Overview
- Hoestgaard-Jensen, K. et al. (2010) Neuropharmacology 58, 702.
Alomone Labs AA 29504 activates GABA(A) receptors expressed in Xenopus oocytes.Time course of GABA(A) α1/β2 currents, reversibly activated in a concentration dependent manner by 1 µM, 5 µM and 25 µM AA 29504 (#A-370), while membrane potential was held at -60mV.
AA 29504, a close analogue of retigabine (KCNQ channel opener), acts as a positive allosteric modulator of GABA(A) receptors. A study in adult rats shows that systemic administration of AA 29504 produces anxiolytic effects and reduces motor coordination1.
AA 29504 decreases the EC50 value of GABA at the GABA (A) receptors in Xenopus oocytes at over 1 µM. The compound also exhibits agonistic activity on KCNQ channels and demonstrates EC50 values of 9.6-13.5 µM1.
GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. These receptors mediate GABA action, a major inhibitory neurotransmitter, throughout the central nervous system (CNS). They play an important role in inhibiting cell excitation in the CNS. The GABA(A) receptor is considered to be a major target of antiseizure drugs2,3.
