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β ‐Carbolines: Endogenous Ligands for the Benzodiazepine Receptor
Author(s) -
Ogawa Norio,
Mori Akitane
Publication year - 1984
Publication title -
psychiatry and clinical neurosciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.609
H-Index - 74
eISSN - 1440-1819
pISSN - 1323-1316
DOI - 10.1111/j.1440-1819.1984.tb02826.x
Subject(s) - chemistry , diazepam , ligand (biochemistry) , benzodiazepine , endogeny , receptor , intraperitoneal injection , carboxylic acid , gabaa receptor , pharmacology , medicinal chemistry , stereochemistry , biochemistry , medicine
Abstract: The interaction of benzodiazepines (BDZ) and β ‐carbolines with metal cations was investigated. Δmong the numerous transition metal cations, only four, Co 2+ , Ni 2 , Cu 2+ and Zn 2+ , specifically affected the receptor binding of [ 3 H]diazepam and [ 3 H] β ‐carboline‐3‐carboxylic acid ethyl ester ( β ‐CCE). The effects of these cations on [ 3 H]diazepam binding were exactly opposite to those on [ 3 H] β ‐CCE binding. An intraperitoneal injection of β ‐carboline‐3‐carboxylic acid methyl ester ( β ‐CCM) produced spike discharges and β‐CCM induced spike discharges were prevented by an intramuscular injection of BDZ. These findings suggest that β ‐carbolines could be related to the proposed endogenous ligand and that BDZ might be antagonistic rather than agonistic of the naturally occurring ligand.