Overview
- Thompson, S.A. et al. (2002) Mol. Pharmacol. 61, 861.
Alomone Labs Tracazolate hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.Time course of GABA(A) α1/β2 currents, reversibly activated in a concentration dependent manner by 10 µM, 35 µM and 100 µM Tracazolate hydrochloride (#T-230) while membrane potential was held at -60 mV.
Tracazolate hydrochloride, a pyrazolopyridine, is a non-sedative anxiolytic compound that acts as an allosteric modulator of GABA(A) receptors. Tracazolate was shown to potentiate the GABA(A) receptor with an EC50 value of 1.1 µM and inhibit with an IC50 value of 1.2 µM1.
In addition to its anxiolytic activity, tracazolate possesses anticonvulsant activity that was shown in behavioral studies. Tracazolate seems to cause less adverse interactions in combination with barbiturates and alcohol and demonstrates a wider separation between sedative and therapeutic doses than the benzodiazepines1,2.
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. They also play an important role in inhibiting cell excitation in the central nervous system, and are considered to be a major target of antiseizure drugs3,4.
