桃酸、肾上腺素或去甲肾上腺素的排泄没有变化。我们得出结论,当以常规临床剂量使用时,赛庚啶不会抑制人体内的MAO。