6-甲氧基-1,2,3,4-四氢-β-咔啉的摄取及其对血小板中5-羟色胺摄取和释放的影响。

The uptake of 6-methoxy-1,2,3,4-tetrahydro-beta-carboline and its effect on 5-hydroxytryptamine uptake and release in blood platelets.

作者信息

Airaksinen M M, Huang J T, Ho B T, Taylor D, Walker K

出版信息

Acta Pharmacol Toxicol (Copenh). 1978 Nov;43(5):375-80. doi: 10.1111/j.1600-0773.1978.tb02281.x.

DOI:10.1111/j.1600-0773.1978.tb02281.x

Abstract

The uptake of 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-MeOTHBC, 5-methoxytryptoline) by rabbit blood platelets was studied by using 3H-labelled compound. A high rate active uptake (Km 6.6 micron), which was inhibited by 5-hydroxytryptamine (5-HT) and cinnanserine, and a slow rate uptake, not inhibited by 5-HT were observed. The intracellular distribution of 3H-6-MeOTHBC in platelets clearly differed from that of 14C-5-HT. 6-MeOTHBC also competitively inhibited the high-rate active (but not the slow passive) uptake of 14C-5-HT, being more active than 5-HT itself. The spontaneous release of the newly taken-up 14C-5-HT from platelets was increased only with high concentrations of 6-MeOTHBC.

摘要

采用³H标记的化合物研究了家兔血小板对6-甲氧基-1,2,3,4-四氢-β-咔啉（6-MeOTHBC，5-甲氧基色胺）的摄取。观察到一种高速率的主动摄取（Km为6.6微米），该摄取被5-羟色胺（5-HT）和肉桂赛宁抑制，以及一种5-HT不抑制的低速率摄取。血小板中³H-6-MeOTHBC的细胞内分布与¹⁴C-5-HT的明显不同。6-MeOTHBC还竞争性抑制¹⁴C-5-HT的高速率主动摄取（但不抑制低速率被动摄取），其活性比5-HT本身更强。仅在高浓度的6-MeOTHBC作用下，新摄取的¹⁴C-5-HT从血小板中的自发释放才会增加。