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Volumn 321, Issue 3, 2007, Pages 1032-1045

GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models

(38)  Medhurst, Andrew D a   Atkins, Alan R a   Beresford, Isabel J a   Brackenborough, Kim a   Briggs, Michael A a   Calver, Andrew R a   Cilia, Jackie a   Cluderay, Jane E a   Crook, Barry a   Davis, John B a   Davis, Rebecca K a   Davis, Robert P a   Dawson, Lee A a   Foley, Andrew G c   Gartlon, Jane a   Gonzalez, M Isabel a   Heslop, Teresa a   Hirst, Warren D a   Jennings, Carol a   Jones, Declan N C a   more..


Author keywords

[No Author keywords available]

Indexed keywords

5 (4 CYANOPHENYL) 2 [2 (2 METHYL 1 IMIDAZOLIDINYL)ETHYL]BENZOFURAN; 6 [(3 CYCLOBUTYL 2,3,4,5 TETRAHYDRO 1H 3 BENZAZEPIN 7 YL)OXY] N METHYL 3 PYRIDINECARBOXAMIDE; ACETYLCHOLINE; ALPHA METHYL[IMIDAZOLE 2,5(N) HISTAMINE; ALPHA METHYLHISTAMINE; CIPROXIFAN; CLOBENPROPIT; DOPAMINE; GSK 189254; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; MEPYRAMINE; NORADRENALIN; PROTEIN C FOS; THIOPERAMIDE; UNCLASSIFIED DRUG; ZOLANTIDINE; 6 ((3 CYCLOBUTYL 2,3,4,5 TETRAHYDRO 1H 3 BENZAZEPIN 7 YL)OXY) N METHYL 3 PYRIDINECARBOXAMIDE; 6-((3-CYCLOBUTYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPIN-7-YL)OXY)-N-METHYL-3-PYRIDINECARBOXAMIDE; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; ANTIHISTAMINIC AGENT; BENZAZEPINE DERIVATIVE; DRUG DERIVATIVE; HISTAMINE AGONIST; NICOTINAMIDE; NOOTROPIC AGENT;

EID: 34248562939     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.107.120311     Document Type: Article
Times cited : (290)

