phaclofen

Phaclofen is a selective, competitive antagonist of the gamma-aminobutyric acid type B (GABAB) receptor. It is a phosphonate analogue of the GABAB agonist baclofen. Phaclofen is primarily utilized as a pharmacological research tool to investigate the physiological roles of GABAB receptors in the central nervous system, including their involvement in synaptic plasticity, seizure activity, and pain modulation. In preclinical studies, it has been used to block the effects of baclofen and to demonstrate the contribution of GABAB-mediated inhibition in models of Alzheimer's disease, epilepsy, and neuropathic pain. Due to its relatively low potency and poor blood-brain barrier permeability, it is often administered directly into the central nervous system via intracerebroventricular or intrathecal routes in animal models.

Other names

3-amino-2-(4-chlorophenyl)propylphosphonic acidphosphonobaclofen