Lu AE58054, a 5-HT 6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats

International Journal of Neuropsychopharmacology

Volumn 13, Issue 8, 2010, Pages 1021-1033

  Arnt, Jorn ^a   Bang Andersen, Benny ^a   Grayson, Ben ^b   Bymaster, Franklin P ^c   Cohen, Michael P ^c   Delapp, Neil W ^c   Giethlen, Bruno ^c   Kreilgaard, Mads ^a   McKinzie, David L ^c   Neill, Joanna C ^b   Nelson, David L ^c   Nielsen, Søhren M ^a   Poulsen, Mette N ^a   Schaus, John M ^c   Witten, Louise M ^a  

^a H LUNDBECK A S   (Denmark)

^b UNIVERSITY OF BRADFORD   (United Kingdom)

^c ELI LILLY AND COMPANY   (United States)

Author keywords

5 HT6 receptor antagonist.; Cognition; in vivo binding; Lu AE58054; novel object recognition

Indexed keywords

5 CHLORO N [4 METHOXY 3 (1 PIPERAZINYL)PHENYL] 3 METHYL 2 BENZOTHIOPHENESULFONAMIDE; [2 (6 FLUORO 1H INDOL 3 YL) ETHYL] [3 (2,2,3,3 TETRAFLUOROPROPOXY) BENZYL] AMINE; [8 (4 METHYLPIPERAZIN 1 YL) 3 PHENYLSULFONYLQUINOLINE]; LU AE58054; PHENCYCLIDINE; RADIOLIGAND; SEROTONIN 6 ANTAGONIST; TRITIUM; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; CELL STRAIN HEK293; COGNITIVE DEFECT; COGNITIVE IMPAIRMENT ASSOCIATED WITH SCHIZOPHRENIA; COMPETITIVE INHIBITION; CONTROLLED STUDY; CORPUS STRIATUM; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; IN VIVO STUDY; MALE; NONHUMAN; PRIORITY JOURNAL; PSYCHOPHARMACOTHERAPY; RAT; RECOGNITION; SCHIZOPHRENIA; SINGLE DRUG DOSE; STEADY STATE; TASK PERFORMANCE;

ANIMALS; BENZYLAMINES; CELLS, CULTURED; COGNITION DISORDERS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; HEK293 CELLS; HUMANS; INDOLES; MALE; PHENCYCLIDINE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN; RECOGNITION (PSYCHOLOGY); SEROTONIN ANTAGONISTS;

EID: 77957240422     PISSN: 14611457     EISSN: 14695111     Source Type: Journal    
DOI: 10.1017/S1461145710000659     Document Type: Article

References (66)

