右美沙芬抑制人血小板对5-羟色胺的摄取，并降低大鼠脑中5-羟吲哚乙酸的含量。

Dextromethorphan inhibits 5-hydroxytryptamine uptake by human blood platelets and decreases 5-hydroxyindoleacetic acid content in rat brain.

作者信息

Ahtee L

出版信息

J Pharm Pharmacol. 1975 Mar;27(3):177-80. doi: 10.1111/j.2042-7158.1975.tb09433.x.

DOI:10.1111/j.2042-7158.1975.tb09433.x

Abstract

The effect of dextromethorphan on the uptake and metabolism of 5-hydroxytryptamine (5-HT) was studied in human blood platelets and in rat brain. In the concentration of 120 nM dextromethorphan inhibited the uptake of 5-HT (1 mu-M) into platelets by 50%. The corresponding concentrations of imipramine and methadone under similar conditions were 22 and 590 nM, respectively. Dextromethorphan (20 to 40 mg kg-1) decreased the concentration of brain 5-hydroxyindoleacetic acid (5-HIAA) and the probenecid-induced accumulation of 5-HIAA time- and dose-dependently. However, dextromethorphan did not alter the pargyline-induced changes in brain 5-HT metabolism. Dextromethorphan-induced changes in brain 5-HT metabolism could arise from the inhibition of the re-uptake of 5-HT into neurons.

摘要

在人体血小板和大鼠脑中研究了右美沙芬对5-羟色胺（5-HT）摄取和代谢的影响。在120 nM的浓度下，右美沙芬可使5-HT（1 μM）进入血小板的摄取量降低50%。在类似条件下，丙咪嗪和美沙酮的相应浓度分别为22 nM和590 nM。右美沙芬（20至40 mg kg-1）可使脑5-羟吲哚乙酸（5-HIAA）的浓度以及丙磺舒诱导的5-HIAA蓄积呈时间和剂量依赖性降低。然而，右美沙芬并未改变帕吉林引起的脑5-HT代谢变化。右美沙芬引起的脑5-HT代谢变化可能源于其对5-HT再摄取进入神经元的抑制作用。