메뉴 건너뛰기




Volumn 53, Issue 6, 2012, Pages 969-976

Radiosynthesis and preclinical evaluation of 18F-F13714 as a fluorinated 5-HT 1A receptor agonist radioligand for PET neuroimaging

Author keywords

Agonist; Cat; PET; Rat; Serotonin 1A receptor

Indexed keywords

DRUG METABOLITE; F 13714 F 18; SEROTONIN 1A RECEPTOR; TRACER; UNCLASSIFIED DRUG;

EID: 84861880589     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.111.101212     Document Type: Article
Times cited : (24)

References (40)
  • 1
    • 0036119338 scopus 로고    scopus 로고
    • Molecular, pharmacological and functional diversity of 5-HT receptors
    • DOI 10.1016/S0091-3057(01)00746-8, PII S0091305701007468
    • Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav. 2002;71:533-554. (Pubitemid 34219205)
    • (2002) Pharmacology Biochemistry and Behavior , vol.71 , Issue.4 , pp. 533-554
    • Hoyer, D.1    Hannon, J.P.2    Martin, G.R.3
  • 3
    • 0035145554 scopus 로고    scopus 로고
    • 1A) receptors in the central nervous system
    • DOI 10.1007/s002590000394
    • Passchier J, van Waarde A. Visualisation of serotonin-1A (5-HT1A) receptors in the central nervous system. Eur J Nucl Med. 2001;28:113-129. (Pubitemid 32120814)
    • (2001) European Journal of Nuclear Medicine , vol.28 , Issue.1 , pp. 113-129
    • Passchier, J.1    Van Waarde, A.2
  • 4
    • 0035226193 scopus 로고    scopus 로고
    • Radioligands for the study of brain 5-HT1A receptors in vivo
    • Pike VW, Halldin C, Wikstrom HV. Radioligands for the study of brain 5-HT1A receptors in vivo. Prog Med Chem. 2001;38:189-247.
    • (2001) Prog Med Chem , vol.38 , pp. 189-247
    • Pike, V.W.1    Halldin, C.2    Wikstrom, H.V.3
  • 5
    • 33846889762 scopus 로고    scopus 로고
    • 18F]MPPF as a tool for the in vivo imaging of 5-HT1A receptors in animal and human brain
    • 18F]MPPF as a tool for the in vivo imaging of 5-HT1A receptors in animal and human brain. Neuropharmacology. 2007;52:695-707.
    • (2007) Neuropharmacology , vol.52 , pp. 695-707
    • Aznavour, N.1    Zimmer, L.2
  • 6
    • 34548413531 scopus 로고    scopus 로고
    • 1A receptors and uses thereof
    • DOI 10.1016/j.drudis.2007.07.008, PII S1359644607002747
    • Kumar JS, Mann JJ. PET tracers for 5-HT(1A) receptors and uses thereof. Drug Discov Today. 2007;12:748-756. (Pubitemid 47364834)
    • (2007) Drug Discovery Today , vol.12 , Issue.17-18 , pp. 748-756
    • Kumar, J.S.D.1    Mann, J.J.2
  • 7
    • 0025070043 scopus 로고
    • Physical evidence of the coupling of solubilized 5-HT(1A) binding sites with G regulatory proteins
    • DOI 10.1016/0006-2952(90)90642-X
    • Emerit MB, el Mestikawy S, Gozlan H, Rouot B, Hamon M. Physical evidence of the coupling of solubilized 5-HT1A binding sites with G regulatory proteins. Biochem Pharmacol. 1990;39:7-18. (Pubitemid 20027964)
    • (1990) Biochemical Pharmacology , vol.39 , Issue.1 , pp. 7-18
    • Emerit, M.B.1    El, M.S.2    Gozlan, H.3    Rouot, B.4    Hamon, M.5
  • 8
    • 0026551650 scopus 로고
    • Adrenergic receptors as models for G protein-coupled receptors
    • Kobilka B. Adrenergic receptors as models for G protein-coupled receptors. Annu Rev Neurosci. 1992;15:87-114.
    • (1992) Annu Rev Neurosci , vol.15 , pp. 87-114
    • Kobilka, B.1
  • 9
    • 0021892571 scopus 로고
