CGP-7930

CGP-7930
(IUPAC) ime
	2,6-Di-tert-butil-4-(3-hidroksi-2,2-dimetil-propil)-fenol
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	5024764
Hemijski podaci
Formula	C19H32O2
Mol. masa	292,455 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=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 ; Key: XLWJPQQFJNGUPA-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

CGP-7930 je jedinjenje koje se koristi u naučnim istraživanjima kao pozitivni alosterni modulator GABA_B receptor.^[3]^[4]^[5]^[6] On ima anksiolitičko dejstvo u životinjskim studijama,^[7]^[8] kao i sinergističke efekte sa GABA_B agonistima, poput baklofena i GHB.^[9]^[10] On umanjuje samo-administraciju etanola i kokaina.^[11]^[12]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ 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. DOI:10.1111/j.1527-3458.2007.00021.x PMID 17894647
↑ 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
↑ 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
↑ 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

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] 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

[4] 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

[5] 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

[6] Adams CL, Lawrence AJ. CGP7930: a positive allosteric modulator of the GABAB receptor. CNS Drug Reviews. 2007 Fall;13(3):308-16. DOI:10.1111/j.1527-3458.2007.00021.x PMID 17894647

[7] 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

[8] 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

[9] 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

[10] 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

[11] 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

[12] 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

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