메뉴 건너뛰기




Volumn 34, Issue 6, 2006, Pages 1004-1011

Metabolism and disposition of a potent and selective GABA-A α2/3 receptor agonist in healthy male volunteers

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 7 (1,1 DIMETHYLETHY) 6 (2 ETHYL 2H 1,2,4 TRIAZOL 3 YLMETHOXY) 3 (2 FLUOROPHENYL) 1,2,4 TRIAZOLO[4,3 B]PYRIDAZINE; DRUG METABOLITE; PROPYLENE GLYCOL; TPA 023; UNCLASSIFIED DRUG; WATER;

EID: 33646780891     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.008193     Document Type: Article
Times cited : (11)

References (26)
  • 1
    • 29244437830 scopus 로고    scopus 로고
    • TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H- 1,2,4-triazol-3-ylmethoxy)- 3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for α2-and α3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates
    • Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, et al. (2006) TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl- 2H- 1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b] pyridazine], an agonist selective for α2-and α3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates. J Pharmacol Exp Ther 316:410-422.
    • (2006) J Pharmacol Exp Ther , vol.316 , pp. 410-422
    • Atack, J.R.1    Wafford, K.A.2    Tye, S.J.3    Cook, S.M.4    Sohal, B.5    Pike, A.6    Sur, C.7    Melillo, D.8    Bristow, L.9    Bromidge, F.10
  • 2
    • 0030068752 scopus 로고    scopus 로고
    • Rifampin drastically reduces plasma concentrations and effects of oral midazolam
    • Backman JT, Olkkola KT, and Neuvonen PJ (1996) Rifampin drastically reduces plasma concentrations and effects of oral midazolam. Clin Pharmacol Ther 59:7-13.
    • (1996) Clin Pharmacol Ther , vol.59 , pp. 7-13
    • Backman, J.T.1    Olkkola, K.T.2    Neuvonen, P.J.3
  • 3
    • 0031799363 scopus 로고    scopus 로고
    • International Union of Pharmacology. XV. Subtypes of -aminobutyric acid A receptors: Classification on the basis of subunit structure and receptor function
    • Barnard EA, Skolnick P, Olsen RW, Mohler H, Sieghart W, Biggio G, Braestrup C, Bateson AN, and Langer SZ (1998) International Union of Pharmacology. XV. Subtypes of -aminobutyric acid A receptors: classification on the basis of subunit structure and receptor function. Pharmacol Rev 50:291-313.
    • (1998) Pharmacol Rev , vol.50 , pp. 291-313
    • Barnard, E.A.1    Skolnick, P.2    Olsen, R.W.3    Mohler, H.4    Sieghart, W.5    Biggio, G.6    Braestrup, C.7    Bateson, A.N.8    Langer, S.Z.9
  • 5
    • 28544446472 scopus 로고    scopus 로고
    • 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy) -3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: A functionally selective gamma-aminobutyric acid (A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models
    • Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, et al. (2006) 7-(1,1-Dimethylethyl)-6-(2-ethyl- 2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b] pyridazine: a functionally selective gamma-aminobutyric acid (A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. J Med Chem 48:7089-7092.
    • (2006) J Med Chem , vol.48 , pp. 7089-7092
    • Carling, R.W.1    Madin, A.2    Guiblin, A.3    Russell, M.G.4    Moore, K.W.5    Mitchinson, A.6    Sohal, B.7    Pike, A.8    Cook, S.M.9    Ragan, I.C.10
  • 6
    • 0034692175 scopus 로고    scopus 로고
    • GABA-activated ligand gated ion channels: Medicinal chemistry and molecular biology
    • Chebib M and Johnston GAR (2000) GABA-activated ligand gated ion channels: medicinal chemistry and molecular biology. J Med Chem 43:1427-1447.
    • (2000) J Med Chem , vol.43 , pp. 1427-1447
