大鼠颌下腺体外转运δ9-四氢大麻酚的机制研究。

A study of the mechanism of transport of delta9-tetrahydrocannabinol in the rat submaxillary gland in vitro.

作者信息

McConnel W R, Borzelleca J F

出版信息

Arch Int Pharmacodyn Ther. 1978 Oct;235(2):180-6.

Abstract

In vitro studies on rat submaxillary gland slices with 3H-delta9-THC (3.6 X 10(-6)M) showed that this drug was transported into and accumulated by salivary tissue. Approximately 50% of the delta9-THC was firmly bound in or on the tissue. The uptake of 3H-delta9-THC was unchanged from control conditions (pH 7.4, 37 degrees C, 100% oxygen, 3.2 X 10(-6)M) when the metabolic inhibitors, 2,4-dinitrophenol (10(-3)M) and cyanide (10(-3)M) were used or when oxygen was replaced by nitrogen. The efflux of 3H-delta9-THC from salivary gland slices increased following addition of an excess of unlabeled drug. These data suggest a passive transport process for the movement of delta9-THC into salivary tissue with a possible saturable binding site operating on or in the interior of the salivary cell.

摘要

对大鼠下颌下腺切片进行的体外研究表明，用3H-δ9-四氢大麻酚（3.6×10−6M）处理时，这种药物被转运至唾液组织并在其中蓄积。约50%的δ9-四氢大麻酚牢固结合于组织内或组织上。当使用代谢抑制剂2,4-二硝基苯酚（10−3M）和氰化物（10−3M），或用氮气替代氧气时，在对照条件（pH 7.4、37℃、100%氧气、3.2×10−6M）下，3H-δ9-四氢大麻酚的摄取未发生变化。加入过量未标记药物后，唾液腺切片中3H-δ9-四氢大麻酚的流出增加。这些数据表明，δ9-四氢大麻酚进入唾液组织的过程为被动转运，在唾液细胞内或细胞表面可能存在一个可饱和的结合位点。