메뉴 건너뛰기




Volumn 65, Issue 9, 2011, Pages 910-918

[76Br]BMK-152, a nonpeptide analogue, with high affinity and low nonspecific binding for the corticotropin-releasing factor type 1 receptor

Author keywords

Br 76 BMK; Corticotropin releasing factor type 1 receptors; CRF1 receptor; PET

Indexed keywords

[8 (4 BROMO 2,6 DIMETHOXYPHENYL) 2,7 DIMETHYLPYRAZOLO[1,5 A][1,3,5]TRIAZIN 4 YL] N,N BIS(2 METHOXYETHYL)AMINE; BROMINE 76; CONTRAST MEDIUM; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; GLYCOPROTEIN P; UNCLASSIFIED DRUG;

EID: 79959985843     PISSN: 08874476     EISSN: 10982396     Source Type: Journal    
DOI: 10.1002/syn.20919     Document Type: Article
Times cited : (10)

References (50)
  • 1
    • 33744809537 scopus 로고    scopus 로고
    • Comparison of the stress response in rats to repeated isoflurane or CO2:O2 anesthesia used for restraint during serial blood collection via the jugular vein
    • Altholtz LY, Fowler KA, Badura LL, Kovacs MS. 2006. Comparison of the stress response in rats to repeated isoflurane or CO2:O2 anesthesia used for restraint during serial blood collection via the jugular vein. J Am Assoc Lab Anim Sci 45: 17-22.
    • (2006) J Am Assoc Lab Anim Sci , vol.45 , pp. 17-22
    • Altholtz, L.Y.1    Fowler, K.A.2    Badura, L.L.3    Kovacs, M.S.4
  • 2
    • 0032899957 scopus 로고    scopus 로고
    • The role of corticotropin-releasing factor in depression and anxiety disorders
    • Arborelius L, Owens MJ, Plotsky PM, Nemeroff CB. 1999. The role of corticotropin-releasing factor in depression and anxiety disorders. J Endocrinol 160: 1-12.
    • (1999) J Endocrinol , vol.160 , pp. 1-12
    • Arborelius, L.1    Owens, M.J.2    Plotsky, P.M.3    Nemeroff, C.B.4
  • 3
    • 33845217668 scopus 로고    scopus 로고
    • Evidence that corticotropin-releasing factor receptor type 1 couples to Gs- and Gi-proteins through different conformations of its J-domain
    • Berger H, Heinrich N, Wietfeld D, Bienert M, Beyermann M. 2006. Evidence that corticotropin-releasing factor receptor type 1 couples to Gs- and Gi-proteins through different conformations of its J-domain. Br J Pharmacol 149: 942-947.
    • (2006) Br J Pharmacol , vol.149 , pp. 942-947
    • Berger, H.1    Heinrich, N.2    Wietfeld, D.3    Bienert, M.4    Beyermann, M.5
  • 4
    • 34447566050 scopus 로고    scopus 로고
    • Achieving signalling selectivity of ligands for the corticotropin-releasing factor type 1 receptor by modifying the agonist's signalling domain
    • Beyermann M, Heinrich N, Fechner K, Furkert J, Zhang W, Kraetke O, Bienert M, Berger H. 2007. Achieving signalling selectivity of ligands for the corticotropin-releasing factor type 1 receptor by modifying the agonist's signalling domain. Br J Pharmacol 151: 851-859.
    • (2007) Br J Pharmacol , vol.151 , pp. 851-859
    • Beyermann, M.1    Heinrich, N.2    Fechner, K.3    Furkert, J.4    Zhang, W.5    Kraetke, O.6    Bienert, M.7    Berger, H.8
  • 5
    • 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, 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
  • 6
    • 0022558755 scopus 로고
    • Corticotropin-releasing factor receptors in the pituitary gland and central nervous system: Methods and overview
    • De Souza EB, Kuhar MJ. 1986a. Corticotropin-releasing factor receptors in the pituitary gland and central nervous system: Methods and overview. Methods Enzymol 124: 560-590.
    • (1986) Methods Enzymol , vol.124 , pp. 560-590
    • De Souza, E.B.1    Kuhar, M.J.2
  • 7
    • 0022438732 scopus 로고
    • Corticotropin-releasing factor receptors: Autoradiographic identification
    • De Souza EB, Kuhar MJ. 1986b. Corticotropin-releasing factor receptors: Autoradiographic identification. Res Publ Assoc Res Nerv Ment Dis 64: 179-198.
    • (1986) Res Publ Assoc Res Nerv Ment Dis , vol.64 , pp. 179-198
    • De Souza, E.B.1    Kuhar, M.J.2
  • 9
    • 0038689058 scopus 로고    scopus 로고
    • Effects of the selective nonpeptide corticotropin-releasing factor receptor 1 antagonist antalarmin in the chronic mild stress model of depression in mice
    • Ducottet C, Griebel G, Belzung C. 2003. Effects of the selective nonpeptide corticotropin-releasing factor receptor 1 antagonist antalarmin in the chronic mild stress model of depression in mice. Prog Neuropsychopharmacol Biol Psychiatry 27: 625-631.
    • (2003) Prog Neuropsychopharmacol Biol Psychiatry , vol.27 , pp. 625-631
    • Ducottet, C.1    Griebel, G.2    Belzung, C.3
  • 10
    • 2342436512 scopus 로고    scopus 로고
    • PET Studies on P-glycoprotein function in the blood-brain barrier: How it affects uptake and binding of drugs within the CNS
    • Elsinga PH, Hendrikse NH, Bart J, Vaalburg W, van Waarde A. 2004. PET Studies on P-glycoprotein function in the blood-brain barrier: How it affects uptake and binding of drugs within the CNS. Curr Pharm Des 10: 1493-1503.
    • (2004) Curr Pharm Des , vol.10 , pp. 1493-1503
    • Elsinga, P.H.1    Hendrikse, N.H.2    Bart, J.3    Vaalburg, W.4    van Waarde, A.5
  • 11
    • 0029551072 scopus 로고
    • Corticotropin-releasing factor (CRF) receptors in infant rhesus monkey brain and pituitary gland: Biochemical characterization and autoradiographic localization
    • Grigoriadis DE, Dent GW, Turner JG, Uno H, Shelton SE, De Souza EB, Kalin NH. 1995. Corticotropin-releasing factor (CRF) receptors in infant rhesus monkey brain and pituitary gland: Biochemical characterization and autoradiographic localization. Dev Neurosci 17: 357-367.
    • (1995) Dev Neurosci , vol.17 , pp. 357-367
    • Grigoriadis, D.E.1    Dent, G.W.2    Turner, J.G.3    Uno, H.4    Shelton, S.E.5    De Souza, E.B.6    Kalin, N.H.7
  • 12
    • 57649132043 scopus 로고    scopus 로고
    • Drugability of extracellular targets: Discovery of small molecule drugs targeting allosteric, functional, and subunit-selective sites on GPCRs and ion channels
    • Grigoriadis DE, Hoare SR, Lechner SM, Slee DH, Williams JA. 2009. Drugability of extracellular targets: Discovery of small molecule drugs targeting allosteric, functional, and subunit-selective sites on GPCRs and ion channels. Neuropsychopharmacology 34: 106-125.
    • (2009) Neuropsychopharmacology , vol.34 , pp. 106-125
    • Grigoriadis, D.E.1    Hoare, S.R.2    Lechner, S.M.3    Slee, D.H.4    Williams, J.A.5
  • 13
    • 0029665585 scopus 로고    scopus 로고
    • 125I-Tyro-sauvagine: A novel high affinity radioligand for the pharmacological and biochemical study of human corticotropin-releasing factor 2 alpha receptors
    • Grigoriadis DE, Liu XJ, Vaughn J, Palmer SF, True CD, Vale WW, Ling N, De Souza EB. 1996a. 125I-Tyro-sauvagine: A novel high affinity radioligand for the pharmacological and biochemical study of human corticotropin-releasing factor 2 alpha receptors. Mol Pharmacol 50: 679-686.
