Drug intelligence / Profile preview

S(-)-baclofen

Development stage
Preclinical
Lead developer
Osmotica Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

S(-)-baclofen is the levorotatory enantiomer of the GABA-B receptor agonist baclofen. While the R(+)-enantiomer (arbaclofen) is the primary active isomer responsible for the therapeutic muscle-relaxant effects of racemic baclofen, S(-)-baclofen is significantly less potent at the GABA-B receptor. Research has identified that S(-)-baclofen may possess distinct pharmacological properties, particularly in the context of sex-dependent responses to alcohol. In preclinical studies, S(-)-baclofen has been shown to increase dopamine release in the nucleus accumbens and, in some female subjects, paradoxically increase alcohol self-administration. It is primarily used as a research tool to investigate the stereospecificity of baclofen's effects and the underlying neurobiology of alcohol use disorder.

Other names
(S)-baclofenS-baclofen(-)-baclofen
02

Targets

GABA-B (Gamma-aminobutyric acid receptor type B)

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