The 5-hydroxytryptamine 4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations

Journal of Pharmacology and Experimental Therapeutics

Volumn 341, Issue 3, 2012, Pages 681-691

  Johnson, David E ^a   Drummond, Elena ^a   Grimwood, Sarah ^a   Sawant Basak, Aarti ^a   Miller, Emily ^a   Tseng, Elaine ^a   McDowell, Laura L ^a   Vanase Frawley, Michelle A ^a   Fisher, Katherine E ^a   Rubitski, David M ^a   Stutzman Engwall, Kim J ^a   Nelson, Robin T ^a   Horner, Weldon E ^a   Gorczyca, Roxanne R ^a   Hajos, Mihaly ^a   Siok, Chester J ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6,7 DIHYDRO 4 HYDROXY 7 ISOPROPYL 6 OXO N [3 (PIPERIDIN 1 YL)PROPYL]THIENO[2,3]PYRIDINE 5 CARBOXAMIDE; ACETYLCHOLINE; CYCLIC AMP; DONEPEZIL; HISTAMINE; PRUCALOPRIDE; PRX 03140; SEROTONIN 4 AGONIST; SEROTONIN 4 RECEPTOR; UNCLASSIFIED DRUG; 6,7 DIHYDRO 4 HYDROXY 7 ISOPROPYL 6 OXO N (3 (PIPERIDIN 1 YL)PROPYL)THIENO(2,3 B)PYRIDINE 5 CARBOXAMIDE; 6,7-DIHYDRO-4-HYDROXY-7-ISOPROPYL-6-OXO-N-(3-(PIPERIDIN-1-YL)PROPYL)THIENO(2,3-B)PYRIDINE-5-CARBOXAMIDE; BENZOFURAN DERIVATIVE; PYRIDONE DERIVATIVE; SEROTONIN; THIOPHENE DERIVATIVE;

ACETYLCHOLINE BRAIN LEVEL; ACETYLCHOLINE RELEASE; ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN DEPTH STIMULATION; BRAIN LEVEL; COGNITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BINDING; DRUG POTENTIATION; EMBRYO; HIPPOCAMPUS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALE; NEUROPHARMACOLOGY; NONHUMAN; OSCILLATION; PREFRONTAL CORTEX; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN SYNTHESIS; PROTEIN TARGETING; RAT; RECEPTOR OCCUPANCY; ANIMAL; AREA UNDER THE CURVE; CHEMISTRY; DRUG EFFECT; ELECTROENCEPHALOGRAPHY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; METABOLISM; MICRODIALYSIS; SPRAGUE DAWLEY RAT; TANDEM MASS SPECTROMETRY;

ACETYLCHOLINE; ANIMALS; AREA UNDER CURVE; BENZOFURANS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; ELECTROENCEPHALOGRAPHY; HIPPOCAMPUS; HISTAMINE; HUMANS; MALE; MICRODIALYSIS; PREFRONTAL CORTEX; PYRIDONES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN, 5-HT4; SEROTONIN; SEROTONIN 5-HT4 RECEPTOR AGONISTS; TANDEM MASS SPECTROMETRY; THIOPHENES;

EID: 84861534764     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.112.192351     Document Type: Article

References (48)