1. Abdul-Monim Z, Neill JC, Reynolds GP (2007). Sub-chronic PCP induces a deficit in reversal learning and in parvalbumin-immunoreactive GABAergic neurons in the rat. Journal of Psychopharmacology 21, 198-205.
2. Adham N, Kao HT, Schecter LE, Bard J, et al. (1993). Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT receptor subtype coupled to the inhibition of adenylate cyclase. Proceedings of the National Academy of Sciences USA 90, 408-412. (Pubitemid 23028871)
3. Andersen PH, Jansen JA, Nielsen EB (1987). [3H]GBR12935 binding in vivo in mouse brain: labelling of a piperazine acceptor site. European Journal of Pharmacology 144, 1-6.
4. Arnt J, Skarsfeldt T (1998). Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence. Neuropsychopharmacology 18, 63-101. (Pubitemid 28026679)
5. Bard JA, Zgombick J, Adham N, Vaysse P, et al. (1993). Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. Journal of Biological Chemistry 268, 23422-23426. (Pubitemid 23328066)
6. Bentley JC, Bourson A, Boess FG, Fone KC, et al. (1999). Investigation of stretching behaviour induced by the selective 5-HT6 receptor antagonist, Ro 04-6790, in rats. British Journal of Pharmacology 126,1537-1542. (Pubitemid 29182336)
7. Bourson A, Boess FG, Bos M, Sleight AJ (1998). Involvement of 5-HT6 receptors in nigro-striatal function in rodents. British Journal of Pharmacology 125,1562-1566. (Pubitemid 28548569)
8. Branchek TA, Blackburn TP (2000). 5-HT6 receptors as emerging targets for drug discovery. Annual Review of Pharmacology and Toxicology 40, 319-334. (Pubitemid 30340685)
9. Breier A (1999). Cognitive deficit in schizophrenia and its neurochemical basis. British Journal of Psychiatry 37(Suppl.), 16-18. (Pubitemid 29089305)
10. Burnham KE, Baxter MG, Bainton JR, Southam E, et al. (2010). Activation of 5-HT6 receptors facilitates attentional set shifting. Psychopharmacology 208,13-21.
11. Cheng YC, Prusoff WH (1973). Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (IC50) of an enzymatic reaction. Biochemical Pharmacology 22, 3099-3108.
12. Dawson LA, Nguyen HQ, Li P (2001). The 5-HT(6) receptor antagonist SB-271046 selectively enhances excitatory neurotransmission in the rat frontal cortex and hippocampus. Neuropsychopharmacology 25, 662-668. (Pubitemid 32995948)
13. DeLapp NW, McKinzie JH, Sawyer BD, Vandergriff A, et al. (1999). Determination of [35S]guanosine-5'-O-(3-thio)triphosphate binding mediated by cholinergic muscarinic receptors in membranes from Chinese hamster ovary cells and rat striatum using an anti-G protein scintillation proximity assay. Journal of Pharmacology Experimental Therapeutics 289, 946-955. (Pubitemid 29191253)
14. Dere E, Huston JP, de Souza Silva MA (2007). The pharmacology, neuroanatomy and neurogenetics of one-trial object recognition in rodents. Neuroscience Biobehavoural Reviews 31, 673-704. (Pubitemid 46670336)
15. Ennaceur A, Delacour J (1988). A new one-trial test for neurobiological studies of memory in rats. 1: Behavioral data. Behavioural Brain Research 31, 47-59.
16. East SZ, Burnet PW, Leslie RA, Roberts JC, et al. (2002). 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585. Synapse 45, 191-199.
17. Foley AG, Murphy KJ, Hirst WD, Gallagher HC, et al. (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.
18. Fone KCF (2008). An update on the role of the 5-hydroxytryptamine6 receptor in cognitive function. Neuropharmacology 55,1015-1022.
19. Gerard C, Martres MP, Lefevre K, Miquel MC, et al. (1997). Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system. Brain Research 746, 207-219. (Pubitemid 27060349)
20. Gerard C, el Mestikawy S, Lebrand C, Adrien J, et al. (1996). Quantitative RT-PCR distribution of serotonin 5-HT6 receptor mRNA in the central nervous system of control or 5,7-dihydroxytryptamine-treated rats. Synapse 23, 164-173. (Pubitemid 26230563)
21. Grayson B, Idris NF, Neill JC (2007). Atypical antipsychotics attenuate a sub-chronic PCP-induced cognitive deficit in the novel object recognition task in the rat. Behavioural Brain Research 184, 31-38. (Pubitemid 47404650)
22. Hall A (2009). 4th Anglo-Swedish medicinal chemistry symposium. Future Medicinal Chemistry 1, 431-434.
23. Hatcher PD, Brown VJ, Tait DS, Bate S, et al. (2005). 5-HT6 receptor antagonists improve performance in an attentional set shifting task in rats. Psychopharmacology (Berlin) 181, 253-259. (Pubitemid 41492195)
