Dubb J W, Stote R M, Alexander F, Intoccia A P, Geczy M, Pendleton R G
Clin Pharmacol Ther. 1979 Jun;25(6):837-43. doi: 10.1002/cpt1979256837.
DCTQ (SK&F 64139) is a potent inhibitor of both adrenal and central nervous system (CNS) phenylethanolamine N-methyltransferase (PNMT). In animal studies, a plasma level of 0.35 microgram/ml was associated with 50% inhibition of both adrenal and central PNMT. We performed single-dose phase I studies with DCTQ in man. Plasma drug levels up to 6.26 microgram/ml were readily obtained. There were few subjective and no objective clinical changes. DCTQ did not alter blood pressure or cause CNS symptoms in man. Furthermore, resting plasma and urinary catecholamines did not change after DCTQ. The study suggests that acute inhibition of PNMT under resting conditions is without significant clinical effect.
双氯三喹（SK&F 64139）是肾上腺和中枢神经系统（CNS）苯乙醇胺N-甲基转移酶（PNMT）的强效抑制剂。在动物研究中，血浆浓度为0.35微克/毫升时可抑制肾上腺和中枢PNMT达50%。我们对双氯三喹进行了人体单剂量I期研究。很容易获得高达6.26微克/毫升的血浆药物浓度。几乎没有主观症状，也没有客观的临床变化。双氯三喹不会改变人体血压，也不会引起中枢神经系统症状。此外，双氯三喹给药后静息血浆和尿儿茶酚胺没有变化。该研究表明，在静息状态下急性抑制PNMT没有显著临床效果。
