The Sound of Evolution
Baclofen
Mechanism of action:
Baclofen is a centrally acting skeletal muscle relaxant and a selective agonist of the GABA_B receptor in the central nervous system. When baclofen activates GABA_B receptors, it promotes the efflux of potassium ions (K⁺) from neurons, causing membrane hyperpolarization and thereby suppressing motor neuron firing. It also inhibits the influx of calcium ions (Ca²⁺) into neurons, reducing the release of excitatory neurotransmitters such as glutamate and aspartate, and decreasing excitatory input to downstream neurons.
Reference(s):
1. Brennan JL et al. (2013). Clinical effectiveness of baclofen for the treatment of alcohol dependence: a review. Clin Pharmacol.
2. Liu J et al. (2017). Baclofen for alcohol withdrawal. Cochrane Database Syst Rev.
3. Chen K et al. (2005). Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull.