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CGP-7930
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CGP-7930 : ウィキペディア英語版
CGP-7930

CGP-7930 is a compound used in scientific research which acts as a positive allosteric modulator at the GABAB receptor.〔Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, Bettler B, Kaupmann K. 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''. 2001 Nov;60(5):963-71. PMID 11641424〕〔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. ''Journal of Biological Chemistry''. 2004 Jul 9;279(28):29085-91. PMID 15126507〕〔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. ''Journal of Pharmacology and Experimental Therapeutics''. 2006 Jun;317(3):1170-7. PMID 16507713〕〔Adams CL, Lawrence AJ. CGP7930: a positive allosteric modulator of the GABAB receptor. ''CNS Drug Reviews''. 2007 Fall;13(3):308-16. PMID 17894647〕 It has anxiolytic effects in animal studies,〔Frankowska M, Filip M, Przegaliński E. Effects of GABAB receptor ligands in animal tests of depression and anxiety. ''Pharmacological Reports''. 2007 Nov-Dec;59(6):645-55. PMID 18195453〕〔Jacobson LH, Cryan JF. Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents. ''Neuropharmacology''. 2008 Apr;54(5):854-62. PMID 18328507〕 and has a synergistic effect with GABAB agonists such as baclofen and GHB,〔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''. 2004 Nov 19;504(3):213-6. PMID 15541424〕〔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 and Physiology''. 2008 Sep;35(9):1113-5. PMID 18430050〕 as well as reducing self-administration of ethanol and cocaine.〔Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, Beart PM, Lawrence AJ. The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. ''Neuropharmacology''. 2006 Apr;50(5):632-9. PMID 16406445〕〔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''. 2007 Nov 28;574(2-3):148-57. PMID 17698060〕
==References==



抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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