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CGP-7930

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Chemical compound Pharmaceutical compound
CGP-7930
Identifiers
IUPAC name
  • 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H32O2
Molar mass292.463 g·mol
3D model (JSmol)
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 was the first positive allosteric modulator of GABAB receptors described in literature. CGP7930 is also a GABAA receptor positive allosteric modulator and a blocker of Potassium channels.

CGP7930 was developed in Novartis and has been used extensively for scientific research. 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 alcoholic drinks and cocaine.

References

  1. Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, et al. (November 2001). "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. 60 (5): 963–71. PMID 11641424.
  2. Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L (July 2004). "The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor". The Journal of Biological Chemistry. 279 (28): 29085–91. doi:10.1074/jbc.M400930200. PMC 2557059. PMID 15126507.
  3. Chen Y, Menendez-Roche N, Sher E (June 2006). "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". The Journal of Pharmacology and Experimental Therapeutics. 317 (3): 1170–7. doi:10.1124/jpet.105.099176. PMID 16507713.
  4. Adams CL, Lawrence AJ. "CGP7930: a positive allosteric modulator of the GABAB receptor". CNS Drug Reviews. 13 (3): 308–16. doi:10.1111/j.1527-3458.2007.00021.x. PMC 6494120. PMID 17894647.
  5. Hannan SB, Penzinger R, Mikute G, Smart TG (July 2023). "CGP7930 - An allosteric modulator of GABABRs, GABAARs and inwardly-rectifying potassium channels" (PDF). Neuropharmacology. 109644. doi:10.1016/j.neuropharm.2023.109644. PMID 37422181.
  6. Frankowska M, Filip M, Przegaliński E. "Effects of GABAB receptor ligands in animal tests of depression and anxiety". Pharmacological Reports. 59 (6): 645–55. PMID 18195453.
  7. Jacobson LH, Cryan JF (April 2008). "Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents". Neuropharmacology. 54 (5): 854–62. doi:10.1016/j.neuropharm.2008.01.004. PMID 18328507.
  8. Carai MA, Colombo G, Froestl W, Gessa GL (November 2004). "In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor". European Journal of Pharmacology. 504 (3): 213–6. doi:10.1016/j.ejphar.2004.10.008. PMID 15541424.
  9. Parker DA, Marino V, Ong J, Puspawati NM, Prager RH (September 2008). "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 & Physiology. 35 (9): 1113–5. doi:10.1111/j.1440-1681.2008.04948.x. PMID 18430050.
  10. Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, et al. (April 2006). "The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats". Neuropharmacology. 50 (5): 632–9. doi:10.1016/j.neuropharm.2005.11.011. PMID 16406445.
  11. Filip M, Frankowska M, Przegaliński E (November 2007). "Effects of GABA(B) receptor antagonist, agonists and allosteric positive modulator on the cocaine-induced self-administration and drug discrimination". European Journal of Pharmacology. 574 (2–3): 148–57. doi:10.1016/j.ejphar.2007.07.048. PMID 17698060.
GABA receptor modulators
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAA-ρTooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators
Categories:
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