Soblosky J S, Dills C, DuMontier G, Jeng I
Neurochemistry Research Unit, Missouri Institute of Psychiatry, St. Louis 63139.
Biochem Int. 1987 May;14(5):797-803.
The displacement characteristics of [3H]5-hydroxytryptamine (5-HT1) binding by several serotonergic ligands were studied in the chick embryo brain. Although most of ligands tested displaced [3H]5-HT in a manner suggestive of a single site, displacement curves for (+/-)-8-hydroxy-dipropylaminotetralin (8-OH-DPAT), 5-methoxytryptamine, 5-methyltryptamine and 5-methoxy-N,N-dimethyltryptamine displayed non-unity Hill plots, suggesting multiple site interactions. However, if spiperone (2 microM) was included in the assays, the Hill coefficients of these compounds were all similarly increased toward unity, suggesting that 8-OH-DPAT as well as 5-methoxy and 5-methyl substituted tryptamines, have a high affinity for and can discriminate 5-HT1A binding sites in the chick embryo brain.
在鸡胚脑中研究了几种血清素能配体对[3H]5-羟色胺(5-HT1)结合的置换特性。尽管大多数测试的配体以提示单一位点的方式置换[3H]5-羟色胺,但(±)-8-羟基二丙基氨基四氢萘(8-OH-DPAT)、5-甲氧基色胺、5-甲基色胺和5-甲氧基-N,N-二甲基色胺的置换曲线显示出非单一的希尔图,提示存在多位点相互作用。然而,如果在测定中加入螺哌隆(2μM),这些化合物的希尔系数都类似地向单一性增加,表明8-OH-DPAT以及5-甲氧基和5-甲基取代的色胺对鸡胚脑中的5-HT1A结合位点具有高亲和力且能够区分。