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Volumn 676, Issue 1-3, 2012, Pages 6-11

Characterization of [ 3H]Lu AE60157 ([ 3H]8-(4- methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5- hydroxytryptamine 6 (5-HT 6) receptors in vivo

Author keywords

5 HT 6 receptor; Brain; In vivo binding; Occupancy; Radioligand; Striatum

Indexed keywords

3 PHENYLSULFONYL 8 (1 PIPERAZINYL)QUINOLINE; 8 (4 METHYLPIPERAZIN 1 YL) 3 PHENYLSULFONYLQUINOLINE; CLOZAPINE; HALOPERIDOL; LU AE 60157; OLANZAPINE; QUETIAPINE; RISPERIDONE; SEROTONIN 6 ANTAGONIST; SEROTONIN 6 RECEPTOR; SERTINDOLE; TRITIUM; UNCLASSIFIED DRUG; VOLINANSERIN;

EID: 84855609329     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.11.029     Document Type: Article
Times cited : (9)

References (36)
  • 2
    • 0023521754 scopus 로고
    • 3H]GBR 12935 binding in vivo in mouse brain: Labelling of a piperazine acceptor site
    • DOI 10.1016/0014-2999(87)90002-1
    • P.H. Andersen, J.A. Jansen, and E.B. Nielsen [3H]GBR 12935 binding in vivo in mouse brain: labelling of a piperazine acceptor site Eur. J. Pharmacol. 144 1987 1 6 (Pubitemid 18013338)
    • (1987) European Journal of Pharmacology , vol.144 , Issue.1 , pp. 1-6
    • Andersen, P.H.1    Jansen, J.A.2    Nielsen, E.B.3
  • 3
    • 79951525244 scopus 로고    scopus 로고
    • 5-HT6 receptor ligands and their antipsychotic potential
    • J. Arnt, and C.K. Olsen 5-HT6 receptor ligands and their antipsychotic potential Int. Rev. Neurobiol. 96 2011 141 161
    • (2011) Int. Rev. Neurobiol. , vol.96 , pp. 141-161
    • Arnt, J.1    Olsen, C.K.2
  • 4
    • 0032007608 scopus 로고    scopus 로고
    • Do novel antipsychotics have similar pharmacologial characteristics? A review of the evidence
    • DOI 10.1016/S0893-133X(97)00112-7, PII S0893133X97001127
    • J. Arnt, and T. Skarsfeldt Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence Neuropsychopharmacology 18 1998 63 101 (Pubitemid 28026679)
    • (1998) Neuropsychopharmacology , vol.18 , Issue.2 , pp. 63-101
    • Arnt, J.1    Skarsfeldt, T.2
  • 7
    • 0031722106 scopus 로고    scopus 로고
    • 6 receptor
    • F.G. Boess, F.J. Monsma Jr., and A.J. Sleight Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor J. Neurochem. 71 1998 2169 2177 (Pubitemid 28491575)
    • (1998) Journal of Neurochemistry , vol.71 , Issue.5 , pp. 2169-2177
    • Boess, F.G.1    Monsma Jr., F.J.2    Sleight, A.J.3
  • 8
    • 0036707514 scopus 로고    scopus 로고
    • 125I]SB-258585
    • DOI 10.1002/syn.10097
    • S.Z. East, P.W. Burnet, R.A. Leslie, J.C. Roberts, and P.J. Harrison 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585 Synapse 45 2002 191 199 (Pubitemid 34827362)
    • (2002) Synapse , vol.45 , Issue.3 , pp. 191-199
    • East, S.Z.1    Burnet, P.W.J.2    Leslie, R.A.3    Roberts, J.C.4    Harrison, P.J.5
  • 9
    • 67651049001 scopus 로고    scopus 로고
    • The serotonin 5-HT6 receptor: A viable drug target for treating cognitive deficits in Alzheimer's disease
    • W.J. Geldenhuys, and C.J. Van der Schyf The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease Expert. Rev. Neurother. 9 2009 1073 1085
    • (2009) Expert. Rev. Neurother. , vol.9 , pp. 1073-1085
    • Geldenhuys, W.J.1    Van Der Schyf, C.J.2
  • 11
    • 0034672836 scopus 로고    scopus 로고
    • Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907
    • H. Hall, L. Farde, C. Halldin, C. Lundkvist, and G. Sedvall Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907 Synapse 38 2000 421 431
    • (2000) Synapse , vol.38 , pp. 421-431
    • Hall, H.1    Farde, L.2    Halldin, C.3    Lundkvist, C.4    Sedvall, G.5
  • 12
    • 0347824360 scopus 로고    scopus 로고
    • Differences in the Central Nervous System Distribution and Pharmacology of the Mouse 5-Hydroxytryptamine-6 Receptor Compared with Rat and Human Receptors Investigated by Radioligand Binding, Site-Directed Mutagenesis, and Molecular Modeling
    • DOI 10.1124/mol.64.6.1295
    • W.D. Hirst, B. Abrahamsen, F.E. Blaney, A.R. Calver, L. Aloj, G.W. Price, and A.D. Medhurst Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling Mol. Pharmacol. 64 2003 1295 1308 (Pubitemid 37532219)
