Hoeldtke R D, Cilmi K M, Mattis-Graves K
Clin Pharmacol Ther. 1984 Sep;36(3):302-6. doi: 10.1038/clpt.1984.179.
DL-Threo-3,4-dihydroxyphenylserine (DL-DOPS) was given to six subjects with severe orthostatic hypotension (OH). On separate days each subject took either 600 or 800 mg DL-DOPS or placebo. DL-DOPS increased norepinephrine (NE) excretion 10,000% and urinary normetanephrine and dihydroxyphenylglycol excretion 400%. DL-DOPS, however, led to only slight increases in excretion of the major NE metabolites 3-methoxy-4-hydroxyphenylglycol and vanillylmandelic acid. Only approximately 2.2% +/- 0.5% (range 0.65% to 3.8%) of the L-stereoisomer (L-DOPS), when given as DL-DOPS, is converted to NE in vivo over 24 hr. DL-DOPS did not affect either supine or upright blood pressure in our subjects. Our findings do not support reports that DL-DOPS may be therapeutically useful in OH.
给6名患有严重直立性低血压(OH)的受试者服用了消旋苏糖型-3,4-二羟基苯丝氨酸(DL-DOPS)。在不同的日子里,每名受试者分别服用600或800毫克DL-DOPS或安慰剂。DL-DOPS使去甲肾上腺素(NE)排泄量增加了10000%,使尿中去甲变肾上腺素和二羟基苯乙二醇排泄量增加了400%。然而,DL-DOPS仅使主要NE代谢产物3-甲氧基-4-羟基苯乙二醇和香草扁桃酸的排泄量略有增加。当以DL-DOPS形式给药时,在24小时内只有约2.2%±0.5%(范围为0.65%至3.8%)的L-立体异构体(L-DOPS)在体内转化为NE。DL-DOPS对我们受试者的仰卧位或直立位血压均无影响。我们的研究结果不支持关于DL-DOPS可能对OH有治疗作用的报道。