    • (1996) Mol Pharmacol , vol.50 , pp. 679-686
    • Grigoriadis, D.E.1    Liu, X.J.2    Vaughn, J.3    Palmer, S.F.4    True, C.D.5    Vale, W.W.6    Ling, N.7    De Souza, E.B.8
  • 15
    • 0024338774 scopus 로고
    • Normal pattern of labeling of cerebral cortical corticotropin-releasing factor (CRF) receptors in Alzheimer's disease: Evidence from chemical cross-linking studies
    • Grigoriadis DE, Struble RG, Price DL, De Souza EB. 1989. Normal pattern of labeling of cerebral cortical corticotropin-releasing factor (CRF) receptors in Alzheimer's disease: Evidence from chemical cross-linking studies. Neuropharmacology 28: 761-764.
    • (1989) Neuropharmacology , vol.28 , pp. 761-764
    • Grigoriadis, D.E.1    Struble, R.G.2    Price, D.L.3    De Souza, E.B.4
  • 16
    • 33746998914 scopus 로고    scopus 로고
    • Corticotropin releasing factor (CRF) receptor signaling in the central nervous system: New molecular targets
    • Hauger RL, Risbrough V, Brauns O, Dautzenberg FM. 2006. Corticotropin releasing factor (CRF) receptor signaling in the central nervous system: New molecular targets. CNS Neurol Disord Drug Targets 5: 453-479.
    • (2006) CNS Neurol Disord Drug Targets , vol.5 , pp. 453-479
    • Hauger, R.L.1    Risbrough, V.2    Brauns, O.3    Dautzenberg, F.M.4
  • 19
    • 16244383540 scopus 로고    scopus 로고
    • Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors
    • Hoare SR. 2005. Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors. Drug Discov Today 10: 417-427.
    • (2005) Drug Discov Today , vol.10 , pp. 417-427
    • Hoare, S.R.1
  • 20
    • 0037334023 scopus 로고    scopus 로고
    • Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists
    • Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE. 2003a. Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol Pharmacol 63: 751-765.
    • (2003) Mol Pharmacol , vol.63 , pp. 751-765
    • Hoare, S.R.1    Sullivan, S.K.2    Ling, N.3    Crowe, P.D.4    Grigoriadis, D.E.5
  • 21
    • 0842265891 scopus 로고    scopus 로고
    • Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: Detection, and pharmacological evaluation by peptide ligands
    • Hoare SR, Sullivan SK, Pahuja A, Ling N, Crowe PD, Grigoriadis DE. 2003b. Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: Detection, and pharmacological evaluation by peptide ligands. Peptides 24: 1881-1897.
    • (2003) Peptides , vol.24 , pp. 1881-1897
    • Hoare, S.R.1    Sullivan, S.K.2    Pahuja, A.3    Ling, N.4    Crowe, P.D.5    Grigoriadis, D.E.6
  • 22
    • 1842486848 scopus 로고    scopus 로고
    • Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: Regulation by G-protein and nonpeptide antagonists
    • Hoare SR, Sullivan SK, Schwarz DA, Ling N, Vale WW, Crowe PD, Grigoriadis DE. 2004. Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: Regulation by G-protein and nonpeptide antagonists. Biochemistry 43: 3996-4011.
    • (2004) Biochemistry , vol.43 , pp. 3996-4011
    • Hoare, S.R.1    Sullivan, S.K.2    Schwarz, D.A.3    Ling, N.4    Vale, W.W.5    Crowe, P.D.6    Grigoriadis, D.E.7
  • 23
    • 0031679962 scopus 로고    scopus 로고
    • The anesthetic isoflurane decreases ionized calcium and increases parathyroid hormone and osteocalcin in cynomolgus monkeys
    • Hotchkiss CE, Brommage R, Du M, Jerome CP. 1998. The anesthetic isoflurane decreases ionized calcium and increases parathyroid hormone and osteocalcin in cynomolgus monkeys. Bone 23: 479-484.