24. Hirst WD, Minton JA, Bromidge SM, Moss SF, et al. (2000). Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue. British Journal of Pharmacology 130, 1597-1605.
25. Hirst WD, Stean TO, Rogers DC, Sunter D, et al. (2006). SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. European Journal of Pharmacology 553,109-119. (Pubitemid 44779592)
26. Idris NF, Neill JC, Grayson B, Bang-Andersen B, et al. (2010). Sertindole improves subchronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT6 and 5-HT2A receptor mechanisms. Psychopharmacology 208, 23-36.
27. Jentsch JD, Roth RH (1999). The neuropsychopharmacology of phencyclidine: from nmda receptor hypofunction to the dopamine hypothesis of schizophrenia. Neuropsychopharmacology 20, 201-225. (Pubitemid 29067401)
28. Johnson CN, Ahmed M, Miller ND (2008). 5-HT6 receptor antagonists: prospects for the treatment of cognitive disorders including dementia. Current Opinion in Drug Discovery & Development 11, 642-654.
29. Kapur S, VanderSpek SC, Brownlee BA, Nobrega JN (2003). Antipsychotic dosing in preclinical models is often unrepresentative of the clinical condition: a suggested solution based on in vivo occupancy. Journal of Pharmacology and Experimental Therapeutics 305, 625-631. (Pubitemid 36459179)
30. Keefe RS, Bilder RM, Davis SM, Harvey PD, et al. (2007). Neurocognitive effects of antipsychotic medications in patients with chronic schizophrenia in the CATIE Trial. Archives of General Psychiatry 64, 633-647. (Pubitemid 46878665)
31. Lacroix LP, Dawson LA, Hagan JJ, Heidbreder CA (2004). 5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortex. Synapse 51, 158-164.
32. Leff P, Dougall IG (1993). Further concerns over Cheng-Prusoff analysis. Trends in Pharmacological Sciences 14, 110-112. (Pubitemid 23113114)
33. Leng A, Ouagazzal A, Feldon J, Higgins GA (2003). Effect of the 5-HT6 antagonists Ro 04-6790 and Ro 65-7199 on latent inhibition and prepulse inhibition in the rat: comparison to clozapine. Pharmacology Biochemistry & Behaviour 75, 281-288. (Pubitemid 36859812)
34. Leysen JE (2000). Receptor profile of antipsychotics. In: Ellenbroek BA, Cools AR (Eds), Atypical Antipsychotics (pp. 57-81). Basel: Birkhauser Verlag.
35. Li Z, Huang M, Prus AJ, Dai J, et al. (2006). 5-HT6 receptor antagonist sB-399885 potentiates haloperidol and risperidone-induced dopamine efflux in the medial prefrontal cortex or hippocampus. Brain Research 1134, 70-78. (Pubitemid 46135533)
36. Loiseau F, Dekeyne A, Millan MJ (2008). Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex. Psychopharmacology 196, 93-104.
37. Marcos B, Gil-Bea FJ, Hirst WD, Garcia-Alloza M, et al. (2006). Lack of localization of 5-HT6 receptors on cholinergic neurons: implication of multiple neurotransmitter systems in 5-HT6 receptor-mediated acetylcholine release. European Journal of Neuroscience 24, 1299-1306. (Pubitemid 44401652)
38. Maher-Edwards G, Zvartau-Hind M, Hunter AJ, Gold M, Hopton G, et al. (2010). Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer's Disease. Current Alzheimer Research 7, 374-385.
39. McLean SL, Idris NF, Woolley ML, Neill JC (2009). D1-like receptor activation improves PCP-induced cognitive deficits in animal models: implications for mechanisms of improved cognitive function in schizophrenia. European Neuropsychopharmacology 19, 440-450.
40. McLean SL, Shemar GK, Idris NF, Marshall KM, Neill JC (2007).Deficits in attentional set-shifting in rats following sub-chronic phencyclidine (PCP) administration, effect of gender. European Neuropsychopharmacology 17 (Suppl. 4), S275.
41. Mitchell ES, McDevitt RA, Neumaier JF (2009). Adaptations in 5-HT receptor expression and function: imlpications for treatment of cognitive impairment in aging. Journal of Neuroscience Research 87, 2803-2811.
42. Mitchell ES, Neumaier JF (2005). 5-HT6 receptors: a novel target for cognitive enhancement. Pharmacology & Therapeutics 108, 320-333.
43. Mitchell ES, Neumaier JF (2008). 5-HT and receptor antagonist reversal of emotional learning and prepulse inhibition deficits induced by apomorphine and scopolamine. Pharmacology, Biochemistry & Behaviour 88, 291-298.
44. Monsma Jr FJ, Shen Y, Ward RP, Hamblin MW, et al. (1993). Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Molecular Pharmacology 43, 320-327. (Pubitemid 23081986)
