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Volumn 40, Issue 4, 2013, Pages 547-553

Palladium mediated 11C-cyanation and characterization in the non-human primate brain of the novel mGluR5 radioligand [11C]AZD9272

Author keywords

Cynomolgus monkeys; Hydrogen 11C cyanide ( 11C HCN); Metabotropic glutamate receptor 5 (mGluR5); Positron emission tomography (PET); Radiochemistry

Indexed keywords

2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; 3 (6 METHYL PYRIDIN 2 YLETHYNYL) CYCLOHEX 2 ENONE O METHYLOXIME; 3 (6 METHYL PYRIDIN 2 YLETHYNYL) CYCLOHEX 2 ENONE O METHYLOXIME C 11; 3 [(2 METHYL 4 THIAZOLYL)ETHYNYL]PYRIDINE; 3 FLUORO 5 [3 [5 FLUOROPYRIDIN 2 YL] 1,2,4 OXADIAZOL 5 YL]BENZONITRILE; 3 FLUORO 5 [3 [5 FLUOROPYRIDIN 2 YL] 1,2,4 OXADIAZOL 5 YL]BENZONITRILE C 11; 3 FLUORO 5 [[PYRIDIN 3 YL]ETHYNYL]BENZONITRILE F 18; 3-(6-METHYL-PYRIDIN-2-YLETHYNYL)-CYCLOHEX-2-ENONE O METHYLOXIME; ABP 688; AZD 9272; CARBON 11; METABOTROPIC RECEPTOR 5; PALLADIUM; RADIOLIGAND; UNCLASSIFIED DRUG; AZD9272; CARBON; LIGAND; NITRILE; OXADIAZOLE DERIVATIVE; PYRIDINE DERIVATIVE; DIAGNOSTIC AGENT;

EID: 84876731792     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2012.12.012     Document Type: Article
Times cited : (19)

