A positive allosteric modulator of GABAB receptors
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CGP 7930

Item No. 29429

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3,5-bis(1,1-dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol
CAS Number
57717-80-3
Molecular Formula
C19H32O2
Formula Weight
292.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 100 mM
SMILES
CC(C)(C)C1=C(O)C(C(C)(C)C)=CC(CC(C)(C)CO)=C1
InChi Code
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
InChi Key
XLWJPQQFJNGUPA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $143

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    10 mg

    $190

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    Product 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Urwyler, S., Mosbacher, J., Lingenhoehl, K., et al. Positive allosteric modulation of native and recombinant γ-aminobutyric acidB receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol. Pharmacol. 60(5), 963-971 (2001).

    2. Chen, Y., Phillips, K., Minton, G., et al. GABAB receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area. Br. J. Pharmacol. 144(7), 926-932 (2005).

    3. Carai, M.A.M., Colombo, G., Froestl, W., et al. In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor. Eur. J. Pharmacol. 504(3), 213-216 (2004).

    4. Adams, C.L., and Lawrence, A.J. CGP7930: A positive allosteric modulator of the GABAB receptor. CNS Drug Rev. 13(3), 308-316 (2007).

    5. Orrù, A., Lai, P., Lobina, C., et al. Reducing effect of the positive allosteric modulators of the GABAB receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur. J. Pharmacol. 525(1-3), 105-111 (2005).