Biological Activity |
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 uM (human GAT-1), 39 uM (rat GAT-1), 58 uM (rat GAT-2), 119 uM (human GAT-3), 378 uM (rat GAT-3), and 1870 uM (human BGT-3). IC50 & Target: IC50: 14 uM (human GAT-1), 39 uM (rat GAT-1), 58 uM (rat GAT-2), 119 uM (human GAT-3), 378 uM (rat GAT-3), 1870 uM (human BGT-3)[1] In Vitro: Guvacine hydrochloride is a potent inhibitor of GABA transporter, dispalys modest selectivity for cloned GABA transporters with IC50s of 14 uM (human GAT-1), 39 uM (rat GAT-1), 58 uM (rat GAT-2), 119 uM (human GAT-3), 378 uM (rat GAT-3), and 1870 uM (human BGT-3). Guvacine has low affinity at hBGT-1 (IC50 >1 mM)[1]. Guvacine hydrochloride is a potent inhibitor of GABA uptake, but does not inhibit sodium-independent GABA binding, and is weak or inactive as a GABA receptor agonist[2]. Guvacine inhibits the uptake GABA and beta-alanine with IC50s of 23 +/- 2 uM, 66 +/- 11 uM in the Cat spinal cord, and 8 +/- 1 uM, 123 +/- 28 uM in the rat cerebral cortex, respectively[3]. |