(R,S)-BHFF

(R,S)-BHFF is a positive allosteric modulator of GABAB receptors that increases the potency of GABA by 15.3-fold in a GTPgamma[35S] binding assay when used at a concentration of 0.3 µM. It is selective for GABAB over a panel of receptors and ion channels at 10 µM, however, it inhibits the cholecystokinin-1 (CCKA) receptor (IC50 = 4.1 µM). (R,S)-BHFF enhances inhibition of the population spike of CA1 pyramidal cells induced by the GABAB receptor antagonist baclofen (Cay-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.Formal Name: 5,7-bis(1,1-dimethylethyl)-3-hydroxy-3-(trifluoromethyl)-2(3H)-benzofuranone. CAS Number: 123557-91-5. Synonyms: rac-BHFF. Molecular Formula: C17H21F3O3. Formula Weight: 330.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 285 nm. SMILES: CC(C)(C)C1=C2C(C(O)(C(F)(F)F)C(O2)=O)=CC(C(C)(C)C)=C1. InChi Code: InChI=1S/C17H21F3O3/c1-14(2,3)9-7-10(15(4,5)6)12-11(8-9)16(22,13(21)23-12)17(18,19)20/h7-8,22H,1-6H3. InChi Key: RVNOANDLZIIFHB-UHFFFAOYSA-N.