β-咔啉与苯二氮䓬受体的相互作用：构效关系

Interactions of beta-carbolines with the benzodiazepine receptor: structure-activity relationships.

作者信息

Robertson H A, Baker G B, Coutts R T, Benderly A, Locock R A, Martin I L

出版信息

Eur J Pharmacol. 1981 Dec 3;76(2-3):281-4. doi: 10.1016/0014-2999(81)90515-x.

Abstract

The effects of a number of beta-carboline derivatives on [3H]flunitrazepam binding to the benzodiazepine binding site were investigated. The potency of beta-carbolines at the benzodiazepine binding site appeared to be determined largely by the aromaticity of the molecule. Norharmane-3-carboxylic acid ethyl ester was considerably more potent (IC50 10 nM) than its tetrahydro-beta-carboline analogue (IC50 6 microM). There is essentially no difference in potency between the (+)- and (--)-forms of the tetrahydro-beta-carboline-3-carboxylate analogues.

摘要

研究了多种β-咔啉衍生物对[³H]氟硝西泮与苯二氮䓬结合位点结合的影响。β-咔啉在苯二氮䓬结合位点的效力似乎很大程度上由分子的芳香性决定。去氢骆驼蓬碱-3-羧酸乙酯的效力（IC50为10 nM）比其四氢-β-咔啉类似物（IC50为6 μM）强得多。四氢-β-咔啉-3-羧酸酯类似物的(+)-和(–)-形式在效力上基本没有差异。