References (42)
  • 1
    • 0034879048 scopus 로고    scopus 로고
    • Distribution and modulation of histamine H(3) receptors in basal ganglia and frontal cortex of healthy controls and patients with Parkinson's disease
    • Anichtchik OV, Peitsaro N, Rinne JO, Kalimo H, and Panula P (2001) Distribution and modulation of histamine H(3) receptors in basal ganglia and frontal cortex of healthy controls and patients with Parkinson's disease. Neurobiol Dis 8:707-716.
    • (2001) Neurobiol Dis , vol.8 , pp. 707-716
    • Anichtchik, O.V.1    Peitsaro, N.2    Rinne, J.O.3    Kalimo, H.4    Panula, P.5
  • 2
    • 0020587209 scopus 로고
    • Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor
    • Arrang JM, Garbarg M, and Schwartz JC (1983) Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature (Lond) 302:832-837.
    • (1983) Nature (Lond) , vol.302 , pp. 832-837
    • Arrang, J.M.1    Garbarg, M.2    Schwartz, J.C.3
  • 3
    • 34248528678 scopus 로고    scopus 로고
    • Bamford MJ, Dean DK, Sehmi SS, Wilson DM, and Witherington J (2004) inventors; Glaxo Group Limited, assignees. Benzodiazepine derivatives for the treatment of neurological disorders. World patent WO 2004/056369 A1. 2004 Jul 8
    • Bamford MJ, Dean DK, Sehmi SS, Wilson DM, and Witherington J (2004) inventors; Glaxo Group Limited, assignees. Benzodiazepine derivatives for the treatment of neurological disorders. World patent WO 2004/056369 A1. 2004 Jul 8.
  • 7
    • 29144437722 scopus 로고    scopus 로고
    • Keynote review: Histamine H3 receptor antagonists reach out for the clinic
    • Celanire S, Wijtmans M, Talaga P, Leurs R, and de Esch IJ (2005) Keynote review: histamine H3 receptor antagonists reach out for the clinic. Drug Discov Today 10:1613-1627.
    • (2005) Drug Discov Today , vol.10 , pp. 1613-1627
    • Celanire, S.1    Wijtmans, M.2    Talaga, P.3    Leurs, R.4    de Esch, I.J.5
  • 8
    • 0037466442 scopus 로고    scopus 로고
    • Molecular and pharmacological characterization of the mouse histamine H3 receptor
    • Chen J, Liu C, and Lovenberg TW (2003) Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol 467:57-65.
    • (2003) Eur J Pharmacol , vol.467 , pp. 57-65
    • Chen, J.1    Liu, C.2    Lovenberg, T.W.3
  • 9
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
    • Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
    • (1973) Biochem Pharmacol , vol.22 , pp. 3099-3108
    • Cheng, Y.1    Prusoff, W.H.2
  • 10
    • 0027340047 scopus 로고
    • Histamine H3 receptor-mediated modulation of water consumption in the rat
    • Clapham J and Kilpatrick GJ (1993) Histamine H3 receptor-mediated modulation of water consumption in the rat. Eur J Pharmacol 232:99-103.
    • (1993) Eur J Pharmacol , vol.232 , pp. 99-103
    • Clapham, J.1    Kilpatrick, G.J.2
  • 11
    • 0033524384 scopus 로고    scopus 로고
    • Transient and stable gene expression in mammalian cells transduced with a recombinant baculovirus vector
    • Condreay JP, Witherspoon SM, Clay WC, and Kost TA (1999) Transient and stable gene expression in mammalian cells transduced with a recombinant baculovirus vector. Proc Natl Acad Sci USA 96:127-132.
    • (1999) Proc Natl Acad Sci USA , vol.96 , pp. 127-132
    • Condreay, J.P.1    Witherspoon, S.M.2    Clay, W.C.3    Kost, T.A.4
  • 12
    • 0036990186 scopus 로고    scopus 로고
    • The ABC of Alzheimer's disease: Cognitive changes and their management in Alzheimer's disease and related dementias
    • Corey-Bloom J (2002) The ABC of Alzheimer's disease: cognitive changes and their management in Alzheimer's disease and related dementias. Int Psychogeriatr 14 (Suppl 1):51-75.
    • (2002) Int Psychogeriatr , vol.14 , Issue.SUPPL. 1 , pp. 51-75
    • Corey-Bloom, J.1
  • 13
    • 0023691166 scopus 로고
    • A new one-trial test for neurobiological studies of memory in rats. 1: Behavioral data
    • Ennaceur A and Delacour J (1988) A new one-trial test for neurobiological studies of memory in rats. 1: Behavioral data. Behav Brain Res 31:47-59.
    • (1988) Behav Brain Res , vol.31 , pp. 47-59
    • Ennaceur, A.1    Delacour, J.2
  • 14
    • 20144376337 scopus 로고    scopus 로고
    • Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, et al. (2005) Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile] : I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J Pharmacol Exp Ther 313:165-175.
    • Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, et al. (2005) Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile] : I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J Pharmacol Exp Ther 313:165-175.
  • 16
    • 0346057791 scopus 로고    scopus 로고
    • The 5-HT(6) receptor antagonist SB-271046 reverses scopolamine-disrupted consolidation of a passive avoidance task and ameliorates spatial task deficits in aged rats
    • Foley AG, Murphy KJ, Hirst WD, Gallagher HC, Hagan JJ, Upton N, Walsh FS, and Regan CM (2004) The 5-HT(6) receptor antagonist SB-271046 reverses scopolamine-disrupted consolidation of a passive avoidance task and ameliorates spatial task deficits in aged rats. Neuropsychopharmacology 29:93-100.
    • (2004) Neuropsychopharmacology , vol.29 , pp. 93-100
    • Foley, A.G.1    Murphy, K.J.2    Hirst, W.D.3    Gallagher, H.C.4    Hagan, J.J.5    Upton, N.6    Walsh, F.S.7    Regan, C.M.8
  • 17
    • 20144386364 scopus 로고    scopus 로고
    • Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, et al. (2005) Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl) benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J Pharmacol Exp Ther 313:176-190.
    • Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, et al. (2005) Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl) benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J Pharmacol Exp Ther 313:176-190.
  • 20
    • 5444268112 scopus 로고    scopus 로고
    • Perspectives on cognitive domains, H3 receptor ligands and neurological disease
    • Hancock AA and Fox GB (2004) Perspectives on cognitive domains, H3 receptor ligands and neurological disease. Expert Opin Investig Drugs 13:1237-1248.
    • (2004) Expert Opin Investig Drugs , vol.13 , pp. 1237-1248
    • Hancock, A.A.1    Fox, G.B.2
  • 22
    • 3142668938 scopus 로고    scopus 로고
    • Cognitive correlates of Abeta deposition in male and female mice bearing amyloid precursor protein and presenilin-1 mutant transgenes
    • Howlett DR, Richardson JC, Austin A, Parsons AA, Bate ST, Davies DC, and Gonzalez MI (2004) Cognitive correlates of Abeta deposition in male and female mice bearing amyloid precursor protein and presenilin-1 mutant transgenes. Brain Res 1017:130-136.
    • (2004) Brain Res , vol.1017 , pp. 130-136
    • Howlett, D.R.1    Richardson, J.C.2    Austin, A.3    Parsons, A.A.4    Bate, S.T.5    Davies, D.C.6    Gonzalez, M.I.7
  • 23
    • 1542344509 scopus 로고    scopus 로고
    • Differential autoreceptor control of extracellular 5-HT in guinea pig and rat: Species and regional differences
    • Hughes ZA and Dawson LA (2004) Differential autoreceptor control of extracellular 5-HT in guinea pig and rat: species and regional differences. Psychopharmacology (Berl) 172:87-93.
    • (2004) Psychopharmacology (Berl) , vol.172 , pp. 87-93
    • Hughes, Z.A.1    Dawson, L.A.2
  • 25
    • 13444278941 scopus 로고    scopus 로고
    • New symptomatic strategies in Alzheimer's disease
    • Johnson CN, Roland A, and Upton N (2004) New symptomatic strategies in Alzheimer's disease. Drug Discov Today 1:13-19.
    • (2004) Drug Discov Today , vol.1 , pp. 13-19
    • Johnson, C.N.1    Roland, A.2    Upton, N.3
  • 26
    • 0346250850 scopus 로고    scopus 로고
    • 5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortex
    • Lacroix LP, Dawson LA, Hagan JJ, and Heidbreder CA (2004) 5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortex. Synapse 51:158-164.
    • (2004) Synapse , vol.51 , pp. 158-164
    • Lacroix, L.P.1    Dawson, L.A.2    Hagan, J.J.3    Heidbreder, C.A.4
  • 27
  • 29
    • 0034047202 scopus 로고    scopus 로고
    • Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles
    • Lovenberg TW, Pyati J, Chang H, Wilson SJ, and Erlander MG (2000) Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles. J Pharmacol Exp Ther 293:771-778.
    • (2000) J Pharmacol Exp Ther , vol.293 , pp. 771-778
    • Lovenberg, T.W.1    Pyati, J.2    Chang, H.3    Wilson, S.J.4    Erlander, M.G.5
  • 32
    • 34248535273 scopus 로고    scopus 로고
    • 3 receptors in human brain and improved cognitive performance in rats
    • Jul; Madrid, Spain. Alzheimer's Association, Chicago, IL
    • 3 receptors in human brain and improved cognitive performance in rats, in 10th International Conference on Alzheimer's Disease and Related Disorders; 2006 Jul; Madrid, Spain. Alzheimer's Association, Chicago, IL.
    • (2006) 10th International Conference on Alzheimer's Disease and Related Disorders
    • Medhurst, A.D.1
  • 34
  • 36
    • 7644220658 scopus 로고    scopus 로고
    • The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders
    • Passani MB, Lin JS, Hancock A, Crochet S, and Blandina P (2004) The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders. Trends Pharmacol Sci 25:618-625.
    • (2004) Trends Pharmacol Sci , vol.25 , pp. 618-625
    • Passani, M.B.1    Lin, J.S.2    Hancock, A.3    Crochet, S.4    Blandina, P.5
  • 38
    • 0027454927 scopus 로고
    • A detailed autoradiographic mapping of histamine H3 receptors in rat brain areas
    • Pollard H, Moreau J, Arrang JM, and Schwartz JC (1993) A detailed autoradiographic mapping of histamine H3 receptors in rat brain areas. Neuroscience 52:169-189.
    • (1993) Neuroscience , vol.52 , pp. 169-189
    • Pollard, H.1    Moreau, J.2    Arrang, J.M.3    Schwartz, J.C.4
  • 39
    • 0346221274 scopus 로고    scopus 로고
    • 3H]Resiniferatoxin autoradiography in the CNS of wild-type and TRPV1 null mice defines TRPV1 (VR-1) protein distribution
    • 3H]Resiniferatoxin autoradiography in the CNS of wild-type and TRPV1 null mice defines TRPV1 (VR-1) protein distribution. Brain Res 995:176-183.
    • (2004) Brain Res , vol.995 , pp. 176-183
    • Roberts, J.C.1    Davis, J.B.2    Benham, C.D.3
  • 40
    • 77957039092 scopus 로고    scopus 로고
    • Modulation of in vitro neurotransmission in the CNS and in the retina via H3 heteroreceptors
    • Leurs R and Timmerman H eds pp, Elsevier, Amsterdam, The Netherlands
    • Schlicker E and Kathmann M(1998) Modulation of in vitro neurotransmission in the CNS and in the retina via H3 heteroreceptors, in The Histamine H3 Receptor: A Target for New Drugs (Leurs R and Timmerman H eds) pp 13-26, Elsevier, Amsterdam, The Netherlands.
    • (1998) The Histamine H3 Receptor: A Target for New Drugs , pp. 13-26
    • Schlicker, E.1    Kathmann, M.2
  • 42
    • 3042748136 scopus 로고    scopus 로고
    • Selective histamine H3 receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous system
    • Witkin JM and Nelson DL (2004) Selective histamine H3 receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous system. Pharmacol Ther 103:1-20.
    • (2004) Pharmacol Ther , vol.103 , pp. 1-20
    • Witkin, J.M.1    Nelson, D.L.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.