    • Chebib, M.1    Johnston, G.A.R.2
  • 7
    • 32044440715 scopus 로고    scopus 로고
    • Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA(A) agonists for the treatment of anxiety
    • Goodacre SC, Hallett DJ, Carling RW, Castro JL, Reynolds DS, Pike A, Wafford KA, Newman R, Atack JR, and Street LJ (2006a) Imidazo[1,2-a]pyrazin-8- ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8- ones as alpha2/alpha3 subtype selective GABA(A) agonists for the treatment of anxiety. Bioorg Med Chem Lett 16:1582-1585.
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 1582-1585
    • Goodacre, S.C.1    Hallett, D.J.2    Carling, R.W.3    Castro, J.L.4    Reynolds, D.S.5    Pike, A.6    Wafford, K.A.7    Newman, R.8    Atack, J.R.9    Street, L.J.10
  • 11
    • 0001263889 scopus 로고
    • Cross relaxation without TOCSY: Transverse rotating-frame Overhauser effect spectroscopy
    • Hwang TL and Shaka AJ (1992) Cross relaxation without TOCSY: transverse rotating-frame Overhauser effect spectroscopy. J Am Chem Soc 114:3157-3159.
    • (1992) J Am Chem Soc , vol.114 , pp. 3157-3159
    • Hwang, T.L.1    Shaka, A.J.2
  • 15
    • 0028357256 scopus 로고
    • Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole and itraconazole
    • Olkkola KT, Backman JT, and Neuvonen PJ (1994) Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole and itraconazole. Clin Pharmacol Ther 55:481-485.
    • (1994) Clin Pharmacol Ther , vol.55 , pp. 481-485
    • Olkkola, K.T.1    Backman, J.T.2    Neuvonen, P.J.3
  • 16
    • 0035313382 scopus 로고    scopus 로고
    • GABAA receptor subtypes; dissecting their pharmacological functions
    • Rudolph U, Crestani F, and Mohler H (2001) GABAA receptor subtypes; dissecting their pharmacological functions. Trends Pharmacol Sci 22:188-194.
    • (2001) Trends Pharmacol Sci , vol.22 , pp. 188-194
    • Rudolph, U.1    Crestani, F.2    Mohler, H.3
  • 18
    • 0033461821 scopus 로고    scopus 로고
    • Simultaneous assessment of CYP3A4 and CYP1A2 activity in vivo with alprazolam and caffeine
    • Schmider J, Brockmoller J, Arnold G, Bauer S, and Roots I (1999) Simultaneous assessment of CYP3A4 and CYP1A2 activity in vivo with alprazolam and caffeine. Pharmacogenetics 9:725-734.
    • (1999) Pharmacogenetics , vol.9 , pp. 725-734
    • Schmider, J.1    Brockmoller, J.2    Arnold, G.3    Bauer, S.4    Roots, I.5
  • 19
    • 0039965711 scopus 로고
    • Complete 1H and 13C assignments of coenzyme B12 through the use of new two-dimensional NMR experiments
    • Summers MF, Marzilli LG, and Bax A (1986) Complete 1H and 13C assignments of coenzyme B12 through the use of new two-dimensional NMR experiments. J Am Chem Soc 108:4258-4294.
    • (1986) J Am Chem Soc , vol.108 , pp. 4258-4294
    • Summers, M.F.1    Marzilli, L.G.2    Bax, A.3
  • 20
  • 21
    • 0028568243 scopus 로고
    • Oral triazolam is potentially hazardous to patients receiving systemic antimycotics ketoconazole or itraconazole
    • Varhe A, Olkkola KT, and Neuvonen PJ (1994) Oral triazolam is potentially hazardous to patients receiving systemic antimycotics ketoconazole or itraconazole. Clin Pharmacol Ther 56:601-607.
    • (1994) Clin Pharmacol Ther , vol.56 , pp. 601-607
    • Varhe, A.1    Olkkola, K.T.2    Neuvonen, P.J.3
  • 25
  • 26
    • 0025596894 scopus 로고
    • B receptors in mammalian brain: Potential targets for drug development
    • B receptors in mammalian brain: potential targets for drug development. Drug Dev Res 21:161-167.
    • (1990) Drug Dev Res , vol.21 , pp. 161-167
    • Young, A.B.1    Chu, D.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.