1. Acquas E and Fibiger HC (1996) Chronic lithium attenuates dopamine D1-receptor mediated increases in acetylcholine release in rat frontal cortex. Psychopharmacology 125:162-167. (Pubitemid 26173186)
2. Airaksinen MS, Paetau A, Paljärvi L, Reinikainen K, Riekkinen P, Suomalainen R, and Panula P (1991) Histamine neurons in human hypothalamus: anatomy in normal and Alzheimer's diseased brains. Neuroscience 44:465-481.
3. Bacciottini L, Passani MB, Giovannelli L, Cangioli I, Mannaioni PF, Schunack W, and Blandina P (2002) Endogenous histamine in the medial septum-diagonal band complex increases the release of acetylcholine from the hippocampus: a dual-probe microdialysis study in the freely moving rat. Eur J Neurosci 15:1669-1680. (Pubitemid 35471923)
4. Bartus RT, Dean RL 3rd, Beer B, and Lippa AS (1982) The cholinergic hypothesis of geriatric memory dysfunction. Science 217:408-414.
5. Blandina P, Efoudebe M, Cenni G, Mannaioni P, and Passani MB (2004) Acetylcholine, histamine, and cognition: two sides of the same coin. Learn Mem 11:1-8. (Pubitemid 38167052)
6. Blondel O, Gastineau M, Dahmoune Y, Langlois M, and Fischmeister R (1998) Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J Neurochem 70:2252-2261. (Pubitemid 28252350)
7. Boddeke HW and Kalkman HO (1990) Zacopride and BRL 24924 induce an increase in EEG-energy in rats. Br J Pharmacol 101:281-284. (Pubitemid 20292877)
8. 4 receptor mRNA and ligand binding sites in the post-mortem human brain. Synapse 36:35-46.
9. 4(i). Naunyn Schmiedebergs Arch Pharmacol 369:616-628.
10. Briejer MR, Bosmans JP, Van Daele P, Jurzak M, Heylen L, Leysen JE, Prins NH, and Schuurkes JA (2001) The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Eur J Pharmacol 423:71-83. (Pubitemid 32595730)
11. Cachard-Chastel M, Devers S, Sicsic S, Langlois M, Lezoualc'h F, Gardier AM, and Belzung C (2008) Prucalopride and donepezil act synergistically to reverse scopolamine-induced memory deficit in C57Bl/6j mice. Behav Brain Res 187:455-461.
12. 1 receptors in the nucleus basalis magnocellularis: a dual-probe microdialysis study in the freely moving rat. Eur J Neurosci 13:68-78.
13. 4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain. Mol Pharmacol 55:910-920.
14. 4 receptor stimulation facilitates acetylcholine release in rat frontal cortex. Neuroreport 5:1230-1232.
15. 4 receptor or the serotonin transporter in the dorsolateral prefrontal cortex from subjects with schizophrenia. Neurochem Int 34:109-115.
16. Dumuis A, Bouhelal R, Sebben M, Cory R, and Bockaert J (1988) A nonclassical 5-hyrdoxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. Mol Pharmacol 34:880-887. (Pubitemid 19014410)
17. 4 receptors. Trends Pharmacol Sci 16:391-398.
18. Fontana DJ, Daniels SE, Eglen RM, and Wong EH (1996) Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats. Neuropharmacology 35:321-327. (Pubitemid 26173168)
19. 4 receptor ligands in rat spatial navigation. Neuropharmacology 36:689-696.
20. 4 receptors in the mouse passive avoidance test. J Pharmcol Exp Ther 286:1115-1121.
21. 4 receptor: molecular cloning and pharmacological characterization of two splice variants. EMBO J 14:2806-2815.
22. Grimwood S and Hartig PR (2009) Target site occupancy: emerging generalizations from clinical and preclinical studies. Pharmacol Ther 122:281-301.
23. Hajós M, Siok CJ, Hoffmann WE, Li S, and Kocsis B (2008) Modulation of hippocampal theta oscillation by histamine H3 receptors. J Pharmacol Exp Ther 324:391-398. (Pubitemid 350294183)
24. Horner WE, Johnson DE, Schmidt AW, and Rollema H (2007) Methylphenidate and atomoxetine increase histamine release in the rat prefrontal cortex. Eur J Pharmacol 558:96-97. (Pubitemid 46328877)
25. Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed, National Academies Press, Washington, DC, National Institutes of Health Publication 85-23.
26. Kahana MJ (2006) The cognitive correlates of human brain oscillations. J Neurosci 26:1669-1672.