45. Mork A, Witten LM, Arnt J (2009). Effect of sertindole on extracellular dopamine, acetylcholine and glutamate in the medial prefrontal cortex of conscious rats; a comparison with risperidone and exploration of mechanisms involved. Psychopharmacology 206, 39-49.
46. Parker CA, Cunningham VJ, Martarelo L, Rabiner EA, et al. (2008). Evaluation of the novel 5-HT6 receptor radioligand, [11C]GSK-215083 in human. Neuroimage 41, T20.
47. Pouzet B, Didriksen M, Arnt J (2002). Effects of the 5-HT6 receptor antagonist, SB-271046, in animal models for schizophrenia. Pharmacology Biochemistry & Behaviour 71, 635-643. (Pubitemid 34219214)
48. Roberts JC, Reavill C, East SZ, Harrison PJ, et al. (2002). 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 Research 934, 49-57.
49. Rodefer JS, Nguyen TN, Karlsson JJ, Arnt J (2008). Reversal of subchronic pcp-induced deficits in attentional set shifting in rats by sertindole and a 5-HT6 receptor antagonist: comparison among antipsychotics. Neuropsychopharmacology 33, 2657-2666.
50. Rogers D, Hagan J (2001). 5-HT 6 receptor antagonists enhance retention of a water maze task in the rat. Psychopharmacology (Berlin) 158,114-119. (Pubitemid 33020829)
51. Schechter LE, Lin Q, Smith DL, Zhang G, et al. (2008). Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology 33,1323-1335. (Pubitemid 351521711)
52. Schreiber R, Vivian J, Hedley L, Szczepanski K, et al. (2007). Effects of the novel 5-HT6 receptor antagonist RO4368554 in rat models for cognition and sensorimotor gating. European Neuropsychopharmacology 17, 277-288. (Pubitemid 46135932)
53. Sheiner LB, Stanski DR, Vozeh S, Miller RD, et al. (1979). Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to d-tubocurarine. Clinical Pharmacology Therapeutics 25, 358-371. (Pubitemid 9164953)
54. Shirazi-Southall S, Rodriquez DE, Nomikos GG (2002). Effects of typical and atypical antipsychotics and receptor selective compounds on acetylcholine efflux in the hippocampus of the rat. Neuropsychopharmacology 26, 583-594. (Pubitemid 34260977)
55. Sleight AJ, Boess FG, Bos M, Levet-Trafit B, et al. (1998). Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors. British Journal of Pharmacology 124, 556-562. (Pubitemid 28254513)
56. Smith PK, Krohn RI, Hermanson GT, Mallia AK, et al. (1985). Measurement of protein using bicinchoninic acid. Annals of Biochemistry 150, 76-85.
57. Snigdha S, Li Z, Dai J, Shahid M, et al. (2008). Effect of PCP to attenuate DA efflux in rats performing the object recognition task: an in vivo investigation. Society for Neuroscience Abstracts 791.4.
58. Sutcliffe JS, Marshall K, Neill JC (2007). Influence of gender on working and spatial memory in the novel object recognition task in the rat. Behavioural Brain Research 177, 117-125. (Pubitemid 46054189)
59. Upton N, Chuang TT, Hunter AJ, Virley DJ (2008). 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics 5, 458-469. (Pubitemid 351952494)
60. Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL et al. (1996). Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences. Journal of Pharmacology Experimental Therapeutics 276, 720-727. (Pubitemid 126660513)
61. Ward RP, Dorsa DM (1996). Co-localization of serotonin receptor subtypes 5-HT2A, 5-HT2C, and 5-HT6 with neuropeptides in rat striatum. Journal of Comparative Neurology 370, 405-414
62. Ward RP, Hamblin MW, Lachowicz JE, Hoffman BJ, et al. (1995). Localization of serotonin subtype 6 receptor messenger RNA in the rat brain by in situ hybridization histochemistry. Neuroscience 64, 1105-1111.
63. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, et al. (1992). Human serotonin1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proceedings of the National Academy of Science USA 89, 3630-3634.
64. Woolley ML, Marsden CA, Fone CF (2004). 5-HT6 receptors. Current Drug Targets - CNS & Neurological Disorders 3, 59-79.
65. Zgombick JM, Weinshank RL, Macchi M, Schechter LE, et al. (1991). Expression and pharmacological characterization of a canine 5- hydroxytryptamine1D receptor subtype. Molecular Pharmacology 40,1036-1042.
66. Zhang M-Y, Hughes ZA, Kerns EH, Lin Q, et al. (2007). Development of a liquid chromatography/tandem mass spectrometry method for the quantitation of acetylcholine and related neurotransmitters in brain microdialysis samples. Journal of Pharmaceutical and Biomedical Analysis 44,586-593. (Pubitemid 46880097)