CGP-7930

CGP-7930

Systematic (IUPAC) name
2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol
Identifiers
PubChem	CID 5024764
IUPHAR/BPS	1079
ChemSpider	4203613
Chemical data
Formula	C19H32O2
Molar mass	292.455 g/mol
SMILES CC(C)(C)c1cc(CC(C)(C)CO)cc(C(C)(C)C)c1O
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 Key:XLWJPQQFJNGUPA-UHFFFAOYSA-N
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CGP-7930 is a compound used in scientific research which acts as a positive allosteric modulator at the GABA_B receptor.^[1][2][3][4] It has anxiolytic effects in animal studies,^[5][6] and has a synergistic effect with GABA_B agonists such as baclofen and GHB,^[7][8] as well as reducing self-administration of ethanol and cocaine.^[9][10]

References

1. Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, Bettler B, Kaupmann K. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Molecular Pharmacology. 2001 Nov;60(5):963-71. PMID 11641424
2. Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L. The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor. Journal of Biological Chemistry. 2004 Jul 9;279(28):29085-91. PMID 15126507
3. Chen Y, Menendez-Roche N, Sher E. Differential modulation by the GABAB receptor allosteric potentiator 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)-phenol (CGP7930) of synaptic transmission in the rat hippocampal CA1 area. Journal of Pharmacology and Experimental Therapeutics. 2006 Jun;317(3):1170-7. PMID 16507713
4. Adams CL, Lawrence AJ. CGP7930: a positive allosteric modulator of the GABAB receptor. CNS Drug Reviews. 2007 Fall;13(3):308-16. doi:10.1111/j.1527-3458.2007.00021.x PMID 17894647
5. Frankowska M, Filip M, Przegaliński E. Effects of GABAB receptor ligands in animal tests of depression and anxiety. Pharmacological Reports. 2007 Nov-Dec;59(6):645-55. PMID 18195453
6. Jacobson LH, Cryan JF. Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents. Neuropharmacology. 2008 Apr;54(5):854-62. PMID 18328507
7. Carai MA, Colombo G, Froestl W, Gessa GL. In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor. European Journal of Pharmacology. 2004 Nov 19;504(3):213-6. PMID 15541424
8. Parker DA, Marino V, Ong J, Puspawati NM, Prager RH. The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors. Clinical and Experimental Pharmacology and Physiology. 2008 Sep;35(9):1113-5. PMID 18430050
9. Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, Beart PM, Lawrence AJ. The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology. 2006 Apr;50(5):632-9. PMID 16406445
10. Filip M, Frankowska M, Przegaliński E. Effects of GABA(B) receptor antagonist, agonists and allosteric positive modulator on the cocaine-induced self-administration and drug discrimination. European Journal of Pharmacology. 2007 Nov 28;574(2-3):148-57. PMID 17698060