(R,S)-BHFF

(R,S)-BHFF is a positive allosteric modulator of GABA_B receptors that increases the potency of GABA by 15.3-fold in a GTPγ[³⁵S] binding assay when used at a concentration of 0.3 μM.¹ It is selective for GABA_B over a panel of receptors and ion channels at 10 μM, however, it inhibits the cholecystokinin-1 (CCK_A) receptor (IC₅₀ = 4.1 μM). (R,S)-BHFF enhances inhibition of the population spike of CA1 pyramidal cells induced by the GABA_B receptor antagonist baclofen (Item No. 18600) in rat hippocampal slices. In vivo, (R,S)-BHFF increases the baclofen-induced loss of righting reflex and reverses stress-induced hyperthermia in mice. (R,S)-BHFF (50, 100, and 200 mg/kg) reduces the number of lever responses to alcohol by 30, 65, and 90%, respectively, and increases latency to the first response on the alcohol lever in Sardinian alcohol preferring (sP) rats when administered pre-conditioning at a dose of 200 mg/kg.²

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1. Malherbe, P., Masciardi, R., Norcross, R.D., 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. Pharmacol. 154(4), 797-811 (2008).

2. Maccioni, P., Thomas, A.W., Carai, M.A., et al. The positive allosteric modulator of the GABAB receptor, rac-BHFF, suppresses alcohol self-administration. Drug Alcohol Depend. 109(1-3), 96-103 (2010).