Википедија

CGP-7930

CGP-7930 je jedinjenje koje se koristi u naučnim istraživanjima kao pozitivni alosterni modulator GABAB receptor.[1][2][3][4] On ima anksiolitičko dejstvo u životinjskim studijama,[5][6] kao i sinergističke efekte sa GABAB agonistima, poput baklofena i GHB.[7][8] On umanjuje samo-administraciju etanola i kokaina.[9][10]

CGP-7930
IUPAC ime
2,6-Di-tert-butil-4-(3-hidroksi-2,2-dimetil-propil)-fenol
Identifikatori
ATC kodnone
PubChemCID 5024764
IUPHAR/BPS1079
Hemijski podaci
FormulaC19H32O2
Molarna masa292,455 g/mol
  • CC(C)(C)c1cc(CC(C)(C)CO)cc(C(C)(C)C)c1O

Reference уреди

  1. ^ Urwyler, S.; Mosbacher, J.; Lingenhoehl, K.; Heid, J.; Hofstetter, K.; Froestl, W.; Bettler, B.; Kaupmann, K. (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—971. PMID 11641424. doi:10.1124/mol.60.5.963. 
  2. ^ Binet, V.; Brajon, C.; Le Corre, L.; Acher, F.; Pin, J. P.; Prézeau, L. (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—29091. PMC 2557059  . PMID 15126507. doi:10.1074/jbc.M400930200  . 
  3. ^ Chen, Y.; Menendez-Roche, N.; Sher, E. (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—1177. PMID 16507713. S2CID 17821271. doi:10.1124/jpet.105.099176. 
  4. ^ Adams, C. L.; Lawrence, A. J. (2007). „CGP7930: A Positive Allosteric Modulator of the GABABReceptor”. CNS Drug Reviews. 13 (3): 308—316. PMC 6494120  . PMID 17894647. doi:10.1111/j.1527-3458.2007.00021.x. 
  5. ^ Frankowska, M.; Filip, M.; Przegaliński, E. (2007). „Effects of GABAB receptor ligands in animal tests of depression and anxiety”. Pharmacological Reports : Pr. 59 (6): 645—655. PMID 18195453. 
  6. ^ Jacobson, L. H.; Cryan, J. F. (2008). „Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents”. Neuropharmacology. 54 (5): 854—862. PMID 18328507. S2CID 45852297. doi:10.1016/j.neuropharm.2008.01.004. 
  7. ^ Carai, M. A.; Colombo, G.; Froestl, W.; Gessa, G. L. (2004). „In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor”. European Journal of Pharmacology. 504 (3): 213—216. PMID 15541424. doi:10.1016/j.ejphar.2004.10.008. 
  8. ^ Parker, D. A.; Marino, V.; Ong, J.; Puspawati, N. M.; Prager, R. H. (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—1115. PMID 18430050. S2CID 25608408. doi:10.1111/j.1440-1681.2008.04948.x. 
  9. ^ Liang, J. H.; Chen, F.; Krstew, E.; Cowen, M. S.; Carroll, F. Y.; Crawford, D.; Beart, P. M.; Lawrence, A. J. (2006). „The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats”. Neuropharmacology. 50 (5): 632—639. PMID 16406445. S2CID 54264313. doi:10.1016/j.neuropharm.2005.11.011. 
  10. ^ Filip, M.; Frankowska, M.; Przegaliński, E. (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—157. PMID 17698060. doi:10.1016/j.ejphar.2007.07.048. 

Spoljašnje veze уреди

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