Formulation: A crystalline solid
Formal Name: 5,7-bis(1,1-dimethylethyl)-3-hydroxy-3-(trifluoromethyl)-2(3H)-benzofuranone
Purity: ≥95%
Formula Markup: C17H21F3O3
Formula Weight: 330,3
Shelf life (days): 1460
CAS Number: 123557-91-5
Notes: (R,S)-BHFF is a positive allosteric modulator of GABAB 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.{42368} 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 (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.{42369}
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