    • (2003) Molecular Pharmacology , vol.64 , Issue.6 , pp. 1295-1308
    • Hirst, W.D.1    Abrahamsen, B.2    Blaney, F.E.3    Calver, A.R.4    Aloj, L.5    Price, G.W.6    Medhurst, A.D.7
  • 15
    • 72649104250 scopus 로고    scopus 로고
    • Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: Involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms
    • N. Idris, J. Neill, B. Grayson, B. Bang-Andersen, L.M. Witten, L.T. Brennum, and J. Arnt Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms Psychopharmacology (Berl) 208 2010 23 36
    • (2010) Psychopharmacology (Berl) , vol.208 , pp. 23-36
    • Idris, N.1    Neill, J.2    Grayson, B.3    Bang-Andersen, B.4    Witten, L.M.5    Brennum, L.T.6    Arnt, J.7
  • 16
    • 0037405871 scopus 로고    scopus 로고
    • Antipsychotic dosing in preclinical models is often unrepresentative of the clinical condition: A suggested solution based on in vivo occupancy
    • DOI 10.1124/jpet.102.046987
    • S. Kapur, S.C. VanderSpek, B.A. Brownlee, and J.N. Nobrega Antipsychotic dosing in preclinical models is often unrepresentative of the clinical condition: a suggested solution based on in vivo occupancy J. Pharmacol. Exp. Ther. 305 2003 625 631 (Pubitemid 36459179)
    • (2003) Journal of Pharmacology and Experimental Therapeutics , vol.305 , Issue.2 , pp. 625-631
    • Kapur, S.1    Vanderspek, S.C.2    Brownlee, B.A.3    Nobrega, J.N.4
  • 18
    • 0035919145 scopus 로고    scopus 로고
    • 6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop
    • DOI 10.1016/S0169-328X(01)00090-0, PII S0169328X01000900
    • R. Kohen, L.A. Fashingbauer, D.E. Heidmann, C.R. Guthrie, and M.W. Hamblin Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop Brain Res. Mol. Brain Res. 90 2001 110 117 (Pubitemid 32537632)
    • (2001) Molecular Brain Research , vol.90 , Issue.2 , pp. 110-117
    • Kohen, R.1    Fashingbauer, L.A.2    Heidmann, D.E.A.3    Guthrie, C.R.4    Hamblin, M.W.5
  • 19
    • 77957903115 scopus 로고    scopus 로고
    • Exploring the neuroleptic substituent in octoclothepin: Potential ligands for positron emission tomography with subnanomolar affinity for alpha(1)-adrenoceptors
    • J.L. Kristensen, A. Puschl, M. Jensen, R. Risgaard, C.T. Christoffersen, B. Bang-Andersen, and T. Balle Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for alpha(1)-adrenoceptors J. Med. Chem. 53 2010 7021 7034
    • (2010) J. Med. Chem. , vol.53 , pp. 7021-7034
    • Kristensen, J.L.1    Puschl, A.2    Jensen, M.3    Risgaard, R.4    Christoffersen, C.T.5    Bang-Andersen, B.6    Balle, T.7
  • 20
    • 0001962034 scopus 로고    scopus 로고
    • Receptor profile of antipsychotics
    • B.A. Ellenbroek, A.R. Cools, Birkhäuser Verlag Basel
    • J.E. Leysen Receptor profile of antipsychotics B.A. Ellenbroek, A.R. Cools, Atypical Antipsychotics 2000 Birkhäuser Verlag Basel 57 81
    • (2000) Atypical Antipsychotics , pp. 57-81
    • Leysen, J.E.1
  • 22
    • 28044437798 scopus 로고    scopus 로고
    • 6 receptors: A novel target for cognitive enhancement
    • DOI 10.1016/j.pharmthera.2005.05.001, PII S0163725805000975
    • E.S. Mitchell, and J.F. Neumaier 5-HT6 receptors: a novel target for cognitive enhancement Pharmacol. Ther. 108 2005 320 333 (Pubitemid 41691871)
    • (2005) Pharmacology and Therapeutics , vol.108 , Issue.3 , pp. 320-333
    • Mitchell, E.S.1    Neumaier, J.F.2
  • 23
    • 70449467081 scopus 로고    scopus 로고
    • Adaptations in 5-HT receptor expression and function: Implications for treatment of cognitive impairment in aging
    • E.S. Mitchell, R.A. McDevitt, and J.F. Neumaier Adaptations in 5-HT receptor expression and function: implications for treatment of cognitive impairment in aging J. Neurosci. Res. 87 2009 2803 2811
    • (2009) J. Neurosci. Res. , vol.87 , pp. 2803-2811
    • Mitchell, E.S.1    McDevitt, R.A.2    Neumaier, J.F.3
  • 24
    • 0027481384 scopus 로고
    • Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs
    • F.J. Monsma Jr., Y. Shen, R.P. Ward, M.W. Hamblin, and D.R. Sibley Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs Mol. Pharmacol. 43 1993 320 327 (Pubitemid 23081986)
    • (1993) Molecular Pharmacology , vol.43 , Issue.3 , pp. 320-327
    • Monsma Jr., F.J.1    Shen, Y.2    Ward, R.P.3    Hamblin, M.W.4    Sibley, D.R.5
  • 25
    • 0036119234 scopus 로고    scopus 로고
    • 6 receptor antagonist, SB-271046, in animal models for schizophrenia
    • DOI 10.1016/S0091-3057(01)00743-2, PII S0091305701007432
    • B. Pouzet, M. Didriksen, and J. Arnt Effects of the 5-HT(6) receptor antagonist, SB-271046, in animal models for schizophrenia Pharmacol. Biochem. Behav. 71 2002 635 643 (Pubitemid 34219214)
    • (2002) Pharmacology Biochemistry and Behavior , vol.71 , Issue.4 , pp. 635-643
    • Pouzet, B.1    Didriksen, M.2    Arnt, J.3
  • 27
    • 0037177441 scopus 로고    scopus 로고
    • 125I]SB-258585
    • DOI 10.1016/S0006-8993(02)02360-0, PII S0006899302023600
    • J.C. Roberts, C. Reavill, S.Z. East, P.J. Harrison, S. Patel, C. Routledge, and R.A. Leslie The distribution of 5-HT(6) receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT(6) receptor antagonist [(125)I]SB-258585 Brain Res. 934 2002 49 57 (Pubitemid 34286567)
    • (2002) Brain Research , vol.934 , Issue.1 , pp. 49-57
    • Roberts, J.C.1    Reavill, C.2    East, S.Z.3    Harrison, P.J.4    Patel, S.5    Routledge, C.6    Leslie, R.A.7
  • 28
    • 51749091526 scopus 로고    scopus 로고
    • Reversal of subchronic PCP-induced deficits in attentional set shifting in rats by sertindole and a 5-HT(6) receptor antagonist: Comparison among antipsychotics
    • J.S. Rodefer, T.N. Nguyen, J.J. Karlsson, and J. Arnt Reversal of subchronic PCP-induced deficits in attentional set shifting in rats by sertindole and a 5-HT(6) receptor antagonist: comparison among antipsychotics Neuropsychopharmacology 33 2008 2657 2666
    • (2008) Neuropsychopharmacology , vol.33 , pp. 2657-2666
    • Rodefer, J.S.1    Nguyen, T.N.2    Karlsson, J.J.3    Arnt, J.4
  • 32
    • 0022186670 scopus 로고
    • Measurement of protein using bicinchoninic acid
    • DOI 10.1016/0003-2697(85)90442-7
    • P.K. Smith, R.I. Krohn, G.T. Hermanson, A.K. Mallia, F.H. Gartner, M.D. Provenzano, E.K. Fujimoto, N.M. Goeke, B.J. Olson, and D.C. Klenk Measurement of protein using bicinchoninic acid Anal. Biochem. 150 1985 76 85 (Pubitemid 16258399)
    • (1985) Analytical Biochemistry , vol.150 , Issue.1 , pp. 76-85
    • Smith, P.K.1    Krohn, R.I.2    Hermanson, G.T.3
  • 33
    • 46749118971 scopus 로고    scopus 로고
    • 6 Receptor Antagonists as Novel Cognitive Enhancing Agents for Alzheimer's Disease
    • DOI 10.1016/j.nurt.2008.05.008, PII S1933721308001001
    • N. Upton, T.T. Chuang, A.J. Hunter, and D.J. Virley 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease Neurotherapeutics 5 2008 458 469 (Pubitemid 351952494)
    • (2008) Neurotherapeutics , vol.5 , Issue.3 , pp. 458-469
    • Upton, N.1    Chuang, T.T.2    Hunter, A.J.3    Virley, D.J.4
  • 34
    • 0028896011 scopus 로고
    • Localization of serotonin subtype 6 receptor messenger RNA in the rat brain by in situ hybridization histochemistry
    • R.P. Ward, M.W. Hamblin, J.E. Lachowicz, B.J. Hoffman, D.R. Sibley, and D.M. Dorsa Localization of serotonin subtype 6 receptor messenger RNA in the rat brain by in situ hybridization histochemistry Neuroscience 64 1995 1105 1111
    • (1995) Neuroscience , vol.64 , pp. 1105-1111
    • Ward, R.P.1    Hamblin, M.W.2    Lachowicz, J.E.3    Hoffman, B.J.4    Sibley, D.R.5    Dorsa, D.M.6
  • 36
    • 0032967875 scopus 로고    scopus 로고
    • 3, 5HT(2A) and muscarinic receptors
    • DOI 10.1007/s002130050834
    • W. Zhang, and F.P. Bymaster The in vivo effects of olanzapine and other antipsychotic agents on receptor occupancy and antagonism of dopamine D1, D2, D3, 5HT2A and muscarinic receptors Psychopharmacology (Berl) 141 1999 267 278 (Pubitemid 29196076)
    • (1999) Psychopharmacology , vol.141 , Issue.3 , pp. 267-278
    • Zhang, W.1    Bymaster, F.P.2


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