| Identification | Back Directory | [Name]
3,5-BIS(1,1-DIMETHYLETHYL)-4-HYDROXY-B,B-DIMETHYL-BENZENEPROPANOL | [CAS]
57717-80-3 | [Synonyms]
CGP 7930
3-(3',5'-DI-TERT-BUTYL-4'-HYDROXY)PHENYL-2,2-DIMETHYLPROPANOL
3,5-BIS(1,1-DIMETHYLETHYL)-4-HYDROXY-B,B-DIMETHYL-BENZENEPROPANOL
3,5-bis(1,1-Dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol
Benzenepropanol, 3,5-bis(1,1-dimethylethyl)-4-hydroxy-β,β-dimethyl-
3,5-Bis(1,1-dimethylethyl)-4-hydroxy-beta,beta-dimethylbenzenepropanol | [Molecular Formula]
C19H32O2 | [MDL Number]
MFCD04040028 | [MOL File]
57717-80-3.mol | [Molecular Weight]
292.46 |
| Hazard Information | Back Directory | [Description]
CGP 7930 is a positive allosteric modulator of GABAB receptors.1 It enhances GABA binding with a maximal effect of 143% compared to a GABA-only control in CHO cells membranes expressing the GABAB(1b/2) receptor and enhances GABA binding to rat cortical membranes when used at a concentration of 30 μM. It is selective for GABA binding to heterodimeric GABAB(1b/2) over monomeric GABAB(1b) receptors. CGP 7930 potentiates the efficacy of the GABAB receptor agonist baclofen (Item No. 27326) in decreasing the spontaneous firing rate of dopaminergic neurons in the rat ventral tegmental area (VTA) in vitro (EC50 = 0.27 μM).2 It also potentiates the sedative-reducing effects induced by the GABAB receptor agonists baclofen and γ-hydroxybutyric acid (GHB) in rats when administered at doses ranging from 10 to 170 mg/kg, effects that can be blocked by the GABAB receptor antagonist SCH 50911.3 CGP 7930 reduces self-administration of nicotine, alcohol, and cocaine in rodent models.4 It suppresses the acquisition of alcohol drinking behavior in alcohol-naïve Sardinian alcohol-preferring rats over a five-day period when administered at doses ranging from 25 to 100 mg/kg and transiently reduces the maintenance of alcohol drinking behavior in alcohol-experienced rats at a dose of 100 mg/kg.5 | [Definition]
ChEBI: 2,6-ditert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol is an alkylbenzene. | [Biological Activity]
Positive allosteric modulator of GABA B receptors. Increases the potency and efficacy of GABA at both native and recombinant GABA B receptors (EC 50 values are 5.37 and 4.60 μ M respectively) and enhances the inhibitory effect of the agonist L-baclofen in cultured cortical neurons. Reduces operant self-administration of ethanol in alcohol-preferring rats following i.p. administration. | [storage]
Desiccate at RT | [References]
[1] S. URWYLER. 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.[J]. Molecular Pharmacology, 2001, 60 5 1: 963-971. DOI: 10.1124/mol.60.5.963
[2] YING CHEN. GABAB receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area[J]. British Journal of Pharmacology, 2009, 144 7: 926-932. DOI: 10.1038/sj.bjp.0706100
[3] MAURO A.M. CARAI . In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor[J]. European journal of pharmacology, 2004, 504 3: Pages 213-216. DOI: 10.1016/j.ejphar.2004.10.008
[4] C. L. ADAMS A. J L. CGP7930: A Positive Allosteric Modulator of the GABAB Receptor[J]. CNS drug reviews, 2007, 13 3: 308-316. DOI: 10.1111/j.1527-3458.2007.00021.x
[5] ALESSANDRO ORRù . Reducing effect of the positive allosteric modulators of the GABAB receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats[J]. European journal of pharmacology, 2005, 525 1: Pages 105-111. DOI: 10.1016/j.ejphar.2005.10.005 |
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