β-Carbolines as benzodiazepine receptor ligands. II: Synthesis and benzodiazepine receptor affinity of β-carboline-3-carboxylic acid amides

Article abstract of DOI:10.1002/jps.2600740620

Numerous β-carboline-3-carboxamides were synthesized by amidation of β-carboline-3-carboxylic acid, with various amino acids and amino acid esters serving as amine components, and tested in respect to their affinity for the benzodiazepine in mouse brain membranes. The title compounds have affinities in the low micromolar range. The results are discussed with respect to their relevance for a possible β-carboline structure containing the endogenous ligand of the benzodiazepine receptor.