- Stórustovu, S.I. and Ebert, B. (2006) J. Pharmacol. Exp. Ther. 316, 1351.
- Alomone Labs Isoguvacine hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.Time course of GABA(A) α1/β2 currents activation by 0.1 µM and 1 µM Isoguvacine hydrochloride (#I-185) at a holding potential of -60 mV.
Isoguvacine hydrochloride is a specific and potent agonist of GABA(A) receptors with an EC50 value of 3.7–17.3 µM, depending on the subunit composition1. It is a semirigid analogue of trans-4-aminocrotonic acid with limited conformational flexibility and is less potent than GABA1,2.
GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter, through the central nervous system, and play an important role in inhibiting cell excitation in the central nervous system. GABA(A) receptors are considered to be a major target of antiseizure drugs3,4.
Isoguvacine hydrochloride (#I-185) is a highly pure, synthetic, and biologically active compound.