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麦角酸二乙酰胺(LSD)及其衍生物对家兔和大鼠的热效应

Hyperthermic effects of D-lysergic acid diethylamide (LSD) and its derivatives in rabbits and rats.

作者信息

Hashimoto H, Hayashi M, Nakahara Y, Niwaguchi T, Ishii H

出版信息

Arch Int Pharmacodyn Ther. 1977 Aug;228(2):314-21.

PMID:303504
Abstract

Several D-lysergic acid diethylamide (LSD) derivatives including metabolites of LSD in animals liver and Streptomyces such as D-lysergic acid ethyl, 2-hydroxyethylamide (LEO), D-lysergic acid ethylamide (LAE), D-norlysergic acid diethylamide (norLSD) and synthetic N6-allyl-D-norlysergic acid diethylamide (allyl-nor LSD) were studied with rabbits and rats. In rabbits, the order of the hyperthermic activities was allyl-norLSD greater than LSD greater than LEO, LAE, nor-LSD, and this order was parallel to that of 5-hydroxytryptamine-like activities of these compounds which was previously studied. However, the order was LAE greater than LSD greater than norLSD IN RATS. The hyperthermic effect of LSD in rabbits was attenuated by methysergide, but not by atropine when these drugs were intraventricularly administered. These results suggest the possibility that the metabolites of LSD contribute to the hyperthermic effect of LSD in rats but not in rabbits, and support the idea that 5-HT receptors are involved in the hyperthermia induced by LSD in rabbits.

摘要

研究人员用兔子和大鼠对几种麦角酸二乙酰胺(LSD)衍生物进行了研究,这些衍生物包括LSD在动物肝脏和链霉菌中的代谢产物,如麦角酸乙酯、2-羟乙酰胺(LEO)、麦角酸乙酰胺(LAE)、去甲麦角酸二乙酰胺(norLSD)以及合成的N6-烯丙基-去甲麦角酸二乙酰胺(烯丙基-去甲LSD)。在兔子中,致热活性的顺序为烯丙基-去甲LSD大于LSD大于LEO、LAE、去甲-LSD,且该顺序与先前研究的这些化合物的5-羟色胺样活性顺序平行。然而,在大鼠中顺序为LAE大于LSD大于去甲LSD。当脑室内注射这些药物时,美西麦角可减弱LSD对兔子的致热作用,但阿托品则无此作用。这些结果表明,LSD的代谢产物可能对LSD在大鼠而非兔子中的致热作用有贡献,并支持5-羟色胺受体参与LSD诱导兔子体温升高的观点。

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