CGP-7930
{{short description|Chemical compound}}
{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 449578940
| IUPAC_name = 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol
| image = CGP-7930_chemical_structure.svg
| tradename =
| pregnancy_AU =
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| CAS_number = 57717-80-3
| ATC_prefix =
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| PubChem = 5024764
| IUPHAR_ligand = 1079
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 4203613
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = XLWJPQQFJNGUPA-UHFFFAOYSA-N
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = ZAM4WWA5Y4
| chemical_formula =
| C=19 | H=32 | O=2
| smiles = CC(C)(C)c1cc(CC(C)(C)CO)cc(C(C)(C)C)c1O
}}
CGP-7930 was the first positive allosteric modulator of GABAB receptors described in literature.{{cite journal | vauthors = Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, Bettler B, Kaupmann K | display-authors = 6 | title = 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 | journal = Molecular Pharmacology | volume = 60 | issue = 5 | pages = 963–71 | date = November 2001 | pmid = 11641424 }}{{cite journal | vauthors = Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L | title = The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor | journal = The Journal of Biological Chemistry | volume = 279 | issue = 28 | pages = 29085–91 | date = July 2004 | pmid = 15126507 | doi = 10.1074/jbc.M400930200 | doi-access = free | pmc = 2557059 }}{{cite journal | vauthors = Chen Y, Menendez-Roche N, Sher E | title = 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 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 317 | issue = 3 | pages = 1170–7 | date = June 2006 | pmid = 16507713 | doi = 10.1124/jpet.105.099176 }}{{cite journal | vauthors = Adams CL, Lawrence AJ | title = CGP7930: a positive allosteric modulator of the GABAB receptor | journal = CNS Drug Reviews | volume = 13 | issue = 3 | pages = 308–16 | pmid = 17894647 | doi = 10.1111/j.1527-3458.2007.00021.x | pmc = 6494120 }} CGP7930 is also a GABAA receptor positive allosteric modulator and a blocker of Potassium channels.{{cite journal | vauthors = Hannan SB, Penzinger R, Mikute G, Smart TG| title = CGP7930 - An allosteric modulator of GABABRs, GABAARs and inwardly-rectifying potassium channels | journal = Neuropharmacology | volume = 109644 | date = July 2023 | pmid = 37422181 | doi = 10.1016/j.neuropharm.2023.109644| doi-access = free | url = https://discovery.ucl.ac.uk/10173266/1/1-s2.0-S0028390823002344-main.pdf }}
CGP7930 was developed in Novartis and has been used extensively for scientific research. It has anxiolytic effects in animal studies,{{cite journal | vauthors = Frankowska M, Filip M, Przegaliński E | title = Effects of GABAB receptor ligands in animal tests of depression and anxiety | journal = Pharmacological Reports | volume = 59 | issue = 6 | pages = 645–55 | pmid = 18195453 }}{{cite journal | vauthors = Jacobson LH, Cryan JF | title = Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents | journal = Neuropharmacology | volume = 54 | issue = 5 | pages = 854–62 | date = April 2008 | pmid = 18328507 | doi = 10.1016/j.neuropharm.2008.01.004 }} and has a synergistic effect with GABAB agonists such as baclofen and GHB,{{cite journal | vauthors = Carai MA, Colombo G, Froestl W, Gessa GL | title = In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor | journal = European Journal of Pharmacology | volume = 504 | issue = 3 | pages = 213–6 | date = November 2004 | pmid = 15541424 | doi = 10.1016/j.ejphar.2004.10.008 }}{{cite journal | vauthors = Parker DA, Marino V, Ong J, Puspawati NM, Prager RH | title = The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors | journal = Clinical and Experimental Pharmacology & Physiology | volume = 35 | issue = 9 | pages = 1113–5 | date = September 2008 | pmid = 18430050 | doi = 10.1111/j.1440-1681.2008.04948.x }} as well as reducing self-administration of alcoholic drinks and cocaine.{{cite journal | vauthors = Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, Beart PM, Lawrence AJ | display-authors = 6 | title = The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats | journal = Neuropharmacology | volume = 50 | issue = 5 | pages = 632–9 | date = April 2006 | pmid = 16406445 | doi = 10.1016/j.neuropharm.2005.11.011 }}{{cite journal | vauthors = Filip M, Frankowska M, Przegaliński E | title = Effects of GABA(B) receptor antagonist, agonists and allosteric positive modulator on the cocaine-induced self-administration and drug discrimination | journal = European Journal of Pharmacology | volume = 574 | issue = 2-3 | pages = 148–57 | date = November 2007 | pmid = 17698060 | doi = 10.1016/j.ejphar.2007.07.048 }}