    • 3H]8-hydroxy-2-(di-n-propylamino)tetralin binding to pre- And postsynaptic 5-hydroxytryptamine sites in various regions of the rat brain
    • 3H]8-hydroxy-2-(di-n-propylamino)tetralin binding to pre- and postsynaptic 5-hydroxytryptamine sites in various regions of the rat brain. J Neurochem. 1985;44:1685-1696.
    • (1985) J Neurochem , vol.44 , pp. 1685-1696
    • Hall, M.D.1    El Mestikawy, S.2    Emerit, M.B.3    Pichat, L.4    Hamon, M.5    Gozlan, H.6
  • 10
    • 0026662897 scopus 로고
    • Further evidence for differential affinity states of the serotonin1A receptor in rat hippocampus
    • Mongeau R, Welner SA, Quirion R, Suranyi-Cadotte BE. Further evidence for differential affinity states of the serotonin1A receptor in rat hippocampus. Brain Res. 1992;590:229-238.
    • (1992) Brain Res , vol.590 , pp. 229-238
    • Mongeau, R.1    Welner, S.A.2    Quirion, R.3    Suranyi-Cadotte, B.E.4
  • 11
    • 0028273228 scopus 로고
    • 3H] hydroxydipropylaminotetralin
    • Nénonéné EK, Radja F, Carli M, Grondin L, Reader TA. Heterogeneity of cortical and hippocampal 5-HT1A receptors: a reappraisal of homogenate binding with 8-[3H]hydroxydipropylaminotetralin. J Neurochem. 1994;62:1822-1834. (Pubitemid 24121875)
    • (1994) Journal of Neurochemistry , vol.62 , Issue.5 , pp. 1822-1834
    • Nenonene, E.K.1    Radja, F.2    Carli, M.3    Grondin, L.4    Reader, T.A.5
  • 12
    • 33645105867 scopus 로고    scopus 로고
    • A comparison of in vivo and in vitro neuroimaging of 5-HT 1A receptor binding sites in the cat brain
    • Aznavour N, Rbah L, Leger L, et al. A comparison of in vivo and in vitro neuroimaging of 5-HT 1A receptor binding sites in the cat brain. J Chem Neuroanat. 2006;31:226-232.
    • (2006) J Chem Neuroanat , vol.31 , pp. 226-232
    • Aznavour, N.1    Rbah, L.2    Leger, L.3
  • 13
    • 77957718322 scopus 로고    scopus 로고
    • Measuring endogenous 5-HT release by emission tomography: Promises and pitfalls
    • Paterson LM, Tyacke RJ, Nutt DJ, Knudsen GM. Measuring endogenous 5-HT release by emission tomography: promises and pitfalls. J Cereb Blood Flow Metab. 2010;30:1682-1706.
    • (2010) J Cereb Blood Flow Metab , vol.30 , pp. 1682-1706
    • Paterson, L.M.1    Tyacke, R.J.2    Nutt, D.J.3    Knudsen, G.M.4
  • 15
    • 0037822883 scopus 로고    scopus 로고
    • Synthesis and evaluation of 5HT1A agonists as radioligands: Failure of G protein-coupled receptor agonists as in vivo imaging agents
    • Mathis C, Huang Y, Simpson N. Synthesis and evaluation of 5HT1A agonists as radioligands: failure of G protein-coupled receptor agonists as in vivo imaging agents. J Labelled Comp Radiopharm. 1997;40(suppl):563-564.
    • (1997) J Labelled Comp Radiopharm , vol.40 , Issue.SUPPL. , pp. 563-564
    • Mathis, C.1    Huang, Y.2    Simpson, N.3
  • 17
    • 0036701656 scopus 로고    scopus 로고
    • 11C-labeled (S)-N-[[1-(2- phenylethyl) pyrrolidin-2-yl]methyl]-3-methylthiobenzamide as a PET 5-HT(1A) receptor ligand
    • 11C-labeled (S)-N-[[1-(2-phenylethyl) pyrrolidin-2-yl]methyl]-3- methylthiobenzamide as a PET 5-HT(1A) receptor ligand. Nucl Med Biol. 2002;29:657-663.
    • (2002) Nucl Med Biol , vol.29 , pp. 657-663
    • Fujio, M.1    Nagata, S.2    Kawamura, K.3
  • 18
    • 0025914512 scopus 로고