    • (1998) Bone , vol.23 , pp. 479-484
    • Hotchkiss, C.E.1    Brommage, R.2    Du, M.3    Jerome, C.P.4
  • 26
    • 3042789514 scopus 로고    scopus 로고
    • Experiment assessment of mass effects in the rat: Implications for small animal PET imaging
    • Jagoda EM, Vaquero JJ, Seidel J, Green MV, Eckelman WC. 2004. Experiment assessment of mass effects in the rat: Implications for small animal PET imaging. Nucl Med Biol 31: 771-779.
    • (2004) Nucl Med Biol , vol.31 , pp. 771-779
    • Jagoda, E.M.1    Vaquero, J.J.2    Seidel, J.3    Green, M.V.4    Eckelman, W.C.5
  • 27
    • 21344450520 scopus 로고    scopus 로고
    • The effects of CRF antagonists, antalarmin. CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats
    • Jutkiewicz EM, Wood SK, Houshyar H, Hsin LW, Rice KC, Woods JH. 2005. The effects of CRF antagonists, antalarmin. CP154, 526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl) 180: 215-223.
    • (2005) Psychopharmacology (Berl) , vol.180 , pp. 215-223
    • Jutkiewicz, E.M.1    Wood, S.K.2    Houshyar, H.3    Hsin, L.W.4    Rice, K.C.5    Woods, J.H.6
  • 29
    • 77249152214 scopus 로고    scopus 로고
    • Transient early-life forebrain corticotropin-releasing hormone elevation causes long-lasting anxiogenic and despair-like changes in mice
    • Kolber BJ, Boyle MP, Wieczorek L, Kelley CL, Onwuzurike CC, Nettles SA, Vogt SK, Muglia LJ. 2010. Transient early-life forebrain corticotropin-releasing hormone elevation causes long-lasting anxiogenic and despair-like changes in mice. J Neurosci 30: 2571-2581.
    • (2010) J Neurosci , vol.30 , pp. 2571-2581
    • Kolber, B.J.1    Boyle, M.P.2    Wieczorek, L.3    Kelley, C.L.4    Onwuzurike, C.C.5    Nettles, S.A.6    Vogt, S.K.7    Muglia, L.J.8
  • 33
    • 0026332080 scopus 로고
    • Physiology and pharmacology of corticotropin-releasing factor
    • Owens MJ, Nemeroff CB. 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    Nemeroff, C.B.2
  • 36
    • 0030611612 scopus 로고    scopus 로고
    • Autoradiographic localization of CRF1 and CRF2 binding sites in adult rat brain
    • Primus RJ, Yevich E, Baltazar C, Gallager DW. 1997. Autoradiographic localization of CRF1 and CRF2 binding sites in adult rat brain. Neuropsychopharmacology 17: 308-316.
    • (1997) Neuropsychopharmacology , vol.17 , pp. 308-316
    • Primus, R.J.1    Yevich, E.2    Baltazar, C.3    Gallager, D.W.4
  • 37
    • 70449372203 scopus 로고    scopus 로고
    • CRH signaling. Molecular specificity for drug targeting in the CNS
    • Refojo D, Holsboer F. 2009. CRH signaling. Molecular specificity for drug targeting in the CNS. Ann NY Acad Sci 1179: 106-119.
    • (2009) Ann NY Acad Sci , vol.1179 , pp. 106-119
    • Refojo, D.1    Holsboer, F.2
  • 39
    • 0032903611 scopus 로고    scopus 로고
    • Corticotropic-releasing hormone and serotonin interact in the human brainstem: Behavioral implications
    • Ruggiero DA, Underwood MD, Rice PM, Mann JJ, Arango V. 1999. Corticotropic-releasing hormone and serotonin interact in the human brainstem: Behavioral implications. Neuroscience 91: 1343- 1354.
