Guvacine hydrochloride

6027-91-4

163.60

DMSO : < 1 mg/mL (insoluble or slightly soluble); H2O : 41.67 mg/mL (254.71 mM; Need ultrasonic)

Neuronal Signaling; Membrane Transporter/Ion Channel

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].