Molecular structure of rac BHFF, CAS Number: 123557-91-5
rac BHFF (CAS 123557-91-5)
Application:
rac BHFF is a GABAB receptor positive allosteric modulator
CAS Number:
123557-91-5
Molecular Weight:
330.34
Molecular Formula:
C17H21F3O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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Description
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SDS & Certificate of Analysis
Potent and selective GABAB receptor positive allosteric modulator that increases the efficacy and potency of GABA ( > 149% and > 15-fold respectively). Orally active and exhibits anxiolytic activity in vivo.
rac BHFF (CAS 123557-91-5) References
- 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. | Malherbe, P., et al. 2008. Br J Pharmacol. 154: 797-811. PMID: 18536733
- The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration. | Maccioni, P., et al. 2010. Drug Alcohol Depend. 109: 96-103. PMID: 20089372
- GABAB receptor-positive modulators: brain region-dependent effects. | Hensler, JG., et al. 2012. J Pharmacol Exp Ther. 340: 19-26. PMID: 21954301
- Effects of the GABAB receptor-positive modulators CGP7930 and rac-BHFF in baclofen- and γ-hydroxybutyrate-discriminating pigeons. | Koek, W., et al. 2012. J Pharmacol Exp Ther. 341: 369-76. PMID: 22319197
- A fluorescent sensor for GABA and synthetic GABA(B) receptor ligands. | Masharina, A., et al. 2012. J Am Chem Soc. 134: 19026-34. PMID: 23095089
- Reduction of alcohol intake by the positive allosteric modulator of the GABA(B) receptor, rac-BHFF, in alcohol-preferring rats. | Loi, B., et al. 2013. Alcohol. 47: 69-73. PMID: 23218664
- Discriminative stimulus effects of the GABAB receptor-positive modulator rac-BHFF: comparison with GABAB receptor agonists and drugs of abuse. | Koek, W., et al. 2013. J Pharmacol Exp Ther. 344: 553-60. PMID: 23275067
- Positive allosteric modulation of GABAB receptors ameliorates sensorimotor gating in rodent models. | Frau, R., et al. 2014. CNS Neurosci Ther. 20: 679-84. PMID: 24703381
- Inhibition of alcohol self-administration by positive allosteric modulators of the GABAB receptor in rats: lack of tolerance and potentiation of baclofen. | Maccioni, P., et al. 2015. Psychopharmacology (Berl). 232: 1831-41. PMID: 25420609
- New effects of GABAB receptor allosteric modulator rac-BHFF on ambient GABA, uptake/release, Em and synaptic vesicle acidification in nerve terminals. | Pozdnyakova, N., et al. 2015. Neuroscience. 304: 60-70. PMID: 26197223
- The positive allosteric GABAB receptor modulator rac-BHFF enhances baclofen-mediated analgesia in neuropathic mice. | Zemoura, K., et al. 2016. Neuropharmacology. 108: 172-8. PMID: 27108932
- GABABR-Induced EGFR Transactivation Promotes Migration of Human Prostate Cancer Cells. | Xia, S., et al. 2017. Mol Pharmacol. 92: 265-277. PMID: 28424220
- GABAB receptor positive allosteric modulators with different efficacies affect neuroadaptation to and self-administration of alcohol and cocaine. | de Miguel, E., et al. 2019. Addict Biol. 24: 1191-1203. PMID: 30421860
- Structure optimization of positive allosteric modulators of GABAB receptors led to the unexpected discovery of antagonists/potential negative allosteric modulators. | Mugnaini, C., et al. 2020. Bioorg Med Chem Lett. 30: 127443. PMID: 32730942
- 6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators. | Huszár, J., et al. 2022. Bioorg Med Chem Lett. 67: 128714. PMID: 35367591
Activator of:
GABA Receptor.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
rac BHFF, 5 mg | sc-204228 | 5 mg | $112.00 | |||
rac BHFF, 25 mg | sc-204228A | 25 mg | $428.00 |