A positive allosteric modulator of GABAB receptors; increases the potency of GABA by 15.3-fold in a GTPγ[35S] binding assay at 0.3 μM; selective for GABAB over a panel of receptors and ion channels at 10 μM; inhibits the CCKA receptor (IC50 = 4.1 μM); enhances baclofen-induced inhibition of the population spike of CA1 pyramidal cells in rat hippocampal slices; increases the baclofen-induced loss of righting reflex and reverses stress-induced hyperthermia in mice; reduces the number of lever responses to alcohol and increases latency to the first response on the alcohol lever in sP rats at 200 mg/kg

(R,S)-BHFF – 10 mg

Brand:
Cayman
CAS:
123557-91-5
Storage:
-20
UN-No:
Non-Hazardous - /

(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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Description

A positive allosteric modulator of GABAB receptors; increases the potency of GABA by 15.3-fold in a GTPγ[35S] binding assay at 0.3 μM; selective for GABAB over a panel of receptors and ion channels at 10 μM; inhibits the CCKA receptor (IC50 = 4.1 μM); enhances baclofen-induced inhibition of the population spike of CA1 pyramidal cells in rat hippocampal slices; increases the baclofen-induced loss of righting reflex and reverses stress-induced hyperthermia in mice; reduces the number of lever responses to alcohol and increases latency to the first response on the alcohol lever in sP rats at 200 mg/kg ,

Formal name: 5,7-bis(1,1-dimethylethyl)-3-hydroxy-3-(trifluoromethyl)-2(3H)-benzofuranone

Synonyms:  rac-BHFF

Molecular weight: 330.3

CAS: 123557-91-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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