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

Autor: Robertson HA, Baker GB, Coutts RT, Benderly A, Locock RA, Martin IL
Jazyk: angličtina
Zdroj: European journal of pharmacology [Eur J Pharmacol] 1981 Dec 03; Vol. 76 (2-3), pp. 281-4.
DOI: 10.1016/0014-2999(81)90515-x
Abstrakt: 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.
Databáze: MEDLINE