Baclofen

Baclofen is a GABA derivative that acts as an agonist at GABA-B receptors; it is commonly used in animal models to examine the effects of GABAergic neurotransmission in a variety of fields, including substance dependence, spasticity, pain, and feeding behavior. Baclofen exhibits analgesic, antinociceptive, and antiepileptic/anticonvulsant activities. The analgesic effect of baclofen is mediated by its GABA-B receptor activation, inducing a presynaptic block of action potentials induced by mechanical or thermal stimuli that decreases frequency and amplitude of excitatory post-synaptic currents. Baclofen is used clinically to promote abstinence in alcohol dependent subjects, potentially mediating alcohol craving during withdrawal. This compound is also delivered intrathecally to treat spasticity and dystonia.