    • Serotoninergic measures in suicide brain: 5-HT1A binding sites in frontal cortex of suicide victims
    • Matsubara S, Arora RC, Meltzer HY. Serotoninergic measures in suicide brain: 5-HT1A binding sites in frontal cortex of suicide victims. J Neural Transm. 1991;85:181-194.
    • (1991) J Neural Transm , vol.85 , pp. 181-194
    • Matsubara, S.1    Arora, R.C.2    Meltzer, H.Y.3
  • 19
    • 34250314127 scopus 로고    scopus 로고
    • 11C]2-(4-(4-(2-methoxyphenyl) piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine -3,5(2H,4H)dione in nonhuman primates
    • 11C]2-(4- (4-(2-methoxyphenyl) piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine -3,5(2H,4H)dione in nonhuman primates. Eur J Nucl Med Mol Imaging. 2007;34:1050-1060.
    • (2007) Eur J Nucl Med Mol Imaging , vol.34 , pp. 1050-1060
    • Kumar, J.S.1    Prabhakaran, J.2    Majo, V.J.3
  • 20
    • 77954333234 scopus 로고    scopus 로고
    • Evaluation of [C]S14506 and [F]S14506 in rat and monkey as agonist PET radioligands for brain 5-HT (1A) receptors
    • Lu S, Liow JS, Zoghbi SS, Hong J, Innis RB, Pike VW. Evaluation of [C]S14506 and [F]S14506 in rat and monkey as agonist PET radioligands for brain 5-HT (1A) receptors. Curr Radiopharm. 2010;3:9-18.
    • (2010) Curr Radiopharm , vol.3 , pp. 9-18
    • Lu, S.1    Liow, J.S.2    Zoghbi, S.S.3    Hong, J.4    Innis, R.B.5    Pike, V.W.6
  • 21
    • 0038771222 scopus 로고    scopus 로고
    • 11C]methoxyphenyl) piperazin-1-yl]-2-hydroxypropyl]oxy]thioch roman, a presynaptic 5-HT(1A) receptor agonist, and its in vivo evaluation in anaesthetised rat and in awake cat
    • 11C]methoxyphenyl)piperazin-1-yl]-2- hydroxypropyl]oxy]thioch roman, a presynaptic 5-HT(1A) receptor agonist, and its in vivo evaluation in anaesthetised rat and in awake cat. Nucl Med Biol. 2003;30:541-546.
    • (2003) Nucl Med Biol , vol.30 , pp. 541-546
    • Zimmer, L.1    Fournet, G.2    Benoit, J.3    Guillaumet, G.4    Le Bars, D.5
  • 22
    • 42049095298 scopus 로고    scopus 로고
    • 11C-CUMI-101, an agonist radiotracer for imaging serotonin 1A receptor in vivo with PET
    • 11C-CUMI-101, an agonist radiotracer for imaging serotonin 1A receptor in vivo with PET. J Nucl Med. 2008;49:587-596.
    • (2008) J Nucl Med , vol.49 , pp. 587-596
    • Milak, M.S.1    Severance, A.J.2    Ogden, R.T.3
  • 24
  • 25
    • 30444454518 scopus 로고    scopus 로고
    • 11C]2-{4-[4-(7- methoxynaphthalen-1-yl)piperazin-1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3, 5-dione: A novel 5-HT1A receptor agonist positron emission tomography ligand
    • 11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]butyl} -4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. J Med Chem. 2006;49:125-134.
    • (2006) J Med Chem , vol.49 , pp. 125-134
    • Kumar, J.S.1    Majo, V.J.2    Hsiung, S.C.3
  • 26
    • 79551684778 scopus 로고    scopus 로고
    • In vitro assessment of the agonist properties of the novel 5-HT1A receptor ligand, CUMI-101 (MMP), in rat brain tissue
    • Hendry N, Christie I, Rabiner EA, Laruelle M, Watson J. In vitro assessment of the agonist properties of the novel 5-HT1A receptor ligand, CUMI-101 (MMP), in rat brain tissue. Nucl Med Biol. 2011;38:273-277.
    • (2011) Nucl Med Biol , vol.38 , pp. 273-277
