메뉴 건너뛰기




Volumn 305, Issue 1, 2003, Pages 57-69

Pharmacological characterization of a novel nonpeptide antagonist radioligand, (±)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor receptors

Author keywords

[No Author keywords available]

Indexed keywords

BUTYL[2,5 DIMETHYL 7 (2,4,6 TRIMETHYLPHENYL) 7H PYRROLO[2,3 D]PYRIMIDIN 4 YL]ETHYLAMINE; CORTICOTROPIN RELEASING FACTOR; N (2 METHYL 4 METHOXYPHENYL) 1 [1 (METHOXYMETHYL)PROPYL] 6 METHYL 1H 1,2,3 TRIAZOLO[4,5 C]PYRIDIN 4 AMINE; RADIOLIGAND; SN 003; UNCLASSIFIED DRUG;

EID: 0037379954     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.046128     Document Type: Article
Times cited : (32)

References (40)
  • 1
    • 0023634084 scopus 로고
    • Corticotropin-releasing factor receptors: Distribution and regulation in brain, pituitary, and peripheral tissues
    • Aguilera G, Millan MA, Hauger RL, and Catt KJ (1987) Corticotropin-releasing factor receptors: distribution and regulation in brain, pituitary, and peripheral tissues. Ann NY Acad Sci 512:48-66.
    • (1987) Ann NY Acad Sci , vol.512 , pp. 48-66
    • Aguilera, G.1    Millan, M.A.2    Hauger, R.L.3    Catt, K.J.4
  • 4
    • 0029786101 scopus 로고    scopus 로고
    • A single-point slight alteration set as a tool for structure-activity relationship studies of ovine corticotropin releasing factor
    • Beyermann M, Fechner K, Furkert J, Krause E, and Bienert M (1996) A single-point slight alteration set as a tool for structure-activity relationship studies of ovine corticotropin releasing factor. J Med Chem 39:3324-3330.
    • (1996) J Med Chem , vol.39 , pp. 3324-3330
    • Beyermann, M.1    Fechner, K.2    Furkert, J.3    Krause, E.4    Bienert, M.5
  • 5
    • 0034598980 scopus 로고    scopus 로고
    • Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium
    • Bymaster FP and Falcone JF (2000) Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium. Eur J Pharmacol 390:245-248.
    • (2000) Eur J Pharmacol , vol.390 , pp. 245-248
    • Bymaster, F.P.1    Falcone, J.F.2
  • 6
    • 0036468517 scopus 로고    scopus 로고
    • The CRF peptide family and their receptors: Yet more partners discovered
    • Dautzenberg FM and Hauger RL (2002) The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol Sci 23:71-77.
    • (2002) Trends Pharmacol Sci , vol.23 , pp. 71-77
    • Dautzenberg, F.M.1    Hauger, R.L.2
  • 7
    • 0026542671 scopus 로고
    • The role of the amygdala in fear-potentiated startle: Implications for animal models of anxiety
    • Davis M (1992) The role of the amygdala in fear-potentiated startle: implications for animal models of anxiety. Trends Pharmacol Sci 13:35-41.
    • (1992) Trends Pharmacol Sci , vol.13 , pp. 35-41
    • Davis, M.1
  • 8
    • 0023088979 scopus 로고
    • Corticotropin-releasing factor receptors in the rat central nervous system: Characterization and regional distribution
    • De Souza EB (1987) Corticotropin-releasing factor receptors in the rat central nervous system: Characterization and regional distribution. J Neurosci 7:88-100.
    • (1987) J Neurosci , vol.7 , pp. 88-100
    • De Souza, E.B.1
  • 9
    • 0001008136 scopus 로고    scopus 로고
    • Corticotropin-releasing factor. Physiology, pharmacology and role in central nervous system and immune disorders
    • (Bloom FE and Kupfer DJ eds) Raven Press, New York
    • De Souza EB and Grigoriadis DE (1998) Corticotropin-releasing factor. Physiology, pharmacology and role in central nervous system and immune disorders, in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 505-517, Raven Press, New York.
    • (1998) Psychopharmacology: The Fourth Generation of Progress , pp. 505-517
    • De Souza, E.B.1    Grigoriadis, D.E.2
  • 10
    • 0022340954 scopus 로고
    • Corticotropin-releasing factor receptors are widely distributed within the rat central nervous system: An autoradiographic study
    • De Souza EB, Insel TR, Perrin MH, Rivier J, Vale WW, and Kuhar MJ (1985) Corticotropin-releasing factor receptors are widely distributed within the rat central nervous system: an autoradiographic study. J Neurosci 5:3189-3203.
    • (1985) J Neurosci , vol.5 , pp. 3189-3203
    • De Souza, E.B.1    Insel, T.R.2    Perrin, M.H.3    Rivier, J.4    Vale, W.W.5    Kuhar, M.J.6
  • 11
    • 0034124297 scopus 로고    scopus 로고
    • Corticotropin releasing factor (CRF) receptor modulators: Progress and opportunities for new therapeutic agents
