Drug intelligence / Profile preview

baclofen + chlorzoxazone

Development stage
Phase 1
Modality
Small Molecules
Administration
Oral
01

Overview

Baclofen + chlorzoxazone is a combination of two centrally acting muscle relaxants. Baclofen is a gamma-aminobutyric acid (GABA) derivative that acts as an agonist at GABA-B receptors in the central nervous system, reducing excitatory neurotransmitter release and decreasing muscle spasticity. Chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain to inhibit multisynaptic reflex arcs involved in producing skeletal muscle spasms. This combination has been proposed for use in treating cerebellar symptoms, particularly in spinocerebellar ataxia (SCA), where it improves Purkinje neuron firing regularity and motor performance by compensating for reduced potassium channel function. Both drugs are individually approved as muscle relaxants; their combination is under investigation for neurological disorders such as SCA[1][2][3].

Other names
chlorzoxazone-baclofenbaclofen-chlorzoxazone
02

Targets

KCNMA1 (Calcium-activated potassium channel subfamily M alpha member 1)GABA-B (Gamma-aminobutyric acid receptor type B)CACNA1G (T-type Calcium Channel Protein Subunit Alpha-1G)

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