References (32)
  • 1
    • 0035397917 scopus 로고    scopus 로고
    • Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders
    • Spooren W.P., Gasparini F., Salt T.E., Kuhn R. Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders. Trends Pharmacol Sci 2001, 22(7):331-337.
    • (2001) Trends Pharmacol Sci , vol.22 , Issue.7 , pp. 331-337
    • Spooren, W.P.1    Gasparini, F.2    Salt, T.E.3    Kuhn, R.4
  • 2
    • 0029145935 scopus 로고
    • Roles of specific metabotropic glutamate-receptor subtypes in regulation of hippocampal CA1 pyramidal cell excitability
    • Gereau R.W., Conn P.J. Roles of specific metabotropic glutamate-receptor subtypes in regulation of hippocampal CA1 pyramidal cell excitability. J Neurophysiol 1995, 74(1):122-129.
    • (1995) J Neurophysiol , vol.74 , Issue.1 , pp. 122-129
    • Gereau, R.W.1    Conn, P.J.2
  • 3
    • 0028912822 scopus 로고
    • The metabotropic glutamate receptors: structure and functions
    • Pin J.P., Duvoisin R. The metabotropic glutamate receptors: structure and functions. Neuropharmacology 1995, 34(1):1-26.
    • (1995) Neuropharmacology , vol.34 , Issue.1 , pp. 1-26
    • Pin, J.P.1    Duvoisin, R.2
  • 4
    • 0034526844 scopus 로고    scopus 로고
    • Evaluation of the activity of antimicrobial agents against Legionella pneumophila multiplying in a human monocytic cell line, THP-1, and an alveolar epithelial cell line, A549
    • Kunishima H., Takemura H., Yamamoto H., Kanemitsu K., Shimada J. Evaluation of the activity of antimicrobial agents against Legionella pneumophila multiplying in a human monocytic cell line, THP-1, and an alveolar epithelial cell line, A549. J Infect Chemother 2000, 6(4):206-210.
    • (2000) J Infect Chemother , vol.6 , Issue.4 , pp. 206-210
    • Kunishima, H.1    Takemura, H.2    Yamamoto, H.3    Kanemitsu, K.4    Shimada, J.5
  • 5
    • 0034721795 scopus 로고    scopus 로고
    • The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors
    • Pagano A., Ruegg D., Litschig S., Stoehr N., Stierlin C., Heinrich M., et al. The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors. J Biol Chem 2000, 275(43):33750-33758.
    • (2000) J Biol Chem , vol.275 , Issue.43 , pp. 33750-33758
    • Pagano, A.1    Ruegg, D.2    Litschig, S.3    Stoehr, N.4    Stierlin, C.5    Heinrich, M.6
  • 7
    • 0033680311 scopus 로고    scopus 로고
    • Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents
    • Spooren W.P., Vassout A., Neijt H.C., Kuhn R., Gasparini F., Roux S., et al. Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents. J Pharmacol Exp Ther 2000, 295(3):1267-1275.
    • (2000) J Pharmacol Exp Ther , vol.295 , Issue.3 , pp. 1267-1275
    • Spooren, W.P.1    Vassout, A.2    Neijt, H.C.3    Kuhn, R.4    Gasparini, F.5    Roux, S.6
  • 8
    • 3042683441 scopus 로고    scopus 로고
    • Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling
    • Klodzinska A., Tatarczynska E., Chojnacka-Wojcik E., Nowak G., Cosford N.D., Pilc A. Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology 2004, 47(3):342-350.
    • (2004) Neuropharmacology , vol.47 , Issue.3 , pp. 342-350
    • Klodzinska, A.1    Tatarczynska, E.2    Chojnacka-Wojcik, E.3    Nowak, G.4    Cosford, N.D.5    Pilc, A.6
  • 9
    • 27144537834 scopus 로고    scopus 로고
    • Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity
    • Porter R.H., Jaeschke G., Spooren W., Ballard T.M., Buttelmann B., Kolczewski S., et al. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther 2005, 315(2):711-721.
    • (2005) J Pharmacol Exp Ther , vol.315 , Issue.2 , pp. 711-721
    • Porter, R.H.1    Jaeschke, G.2    Spooren, W.3    Ballard, T.M.4    Buttelmann, B.5    Kolczewski, S.6
  • 10
    • 0032078391 scopus 로고    scopus 로고
    • Expression of the human excitatory amino acid transporter 2 and metabotropic glutamate receptors 3 and 5 in the prefrontal cortex from normal individuals and patients with schizophrenia
    • Ohnuma T., Augood S.J., Arai H., McKenna P.J., Emson P.C. Expression of the human excitatory amino acid transporter 2 and metabotropic glutamate receptors 3 and 5 in the prefrontal cortex from normal individuals and patients with schizophrenia. Brain Res Mol Brain Res 1998, 56(1-2):207-217.
    • (1998) Brain Res Mol Brain Res , vol.56 , Issue.1-2 , pp. 207-217
    • Ohnuma, T.1    Augood, S.J.2    Arai, H.3    McKenna, P.J.4    Emson, P.C.5
  • 11
    • 0034451725 scopus 로고    scopus 로고
    • Distribution and roles of metabotropic glutamate receptors in the basal ganglia motor circuit: implications for treatment of Parkinson's disease and related disorders
    • Rouse S.T., Marino M.J., Bradley S.R., Awad H., Wittmann M., Conn P.J. Distribution and roles of metabotropic glutamate receptors in the basal ganglia motor circuit: implications for treatment of Parkinson's disease and related disorders. Pharmacol Ther 2000, 88(3):427-435.
    • (2000) Pharmacol Ther , vol.88 , Issue.3 , pp. 427-435
    • Rouse, S.T.1    Marino, M.J.2    Bradley, S.R.3    Awad, H.4    Wittmann, M.5    Conn, P.J.6
  • 12
    • 0036662945 scopus 로고    scopus 로고
    • Chronic but not acute treatment with a metabotropic glutamate 5 receptor antagonist reverses the akinetic deficits in a rat model of parkinsonism