    • Hendry, N.1    Christie, I.2    Rabiner, E.A.3    Laruelle, M.4    Watson, J.5
  • 30
    • 33748493597 scopus 로고    scopus 로고
    • 1A agonist, F13714: A microdialysis study in the rat
    • DOI 10.1038/sj.bjp.0706859, PII 0706859
    • Assié MB, Lomenech H, Ravailhe V, Faucillon V, Newman-Tancredi A. Rapid desensitization of somatodendritic 5-HT1A receptors by chronic administration of the high-efficacy 5-HT1A agonist, F13714: a microdialysis study in the rat. Br J Pharmacol. 2006;149:170-178. (Pubitemid 44360098)
    • (2006) British Journal of Pharmacology , vol.149 , Issue.2 , pp. 170-178
    • Assie, M.-B.1    Lomenech, H.2    Ravailhe, V.3    Faucillon, V.4    Newman-Tancredi, A.5
  • 33
    • 77957921579 scopus 로고    scopus 로고
    • Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists
    • Bollinger S, Hubner H, Heinemann FW, Meyer K, Gmeiner P. Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. J Med Chem. 2010;53:7167-7179.
    • (2010) J Med Chem , vol.53 , pp. 7167-7179
    • Bollinger, S.1    Hubner, H.2    Heinemann, F.W.3    Meyer, K.4    Gmeiner, P.5
  • 34
    • 77949261526 scopus 로고    scopus 로고
    • 18F]F15599, a novel 5-HT1A receptor agonist, as a radioligand for PET neuroimaging
    • 18F]F15599, a novel 5-HT1A receptor agonist, as a radioligand for PET neuroimaging. Eur J Nucl Med Mol Imaging. 2010;37:594-605.
    • (2010) Eur J Nucl Med Mol Imaging , vol.37 , pp. 594-605
    • Lemoine, L.1    Verdurand, M.2    Vacher, B.3
  • 35
    • 0344983883 scopus 로고    scopus 로고
    • Relationships between radiotracer properties and image quality in molecular imaging of the brain with positron emission tomography
    • DOI 10.1016/j.mibio.2003.09.009, PII S1536163203001677
    • Laruelle M, Slifstein M, Huang Y. Relationships between radiotracer properties and image quality in molecular imaging of the brain with positron emission tomography. Mol Imaging Biol. 2003;5:363-375. (Pubitemid 37489827)
    • (2003) Molecular Imaging and Biology , vol.5 , Issue.6 , pp. 363-375
    • Laruelle, M.1    Slifstein, M.2    Huang, Y.3
  • 38
    • 33747593745 scopus 로고    scopus 로고
    • Regional differences in the coupling of 5-hydroxytryptamine-1A receptors to G proteins in the rat brain
    • DOI 10.1124/mol.106.022756
    • Mannoury la Cour C, El Mestikawy S, Hanoun N, Hamon M, Lanfumey L. Regional differences in the coupling of 5-hydroxytryptamine-1A receptors to G proteins in the rat brain. Mol Pharmacol. 2006;70:1013-1021. (Pubitemid 44268458)
    • (2006) Molecular Pharmacology , vol.70 , Issue.3 , pp. 1013-1021
    • Mannoury, L.C.C.1    El, M.S.2    Hanoun, N.3    Hamon, M.4    Lanfumey, L.5
  • 39
    • 67650222044 scopus 로고    scopus 로고
    • Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist
    • Newman-Tancredi A, Martel JC, Assie MB, et al. Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist. Br J Pharmacol. 2009;156:338-353.
    • (2009) Br J Pharmacol , vol.156 , pp. 338-353
    • Newman-Tancredi, A.1    Martel, J.C.2    Assie, M.B.3
  • 40
    • 0028926033 scopus 로고
    • 3H] WAY-100635, a selective 5-HT1A receptor antagonist
    • 3H] WAY-100635, a selective 5-HT1A receptor antagonist. Brain Res. 1995;673:217-225.
    • (1995) Brain Res , vol.673 , pp. 217-225
    • Khawaja, X.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.