CGP-7930 explained

CGP-7930 was the first positive allosteric modulator of GABA_B receptors described in literature.^{[1] [2] [3] [4]} CGP7930 is also a GABA_A 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 GABA_B agonists such as baclofen and GHB,^{[8] [9]} as well as reducing self-administration of alcoholic drinks and cocaine.^{[10] [11]}

Notes and References

1. Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, Bettler B, Kaupmann K . 6 . 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 . 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 . The Journal of Biological Chemistry . 279 . 28 . 29085–91 . July 2004 . 15126507 . 10.1074/jbc.M400930200 . free . 2557059 .
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 . The Journal of Pharmacology and Experimental Therapeutics . 317 . 3 . 1170–7 . June 2006 . 16507713 . 10.1124/jpet.105.099176 .
4. Adams CL, Lawrence AJ . CGP7930: a positive allosteric modulator of the GABAB receptor . CNS Drug Reviews . 13 . 3 . 308–16 . 17894647 . 10.1111/j.1527-3458.2007.00021.x . 6494120 .
5. Hannan SB, Penzinger R, Mikute G, Smart TG. CGP7930 - An allosteric modulator of GABABRs, GABAARs and inwardly-rectifying potassium channels . Neuropharmacology . 109644 . July 2023 . 37422181 . 10.1016/j.neuropharm.2023.109644. free .
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 . 18195453 .
7. Jacobson LH, Cryan JF . Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents . Neuropharmacology . 54 . 5 . 854–62 . April 2008 . 18328507 . 10.1016/j.neuropharm.2008.01.004 .
8. 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 . 504 . 3 . 213–6 . November 2004 . 15541424 . 10.1016/j.ejphar.2004.10.008 .
9. 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 & Physiology . 35 . 9 . 1113–5 . September 2008 . 18430050 . 10.1111/j.1440-1681.2008.04948.x .
10. Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, Beart PM, Lawrence AJ . 6 . 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 . 16406445 . 10.1016/j.neuropharm.2005.11.011 .
11. 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 . 574 . 2-3 . 148–57 . November 2007 . 17698060 . 10.1016/j.ejphar.2007.07.048 .