CGP7930

• CAT Number: I006065
• CAS Number: 57717-80-3
• Molecular Formula: C19H32O2
• Molecular Weight: 292.46
• Purity: ≥95%
• Target: GABA Receptor
• Solubility: Soluble in DMSO, not in water
• Storage: Store at RT
• IUPAC Name: 2,6-ditert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol
• InChI: InChI=1S/C19H32O2/c1-17(2,3)14-9-13(11-19(7,8)12-20)10-15(16(14)21)18(4,5)6/h9-10,20-21H,11-12H2,1-8H3
• InChIKey: XLWJPQQFJNGUPA-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)CC(C)(C)CO

CGP-7930 (Cat.No:I006065) is a positive allosteric modulator at the GABAB receptor. It has anxiolytic effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and GHB, as well as reducing self-administration of ethanol and cocaine.

Reference

1:The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cells lacking functional GABAB receptors. Olianas MC, Dedoni S, Onali P.Eur J Pharmacol. 2017 Jan 5;794:135-146. doi: 10.1016/j.ejphar.2016.11.030. Epub 2016 Nov 19. PMID: 27876620 2:Elucidation of a CGP7930 in vitro metabolite by liquid chromatography/electrospray ionization quadrupole time-of-flight tandem mass spectrometry. Wang H, Zhang W, Wang X.Rapid Commun Mass Spectrom. 2016 Feb 28;30(4):491-6. doi: 10.1002/rcm.7465. PMID: 26777679 3:Effects of co-administration of the GABAB receptor agonist baclofen and a positive allosteric modulator of the GABAB receptor, CGP7930, on the development and expression of amphetamine-induced locomotor sensitization in rats. Cedillo LN, Miranda F.Pharmacol Rep. 2013;65(5):1132-43. PMID: 24399709 Free Article4:Anticonvulsant and behavioral effects of GABA(B) receptor positive modulator CGP7930 in immature rats. Mareš P, Tichá K, Mikulecká A.Epilepsy Behav. 2013 Jul;28(1):113-20. doi: 10.1016/j.yebeh.2013.04.011. Epub 2013 May 22. PMID: 23708148 5:Effects of intraperitoneal administration of the GABAB receptor positive allosteric modulator 2,6-di tert-butyl-4-(2-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) on food intake in non-deprived rats. Ebenezer IS.Eur J Pharmacol. 2012 Sep 5;690(1-3):115-8. doi: 10.1016/j.ejphar.2012.05.021. Epub 2012 May 28. PMID: 22652431 6:Anticonvulsant action of GABAB receptor positive modulator CGP7930 in immature rats. Mareš P.Epilepsy Res. 2012 Jun;100(1-2):49-54. doi: 10.1016/j.eplepsyres.2012.01.007. Epub 2012 Feb 15. PMID: 22341143 7:Effects of the GABAB receptor-positive modulators CGP7930 and rac-BHFF in baclofen- and γ-hydroxybutyrate-discriminating pigeons. Koek W, France CP, Cheng K, Rice KC.J Pharmacol Exp Ther. 2012 May;341(2):369-76. doi: 10.1124/jpet.111.190975. Epub 2012 Feb 7. PMID: 22319197 Free PMC Article8:The GABA(B) receptor agonist, baclofen, and the positive allosteric modulator, CGP7930, inhibit visceral pain-related responses to colorectal distension in rats. Brusberg M, Ravnefjord A, Martinsson R, Larsson H, Martinez V, Lindström E.Neuropharmacology. 2009 Feb;56(2):362-7. doi: 10.1016/j.neuropharm.2008.09.006. Epub 2008 Sep 25. PMID: 18824012 9:The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors. Parker DA, Marino V, Ong J, Puspawati NM, Prager RH.Clin Exp Pharmacol Physiol. 2008 Sep;35(9):1113-5. doi: 10.1111/j.1440-1681.2008.04948.x. Epub 2008 Apr 21. PMID: 18430050 10:Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents. Jacobson LH, Cryan JF.Neuropharmacology. 2008 Apr;54(5):854-62. doi: 10.1016/j.neuropharm.2008.01.004. Epub 2008 Jan 13. PMID: 18328507