    • Breysse N., Baunez C., Spooren W., Gasparini F., Amalric M. Chronic but not acute treatment with a metabotropic glutamate 5 receptor antagonist reverses the akinetic deficits in a rat model of parkinsonism. J Neurosci 2002, 22(13):5669-5678.
    • (2002) J Neurosci , vol.22 , Issue.13 , pp. 5669-5678
    • Breysse, N.1    Baunez, C.2    Spooren, W.3    Gasparini, F.4    Amalric, M.5
  • 13
    • 84876726646 scopus 로고    scopus 로고
    • Prolonged blockade of NMDA or mGluR5 glutamate receptors reduces nigrostriatal degeneration while inducing selective metabolic changes in the basal ganglia circuitry in a rodent model of Parkinson's disease
    • Armentero M.T., Fancellu R., Nappi G., Bramanti P., Blandini F. Prolonged blockade of NMDA or mGluR5 glutamate receptors reduces nigrostriatal degeneration while inducing selective metabolic changes in the basal ganglia circuitry in a rodent model of Parkinson's disease. Neurobiol Dis 2005.
    • (2005) Neurobiol Dis
    • Armentero, M.T.1    Fancellu, R.2    Nappi, G.3    Bramanti, P.4    Blandini, F.5
  • 14
    • 0034867765 scopus 로고    scopus 로고
    • Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice
    • Chiamulera C., Epping-Jordan M.P., Zocchi A., Marcon C., Cottiny C., Tacconi S., et al. Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice. Nat Neurosci 2001, 4(9):873-874.
    • (2001) Nat Neurosci , vol.4 , Issue.9 , pp. 873-874
    • Chiamulera, C.1    Epping-Jordan, M.P.2    Zocchi, A.3    Marcon, C.4    Cottiny, C.5    Tacconi, S.6
  • 15
    • 30344467530 scopus 로고    scopus 로고
    • Up-regulation of hippocampal metabotropic glutamate receptor 5 in temporal lobe epilepsy patients
    • Notenboom R.G., Hampson D.R., Jansen G.H., van Rijen P.C., van Veelen C.W., van Nieuwenhuizen O., et al. Up-regulation of hippocampal metabotropic glutamate receptor 5 in temporal lobe epilepsy patients. Brain 2006, 129(Pt 1):96-107.
    • (2006) Brain , vol.129 , Issue.PART 1 , pp. 96-107
    • Notenboom, R.G.1    Hampson, D.R.2    Jansen, G.H.3    van Rijen, P.C.4    van Veelen, C.W.5    van Nieuwenhuizen, O.6
  • 16
    • 0032853255 scopus 로고    scopus 로고
    • 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist
    • Gasparini F., Lingenhohl K., Stoehr N., Flor P.J., Heinrich M., Vranesic I., et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 1999, 38(10):1493-1503.
    • (1999) Neuropharmacology , vol.38 , Issue.10 , pp. 1493-1503
    • Gasparini, F.1    Lingenhohl, K.2    Stoehr, N.3    Flor, P.J.4    Heinrich, M.5    Vranesic, I.6
  • 17
    • 0037448394 scopus 로고    scopus 로고
    • 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity
    • Cosford N.D., Tehrani L., Roppe J., Schweiger E., Smith N.D., Anderson J., et al. 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J Med Chem 2003, 46(2):204-206.
    • (2003) J Med Chem , vol.46 , Issue.2 , pp. 204-206
    • Cosford, N.D.1    Tehrani, L.2    Roppe, J.3    Schweiger, E.4    Smith, N.D.5    Anderson, J.6
  • 19
    • 0036882079 scopus 로고    scopus 로고
    • 3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization
    • 3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther 2002, 303(3):1044-1051.
    • (2002) J Pharmacol Exp Ther , vol.303 , Issue.3 , pp. 1044-1051
    • Anderson, J.J.1    Rao, S.P.2    Rowe, B.3    Giracello, D.R.4    Holtz, G.5    Chapman, D.F.6
  • 21
    • 20844455452 scopus 로고    scopus 로고
    • Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers
    • Hamill T.G., Krause S., Ryan C., Bonnefous C., Govek S., Seiders T.J., et al. Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers. Synapse 2005, 56(4):205-216.
    • (2005) Synapse , vol.56 , Issue.4 , pp. 205-216
    • Hamill, T.G.1    Krause, S.2    Ryan, C.3    Bonnefous, C.4    Govek, S.5    Seiders, T.J.6
  • 22
    • 84867865129 scopus 로고    scopus 로고
    • Discovery and characterization of AZD9272 and AZD6538 - two novel mGluR5 negative allosteric modulators selected for clinical development
    • Raboisson P., Breitholtz-Emanuelsson A., Dahllöf H., Edwards L., Heaton W.L., Isaac M., et al. Discovery and characterization of AZD9272 and AZD6538 - two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett 2012, 22:6974-6979.
    • (2012) Bioorg Med Chem Lett , vol.22 , pp. 6974-6979
    • Raboisson, P.1    Breitholtz-Emanuelsson, A.2    Dahllöf, H.3    Edwards, L.4    Heaton, W.L.5    Isaac, M.6
  • 25
  • 26
    • 0002071621 scopus 로고    scopus 로고
    • Special report: the, guide for the care and use of laboratory animals
    • Clark J.D., Gebhart G.F., Gonder J.C., Keeling M.E., Kohn D.F. Special report: the, guide for the care and use of laboratory animals. ILAR J 1996, 38(1):41-48.
    • (1996) ILAR J , vol.38 , Issue.1 , pp. 41-48
    • Clark, J.D.1    Gebhart, G.F.2    Gonder, J.C.3    Keeling, M.E.4    Kohn, D.F.5
  • 31
    • 0002291141 scopus 로고
    • Radioligand disposition and metabolism - key information in early drug development
    • Klüwer Academic Publishers, Dordrecht, D. Comar (Ed.)
    • Halldin C., Swahn C., Farde L., Sedvall G. Radioligand disposition and metabolism - key information in early drug development. PET for drug development and evaluation 1995, 55-65. Klüwer Academic Publishers, Dordrecht. D. Comar (Ed.).
    • (1995) PET for drug development and evaluation , pp. 55-65
    • Halldin, C.1    Swahn, C.2    Farde, L.3    Sedvall, G.4


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