STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS .9. 5-HT1A AND 5-HT2 RECEPTOR AFFINITY OF SOME 2-SUBSTITUTED AND 3-SUBSTITUTED 1,2,3,4-TETRAHYDRO-BETA-CARBOLINES

被引：0

作者：

BOJARSKI, AJ

CEGLA, MT

CHARAKCHIEVAMINOL, S

MOKROSZ, MJ

MACKOWIAK, M

MISZTAL, S

MOKROSZ, JL

机构：

[1] NICHOLAS COPERNICUS MED ACAD,DEPT ORGAN CHEM,PL-31501 KRAKOW,POLAND

[2] POLISH ACAD SCI,DEPT MED CHEM,PL-30060 KRAKOW,POLAND

[3] POLISH ACAD SCI,NEW DRUGS LAB,PL-30060 KRAKOW,POLAND

[4] POLISH ACAD SCI,INST PHARMACOL,PL-30060 KRAKOW,POLAND

来源：

PHARMAZIE | 1993年 / 48卷 / 04期

关键词：

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 5-HT1A and 5-HT2 receptor affinity of 2- and 3-substituted 1,2,3,4-tetrahydro-beta-carbolines 1-8, 10 and 12-15 has been determined. It has been found that the specific 5-HT1A affinity of the protonated form (K(i)AH+) of 2-n-hexyl derivatives 4, 8, 14 and (+)-LSD is of the same order. It has been shown by means of molecular modelling methods that pharmacophores of all the active compounds can adopt a common position at the 5-HT1A receptor model. The model also offers an explanation for the observed stereoselectivity of chiral compounds.

引用

页码：289 / 294

页数：6

共 26 条

[1]

ABRAMOVITCH RA, 1956, J CHEM SOC, V78, P4593

[2]

BAKER RW, 1973, MOL PHARMACOL, V9, P23

[3]

BROSSI A, 1973, J MED CHEM, V16, P419

[4] TETRAHYDRO-BETA-CARBOLINES - AFFINITIES FOR TRYPTAMINE AND SEROTONERGIC BINDING-SITES [J].