    • Gilligan PJ, Robertson DW, and Zaczek R (2000) Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. J Med Chem 43:1641-1660.
    • (2000) J Med Chem , vol.43 , pp. 1641-1660
    • Gilligan, P.J.1    Robertson, D.W.2    Zaczek, R.3
  • 12
    • 18344394149 scopus 로고    scopus 로고
    • 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1- (3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A), a potent and selective corticotrophin-releasing factor1 receptor antagonist. II. Characterization in rodent models of stress-related disorders
    • Griebel G, Simiand J, Steinberg R, Jung M, Gully D, Roger P, Geslin M, Scatton B, Maffrand JP, and Soubrié P (2002) 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl- 1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A), a potent and selective corticotrophin-releasing factor1 receptor antagonist. II. Characterization in rodent models of stress-related disorders. J Pharmacol Exp Ther 301:333-345.
    • (2002) J Pharmacol Exp Ther , vol.301 , pp. 333-345
    • Griebel, G.1    Simiand, J.2    Steinberg, R.3    Jung, M.4    Gully, D.5    Roger, P.6    Geslin, M.7    Scatton, B.8    Maffrand, J.P.9    Soubrié, P.10
  • 13
    • 0023687287 scopus 로고
    • The brain corticotropin-releasing factor (CRF) receptor is of lower apparent molecular weight than the CRF receptor in anterior pituitary: Evidence from chemical cross-linking studies
    • Grigoriadis DE and De Souza EB (1988) The brain corticotropin-releasing factor (CRF) receptor is of lower apparent molecular weight than the CRF receptor in anterior pituitary: evidence from chemical cross-linking studies. J Biol Chem 263:10927-10931.
    • (1988) J Biol Chem , vol.263 , pp. 10927-10931
    • Grigoriadis, D.E.1    De Souza, E.B.2
  • 14
    • 0024459432 scopus 로고
    • Heterogeneity between brain and pituitary corticotropin-releasing factor receptors is due to differential glycosylation
    • Grigoriadis DE and De Souza EB (1989) Heterogeneity between brain and pituitary corticotropin-releasing factor receptors is due to differential glycosylation. Endocrinology 125:1877-1888.
    • (1989) Endocrinology , vol.125 , pp. 1877-1888
    • Grigoriadis, D.E.1    De Souza, E.B.2
  • 15
    • 18344362026 scopus 로고    scopus 로고
    • 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1 (3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): A potent and selective corticotrophin-releasing factorl receptor antagonist. I. Biochemical and pharmacological characterization
    • Gully D, Geslin M, Serva L, Fontaine E, Roger P, Lair C, Darre V, Marcy C, Rouby PE, Simiand J, et al. (2002) 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1 (3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): a potent and selective corticotrophin-releasing factorl receptor antagonist. I. Biochemical and pharmacological characterization. J Pharmacol Exp Ther 301:322-332.
    • (2002) J Pharmacol Exp Ther , vol.301 , pp. 322-332
    • Gully, D.1    Geslin, M.2    Serva, L.3    Fontaine, E.4    Roger, P.5    Lair, C.6    Darre, V.7    Marcy, C.8    Rouby, P.E.9    Simiand, J.10
  • 16
    • 12944262399 scopus 로고    scopus 로고
    • Oral administration of a corticotropin-releasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine and autonomic responses to stress in primates
    • Habib KE, Weld KP, Rice KC, Pushkas J, Champoux M, Listwak S, Webster EL, Atkinson AJ, Schulkin J, Contoreggi C, et al. (2000) Oral administration of a corticotropin-releasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine and autonomic responses to stress in primates. Proc Natl Acad Sci USA 97:6079-6084.
    • (2000) Proc Natl Acad Sci USA , vol.97 , pp. 6079-6084
    • Habib, K.E.1    Weld, K.P.2    Rice, K.C.3    Pushkas, J.4    Champoux, M.5    Listwak, S.6    Webster, E.L.7    Atkinson, A.J.8    Schulkin, J.9    Contoreggi, C.10
  • 17
    • 0030983781 scopus 로고    scopus 로고
    • Regulation of corticotropin-releasing factor receptor function in human Y-79 retinoblastoma cells: Rapid and reversible homologous desensitization but prolonged recovery
    • Hauger RL, Dautzenberg FM, Flaccus A, Liepold T, and Spiess J (1997) Regulation of corticotropin-releasing factor receptor function in human Y-79 retinoblastoma cells: rapid and reversible homologous desensitization but prolonged recovery. J Neurochem 68:2308-2316.
    • (1997) J Neurochem , vol.68 , pp. 2308-2316
    • Hauger, R.L.1    Dautzenberg, F.M.2    Flaccus, A.3    Liepold, T.4    Spiess, J.5
