Potent, selective GABAB positive allosteric modulator. Enhances GABAB agonist-stimulated responses in the FLIPR assay and [35S]GTPγS binding. Enhances inhibitory effect of baclofen on population spike (PS) in hippocampal slices. Orally active in vivo, displaying anxiolytic-like properties.
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM and in ethanol to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Maccioni P et al. The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration. Drug Alcohol Depend109:96-103 (2010).
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Malherbe P et al. 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 Pharmacol154:797-811 (2008).
Read more (PubMed: 18536733) »