27. Kalvass JC and Maurer TS (2002) Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery. Biopharm Drug Dispos 23:327-338. (Pubitemid 36124162)
28. Kinney GG, Patino P, Mermet-Bouvier Y, Starrett JE Jr, and Gribkoff VK (1999) Cognition-enhancing drugs increase stimulated hippocampal θ rhythm amplitude in the urethane-anesthetized rat. J Pharmacol Exp Ther 291:99-106. (Pubitemid 29451578)
29. 4 splice variants. Naunyn Schmiedebergs Arch Pharmacol 371:473-479.
30. 4receptors improve social olfactory memory in the rat. Neuropharmacology 36:681-687.
31. 4 receptors in the human brain in vivo. J Nucl Med 50:900-908.
32. 4 receptors in cholinergic function associated with cognitive processes: behavioral, electrophysiological, and neurochemical studies. J Pharmacol Exp Ther 296:676-682.
33. McNaughton N, Kocsis B, and Hajós M (2007) Elicited hippocampal theta rhythm: a screen for anxiolytic and procognitive drugs through changes in hippocampal function? Behav Pharmacol 18:329-346. (Pubitemid 47356363)
34. 4 receptor in the central nervous system by TaqMan real time RT-PCR. Mol Brain Res 90:125-134.
35. 4-receptor agonists. J Pharmacol Sci 107:251-259.
36. 4agonist, enhances memory and hippocampal acetylcholine efflux. Neuropharmacology 53:563-573.
37. Philippu A and Prast H (2001) Importance of histamine in modulatory processes, locomotion and memory. Behav Brain Res 124:151-159. (Pubitemid 32964633)
38. Reed-Hagen AE, Tsuchiya M, Shimada K, Wentland JA, and Obach RS (1999) Pharmacokinetics of ezlopitant, a novel non-peptidic neurokinin-1 receptor antagonist in preclinical species and metabolite kinetics of the pharmacologically active metabolites. Biopharm Drug Dispos 20:429-439.
39. 4 receptors in post mortem human brain tissue: distribution, pharmacology and effects on neurodegenerative diseases. Br J Pharmacol 114:993-998.
40. Roth BL, Hanizavareh SM, and Blum AE (2004) Serotonin receptors represent highly favorable molecular targets for cognitive enhancement in schizophrenia and other disorders. Psychopharmacology 174:17-24. (Pubitemid 38925086)
41. Scarr E, Cowie TF, Kanellakis S, Sundram S, Pantelis C, and Dean B (2009) Decreased cortical muscarinic receptors define a subgroup of subjects with schizophrenia. Mol Psychiatry 14:1017-1023.
42. Schneider C, Risser D, Kirchner L, Kitzmüller E, Cairns N, Prast H, Singewald N, and Lubec G (1997) Similar deficits of central histaminergic system in patients with Down syndrome and Alzheimer disease. Neurosci Lett 222:183-186. (Pubitemid 27079733)
43. 4 receptor agonist mediated enhancement of cognitive function in vivo and amyloid precursor protein processing in vitro: a pharmacodynamic and pharmacokinetic assessment. Neuropharmacology 61:69-79.
44. Siok CJ, Rogers JA, Kocsis B, and Hajós M (2006) Activation of α7 acetylcholine receptors augments stimulation-induced hippocampal theta oscillation. Eur J Neurosci 23:570-574.
45. Terry AV Jr, Buccafusco JJ, Jackson WJ, Prendergast MA, Fontana DJ, Wong EH, Bonhaus DW, Weller P, and Eglen RM (1998) Enhanced delayed matching performance in younger and older macaques administered the 5-HT4 receptor agonist, RS 17071. Psychopharmacology 135:407-415. (Pubitemid 28254848)
46. Tzavara ET, Bymaster FP, Overshiner CD, Davis RJ, Perry KW, Wolff M, McKinzie DL, Witkin JM, and Nomikos GG (2006) Procholinergic and memory enhancing properties of the selective norepinephine uptake inhibitor atomoxetine. Mol Psychiatry 11:187-195. (Pubitemid 43164620)
47. Vertes RP and Kocsis B (1997) Brainstem-diencephalo-septohippocampal systems controlling the theta rhythm of the hippocampus. Neuroscience 81:893-926. (Pubitemid 27421757)
48. Yamaguchi T, Suzuki M, and Yamamoto M (1997) Facilitation of acetylcholine release in rat frontal cortex by indeloxazine hydrochloride: involvement of endogenous serotonin and 5-HT4 receptors. Naunyn Schmiedebergs Arch Pharmacol 356:712-720. (Pubitemid 27525069)