  • 19
    • 0036289254 scopus 로고    scopus 로고
    • Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist
    • Heinrichs SC, De Souza EB, Schulteis G, Lapsansky JL, and Grigoriadis DE (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27:194-202.
    • (2002) Neuropsychopharmacology , vol.27 , pp. 194-202
    • Heinrichs, S.C.1    De Souza, E.B.2    Schulteis, G.3    Lapsansky, J.L.4    Grigoriadis, D.E.5
  • 21
    • 0035040487 scopus 로고    scopus 로고
    • Hyperactivity of CRH neuronal circuits as a target for therapeutic interventions in affective disorders
    • Keck ME and Holsboer F (2001) Hyperactivity of CRH neuronal circuits as a target for therapeutic interventions in affective disorders. Peptides 22:835-844.
    • (2001) Peptides , vol.22 , pp. 835-844
    • Keck, M.E.1    Holsboer, F.2
  • 22
    • 0036150160 scopus 로고    scopus 로고
    • Brain pharmacokinetics of a non-peptidic corticotropin-releasing factor antagonist
    • Keller C, Bruelisauer A, Lemaire M, and Enz A (2002) Brain pharmacokinetics of a non-peptidic corticotropin-releasing factor antagonist. Drug MetabDispos 30:173-176.
    • (2002) Drug Metab Dispos , vol.30 , pp. 173-176
    • Keller, C.1    Bruelisauer, A.2    Lemaire, M.3    Enz, A.4
  • 26
    • 0030731863 scopus 로고    scopus 로고
    • Localization of agonist-and antagonist-binding domains of human corticotropin-releasing factor receptors
    • Liaw CW, Grigoriadis DE, Lorang MT, De Souza EB, and Maki RA (1997) Localization of agonist- and antagonist-binding domains of human corticotropin-releasing factor receptors. Mol Endocrinol 11:2048-2053.
    • (1997) Mol Endocrinol , vol.11 , pp. 2048-2053
    • Liaw, C.W.1    Grigoriadis, D.E.2    Lorang, M.T.3    De Souza, E.B.4    Maki, R.A.5
  • 28
    • 0032586642 scopus 로고    scopus 로고
    • 1 receptor: Design of small molecule inhibitors, receptor subtypes and clinical indications
    • 1 receptor: design of small molecule inhibitors, receptor subtypes and clinical indications. Curr Pharm Des 5:289-315.
    • (1999) Curr Pharm Des , vol.5 , pp. 289-315
    • McCarthy, J.R.1    Heinrichs, S.C.2    Grigoriadis, D.E.3
  • 29
    • 0036941164 scopus 로고    scopus 로고
    • 1 receptor antagonist DMP696 produces anxiolytic effects and inhibits the stress-induced hypothalamic-pituitary-adrenal axis activation without sedation or ataxia in rats
    • 1 receptor antagonist DMP696 produces anxiolytic effects and inhibits the stress-induced hypothalamic-pituitary-adrenal axis activation without sedation or ataxia in rats. Psychopharmacology 165:86-92.
    • (2002) Psychopharmacology , vol.165 , pp. 86-92
    • McElroy, J.F.1    Ward, K.A.2    Zeller, K.L.3    Jones, K.W.4    Gilligan, P.J.5    He, L.6    Lelas, S.7
  • 30
    • 0026332080 scopus 로고
    • Physiology and pharmacology of corticotropin-releasing factor
    • Owens MJ and Nemeroff (1991) Physiology and pharmacology of corticotropin-releasing factor. Pharmacol Rev 43:425-473.
    • (1991) Pharmacol Rev , vol.43 , pp. 425-473
    • Owens, M.J.1    Nemeroff2
  • 35
    • 0028043957 scopus 로고
    • Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding
    • Rosenkilde MM, Cahir M, Gether U, Hjorth SA, and Schwartz TW (1994) Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding. J Biol Chem 269:28160-28164.
    • (1994) J Biol Chem , vol.269 , pp. 28160-28164
    • Rosenkilde, M.M.1    Cahir, M.2    Gether, U.3    Hjorth, S.A.4    Schwartz, T.W.5
  • 38
    • 0015378131 scopus 로고
    • Culture of enzymatically dispersed anterior pituitary cells: Functional validation of a method
    • Vale W, Grant G, Amoss M, Blackwell R, and Guillemin R (1972) Culture of enzymatically dispersed anterior pituitary cells: functional validation of a method. Endocrinology 91:562-572.
    • (1972) Endocrinology , vol.91 , pp. 562-572
    • Vale, W.1    Grant, G.2    Amoss, M.3    Blackwell, R.4    Guillemin, R.5
  • 39
    • 0019782980 scopus 로고
    • Characterization of a 41 residue ovine hypothalamic peptide that stimulates secretion of corticotropin and β-endorphin
    • Vale W, Spiess J, Rivier C, and Rivier J (1981) Characterization of a 41 residue ovine hypothalamic peptide that stimulates secretion of corticotropin and β-endorphin. Science (Wash DC) 213:1394-1397.
    • (1981) Science (Wash DC) , vol.213 , pp. 1394-1397
    • Vale, W.1    Spiess, J.2    Rivier, C.3    Rivier, J.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.