    • (1999) Neuroscience , vol.91 , pp. 1343-1354
    • Ruggiero, D.A.1    Underwood, M.D.2    Rice, P.M.3    Mann, J.J.4    Arango, V.5
  • 40
    • 0043281643 scopus 로고    scopus 로고
    • Autoradiographic and in situ hybridization localization of corticotropin-releasing factor 1 and 2 receptors in nonhuman primate brain
    • Sanchez MM, Young LJ, Plotsky PM, Insel TR. 1999. Autoradiographic and in situ hybridization localization of corticotropin-releasing factor 1 and 2 receptors in nonhuman primate brain. J Comp Neurol 408: 365-377.
    • (1999) J Comp Neurol , vol.408 , pp. 365-377
    • Sanchez, M.M.1    Young, L.J.2    Plotsky, P.M.3    Insel, T.R.4
  • 44
    • 18144410970 scopus 로고    scopus 로고
    • The role of CRF1 receptors for sympathetic nervous response to laparotomy in anesthetized rats
    • Uetsuki N, Segawa H, Mayahara T, Fukuda K. 2005. The role of CRF1 receptors for sympathetic nervous response to laparotomy in anesthetized rats. Brain Res 1044: 107-115.
    • (2005) Brain Res , vol.1044 , pp. 107-115
    • Uetsuki, N.1    Segawa, H.2    Mayahara, T.3    Fukuda, K.4
  • 45
    • 67650573398 scopus 로고    scopus 로고
    • CRF receptors as a potential target in the development of novel pharmacotherapies for depression
    • Valdez GR. 2009. CRF receptors as a potential target in the development of novel pharmacotherapies for depression. Curr Pharm Des 15: 1587-1594.
    • (2009) Curr Pharm Des , vol.15 , pp. 1587-1594
    • Valdez, G.R.1
  • 46
    • 0019782980 scopus 로고
    • Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin
    • Vale W, Spiess J, Rivier C, Rivier J. 1981. Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin. Science 213: 1394-1397.
    • (1981) Science , vol.213 , pp. 1394-1397
    • Vale, W.1    Spiess, J.2    Rivier, C.3    Rivier, J.4
  • 47
    • 0030445812 scopus 로고    scopus 로고
    • In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: Suppression of pituitary ACTH release and peripheral inflammation
    • Webster EL, Lewis DB, Torpy DJ, Zachman EK, Rice KC, Chrousos GP. 1996. In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: Suppression of pituitary ACTH release and peripheral inflammation. Endocrinology 137: 5747-5750.
    • (1996) Endocrinology , vol.137 , pp. 5747-5750
    • Webster, E.L.1    Lewis, D.B.2    Torpy, D.J.3    Zachman, E.K.4    Rice, K.C.5    Chrousos, G.P.6
  • 49
    • 77952549409 scopus 로고    scopus 로고
    • Progress in corticotropin-releasing factor-1 antagonist development
    • Zorrilla EP, Koob GF. 2010. Progress in corticotropin-releasing factor-1 antagonist development. Drug Discov Today 15: 371-383.
    • (2010) Drug Discov Today , vol.15 , pp. 371-383
    • Zorrilla, E.P.1    Koob, G.F.2
  • 50
    • 0037131064 scopus 로고    scopus 로고
    • Effects of antalarmin, a CRF type 1 receptor antagonist, on anxiety-like behavior and motor activation in the rat
    • Zorrilla EP, Valdez GR, Nozulak J, Koob GF, Markou A. 2002. Effects of antalarmin, a CRF type 1 receptor antagonist, on anxiety-like behavior and motor activation in the rat. Brain Res 952: 188-199.
    • (2002) Brain Res , vol.952 , pp. 188-199
    • Zorrilla, E.P.1    Valdez, G.R.2    Nozulak, J.3    Koob, G.F.4    Markou, A.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.