TISSUE DISTRIBUTION, METABOLISM AND EFFECTS OF BUFOTENINE ADMINISTERED TO RATS
TISSUE DISTRIBUTION, METABOLISM AND EFFECTS OF BUFOTENINE ADMINISTERED TO RATS
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DOI：
10.1016/0028-3908(95)00049-c
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发表时间：
1995-07-01
影响因子：
4.7
通讯作者：
PERRY, KW
中科院分区：
文献类型：
--
作者：
FULLER, RW;SNODDY, HD;PERRY, KW
蟾毒替宁（N，N-二甲基-5-羟色胺）是一种5-羟色胺类似物，据报道具有致幻作用。在s.c.大白鼠腹腔注射蟾毒替宁（1、30、100 mg/kg）。在1小时时，蟾毒替宁在肺、心脏和血液中高，在脑和肝中低。未检测到N-单甲基-5-羟色胺，但由于蟾蜍蝶呤代谢，5-羟基吲哚乙酸（5 HIAA）增加。蟾毒替宁消失几乎完全由8 hr. Bufotenine浓度略高于下丘脑和脑干比纹状体或皮质，血清素略有下降，和5 HIAA在这些脑区增加。帕吉林降低了注射蟾毒替宁后血液和组织中5 HIAA的浓度; LY 51641而不是丙炔苯丙胺模拟帕吉林，表明A型而不是B型单胺氧化酶代谢蟾毒替宁。注射蟾毒特尼可增加血清皮质酮浓度，在阻断奎帕嗪引起的类似增加的剂量下，甲麦角林不会阻断这种作用。虽然只有2%的血清素被发现在血小板贫乏的血浆中，超过99%的蟾蜍烯碱被发现在血小板贫乏的血浆中，表明蟾蜍烯碱不储存在血小板中。这些实验表明，蟾蜍烯碱注射到大鼠体内后，部分通过A型单胺氧化酶迅速消除，蟾蜍烯碱穿透血脑屏障的能力很差。
Bufotenine (N,N-dimethyl-5-hydroxytryptamine) is a serotonin analog reported to be hallucinogenic. Bufotenine concentrations were measured by liquid chromatography with electrochemical detection after the s.c. injection of bufotenine (1,30 or 100 mg/kg) into rats. At 1 hr, bufotenine was high in lung, heart and blood and lower in brain and liver. No N-monomethyl-5-hydroxytryptamine was detected, but 5-hydroxyindoleacetic acid (5HIAA) was increased due to bufotenine metabolism. Bufotenine disappeared nearly completely by 8 hr. Bufotenine concentrations were slightly higher in hypothalamus and brain stem than in striatum or cortex; serotonin was slightly decreased, and 5HIAA was increased in these brain regions. Pargyline reduced concentrations of 5HIAA in blood and tissues after bufotenine injection; LY51641 but not deprenyl mimicked pargyline, suggesting type A not type B monoamine oxidase metabolizes bufotenine. Bufotenine injection increased serum corticosterone concentration, an effect not blocked by metergoline at a dose that blocked a similar increase elicited by quipazine. Although only 2% of the serotonin was found in platelet-poor plasma, more than 99% of the bufotenine was found in platelet-poor plasma, indicating that bufotenine is not stored in platelets. These experiments indicate that bufotenine is rapidly eliminated, in part by type A monoamine oxidase, after its injection into rats and that bufotenine penetrates the blood-brain barrier poorly.