guvacine

Guvacine is a pyridine alkaloid found naturally in the Areca nut (Betel nut). It is an experimental small molecule drug with no approved medical indication. Guvacine acts as a selective inhibitor of GABA reuptake by binding to presynaptic GABA transporters (GATs), specifically inhibiting sodium- and chloride-dependent GABA transporter subtypes (GAT1/SLC6A1; GAT2/SLC6A13; GAT3/SLC6A11; BGT1/SLC6A12). This inhibition increases extracellular levels of gamma-Aminobutyric acid (GABA), the major inhibitory neurotransmitter in the mammalian brain. Notably, guvacine does not bind to or activate postsynaptic GABA receptors. Its main research interest lies in neuropharmacology and potential use for neuropsychiatric disorders[1][2][4][5][7].

Other names

guvacine1,2,5,6-tetrahydropyridine-3-carboxylic acid1,2,5,6-tetrahydro-3-pyridinecarboxylic acid1,2,5,6-tetrahydronicotinic acid