Tracazolate

Tracazolate is a positive allosteric modulator of the GABAA receptor (GABAAR). It potentiates GABA-stimulated currents in X. laevis oocytes expressing alpha1beta3gamma2s and alpha1beta1delta subunit-containing GABAARs (EC50s = 1.5 and 16.7 µM, respectively) and increases the maximal response to GABA in X. laevis oocytes expressing alpha1beta1delta subunit-containing GABAARs, but reduces the maximal response to GABA in X. laevis oocytes expressing alpha1beta3gamma2s subunit-containing GABAARs. Tracazolate selectively potentiates GABA-induced currents in X. laevis oocytes expressing beta3 over beta1 subunit-containing GABAARs (EC50s = 1.5 and 13.2 µM for alpha1beta3gamma2s and alpha1beta1gamma2s subunit-containing GABAARs, respectively). Tracazolate (5 mg/kg) increases time spent in social interactions but does not reduce locomotor activity, indicating anxiolytic but not sedating activity, in rats.. SMILES: O=C(C1=C(C)N=C2C(C=NN2CC)=C1NCCCC)OCC. InChi Code: InChI=1S/C16H24N4O2/c1-5-8-9-17-14-12-10-18-20(6-2)15(12)19-11(4)13(14)16(21)22-7-3/h10H,5-9H2,1-4H3,(H,17,19). InChi Key: PCTRYMLLRKWXGF-UHFFFAOYSA-N