Drug intelligence / Profile preview

ZK-93423

Development stage
Discontinued
Lead developer
Bayer
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
01

Overview

ZK-93423 is an experimental small molecule drug from the β-carboline family with muscle relaxant and anxiolytic properties. It acts as a nonbenzodiazepine full agonist at the benzodiazepine binding site of the GABAA receptor and is not subtype-selective—stimulating α1-, α2-, α3-, and α5-subunit containing GABAA receptors equally. Its pharmacological effects include anticonvulsant activity, muscle relaxation, appetite stimulation, and anxiolysis comparable to benzodiazepines. ZK-93423 has been used in research to develop new beta-carboline derivatives and to map the GABAA receptor binding site. It was initially developed by Bayer AG but has not advanced beyond early clinical development and is currently discontinued for anxiety disorders[1][2][8].

Other names
9H-Pyrido[3,4-b]indole-3-carboxylic acid, 4-(methoxymethyl)-6-(phenylmethoxy)-, ethyl esterethyl 6-(benzyloxy)-4-(methoxymethyl)-9H-pyrido[3,4-b]indole-3-carboxylate
02

Targets

GABRR (GABA-A receptor subunit rho)

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