Chemistry:CGP-7930

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Short description: Chemical compound
CGP-7930
CGP-7930 chemical structure.svg
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC19H32O2
Molar mass292.463 g·mol−1
3D model (JSmol)
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CGP-7930 was the first positive allosteric modulator of GABAB receptors described in literature.[1][2][3][4] CGP7930 is also a GABAA receptor positive allosteric modulator and a blocker of Potassium channels.[5]

CGP7930 was developed in Novartis and has been used extensively for scientific research. It has anxiolytic effects in animal studies,[6][7] and has a synergistic effect with GABAB agonists such as baclofen and GHB,[8][9] as well as reducing self-administration of alcoholic drinks and cocaine.[10][11]

References

  1. ↑ "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. November 2001. PMID 11641424. 
  2. ↑ "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. July 2004. doi:10.1074/jbc.M400930200. PMID 15126507. 
  3. ↑ "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. June 2006. doi:10.1124/jpet.105.099176. PMID 16507713. 
  4. ↑ "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. PMID 17894647. 
  5. ↑ "CGP7930 - An allosteric modulator of GABABRs, GABAARs and inwardly-rectifying potassium channels". Neuropharmacology 109644. July 2023. doi:10.1016/j.neuropharm.2023.109644. PMID 37422181. 
  6. ↑ "Effects of GABAB receptor ligands in animal tests of depression and anxiety". Pharmacological Reports 59 (6): 645–55. PMID 18195453. 
  7. ↑ "Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents". Neuropharmacology 54 (5): 854–62. April 2008. doi:10.1016/j.neuropharm.2008.01.004. PMID 18328507. 
  8. ↑ "In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor". European Journal of Pharmacology 504 (3): 213–6. November 2004. doi:10.1016/j.ejphar.2004.10.008. PMID 15541424. 
  9. ↑ "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. September 2008. doi:10.1111/j.1440-1681.2008.04948.x. PMID 18430050. 
  10. ↑ "The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats". Neuropharmacology 50 (5): 632–9. April 2006. doi:10.1016/j.neuropharm.2005.11.011. PMID 16406445. 
  11. ↑ "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. November 2007. doi:10.1016/j.ejphar.2007.07.048. PMID 17698060. 

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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

}}



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