Biological Description

Potent, selective GABA_B positive allosteric modulator. Enhances GABA_B agonist-stimulated responses in the FLIPR assay and GTPγ35S binding. Enhances inhibitory effect of baclofen on population spike (PS) in hippocampal slices. Orally active in vivo, displaying anxiolytic-like properties.

Useful References

Maccioni et al (2010) The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration. Drug Alcohol Depend. 2010 Jan 18. [Epub ahead of print] abstract

Malherbe et al (2008) characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptors. Br J Pharmacol. 154:797-811. abstract



 

Chemical Information

5,7-Bis(1,1-dimethylethyl)-3-hydroxy-3(trifluoromethyl)-2(3H)-benzofuranone

• Desiccate at +4°C
• MW 330.35
• Soluble to 100 mM in DMSO and to 100 mM in ethanol
• C₁₇H₂₁F₃O₃