碱性药物在兔血小板5-羟色胺储存细胞器中的蓄积。

Accumulation of basic drugs in 5-hydroxytryptamine storage organelles of rabbit blood platelets.

作者信息

Da Prada M, Pletscher A

出版信息

Eur J Pharmacol. 1975 Jun-Jul;32(02):179-85. doi: 10.1016/0014-2999(75)90281-2.

Abstract

The subcellular distribution of basic substances such as mepacrine, chloroquine, chlorpromazine and imipramine was studied in rabbit blood platelets exposed to these compounds in vitro and to some in vivo. All the drugs showed a preferential concentration in the 5-hydroxytryptamine (5HT) storage organelles (5HT vesicles). Chloroquine and mepacrine accumulated more specifically in the organelles than did chlorpromazine and imipramine. After osmotic shock of the 5HT vesicles chlorpromazine sedimented mostly with the vesicular membranes, whereas the other compounds preferentially went into the supernatant. It is concluded that (a) fluorescent basic compounds such as mepacrine are rather specific markers for the 5HT storage organelles in live platelets and (b) drugs such as chlorpromazine and imipramine also have a considerable affinity for these organelles.

摘要

研究了体外及部分体内暴露于米帕林、氯喹、氯丙嗪和丙咪嗪等碱性物质的兔血小板中这些物质的亚细胞分布。所有药物在5-羟色胺（5HT）储存细胞器（5HT囊泡）中均表现出优先富集。氯喹和米帕林比氯丙嗪和丙咪嗪更特异性地积聚在细胞器中。5HT囊泡经渗透压休克后，氯丙嗪大多与囊泡膜一起沉淀，而其他化合物则优先进入上清液。得出的结论是：（a）荧光碱性化合物如米帕林是活血小板中5HT储存细胞器的相当特异的标志物；（b）氯丙嗪和丙咪嗪等药物对这些细胞器也有相当大的亲和力。