Komulainen H, Tuomisto J, Airaksinen M M, Kari I, Peura P, Pollari L
Acta Pharmacol Toxicol (Copenh). 1980 Apr;46(4):299-307. doi: 10.1111/j.1600-0773.1980.tb02458.x.
The structure activity relationships of tryptolines and some other beta-carbolines and tryptamines as inhibitors of serotonin (5-HT), dopamine (DA) and noradrenaline (NA) uptake were studied in rat brain synaptosomes. All beta-carbolines inhibited to higher degree the uptake of 5-HT than that of DA or NA(IC50's 5-100 times lower). The most potent tryptoline derivative was 6-hydroxy-tetrahydro-beta-carboline (5-hydroxytryptoline, 6-OH-THBC) with an IC50 of 5.0 x 10(-7) M at a 5-HT concentration of 10(-7) M. 6-Methoxy-tetrahydro-beta-carboline (5-methoxytryptoline) was slightly weaker; the inhibition of 5-HT uptake and DA uptake being competitive. Also tetrahydro-beta-carboline (tryptoline) was more potent than its 1-methylderivative, tetrahydroharmane (methtryptoline) or norharmane (beta-carboline). All of them were, however, weaker inhibitors of 5-HT uptake than the freely rotating indoleamines N-methyl-tryptamine (N-Me-T) or 5-HT itself. N-Me-T and 5-HT were also more potent inhibitors of DA and NA uptake than most of the beta-carbolines, DA uptake, however, was inhibited better by 6-OH-THBC than by 5-HT or N-ME-T. Tetrahydro-beta-carbolines may inhibit 5-HT uptake also in vivo but is unlikely that catecholamine uptake is affected.
在大鼠脑突触体中研究了色满卡林及其他一些β-咔啉和色胺作为5-羟色胺（5-HT）、多巴胺（DA）和去甲肾上腺素（NA）摄取抑制剂的构效关系。所有β-咔啉对5-HT摄取的抑制程度均高于对DA或NA摄取的抑制程度（IC50低5至100倍）。最有效的色满卡林衍生物是6-羟基-四氢-β-咔啉（5-羟基色满卡林，6-OH-THBC），在5-HT浓度为10(-7) M时，其IC50为5.0×10(-7) M。6-甲氧基-四氢-β-咔啉（5-甲氧基色满卡林）稍弱一些；对5-HT摄取和DA摄取的抑制是竞争性的。此外，四氢-β-咔啉（色满卡林）比其1-甲基衍生物四氢哈尔满（甲基色满卡林）或去氢哈尔满（β-咔啉）更有效。然而，它们对5-HT摄取的抑制作用均弱于可自由旋转的吲哚胺N-甲基色胺（N-Me-T）或5-HT本身。N-Me-T和5-HT对DA和NA摄取的抑制作用也比大多数β-咔啉更强，不过，6-OH-THBC对DA摄取的抑制作用优于5-HT或N-Me-T。四氢-β-咔啉在体内也可能抑制5-HT摄取，但不太可能影响儿茶酚胺摄取。
