Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1A receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405)

Journal of Pharmacology and Experimental Therapeutics

Volumn 325, Issue 1, 2008, Pages 134-145

  Hirst, Warren D ^a   Andree, Terrance H ^a   Aschmies, Suzan ^a   Childers, Wayne E ^a   Comery, Thomas A ^a   Dawson, Lee A ^a   Day, Mark ^a   Feingold, Irene B ^a   Grauer, Steven M ^a   Harrison, Boyd L ^a   Hughes, Zoë A ^a   Kao, John ^a   Kelly, Michael G ^a   Van Der Lee, Heidi ^a   Rosenzweig Lipson, Sharon ^a   Saab, Annmarie L ^a   Smith, Deborah L ^a   Sullivan, Kelly ^a   Rizzo, Stacey J Sukoff ^a   Tio, Cesario ^a   Zhang, Mei Yi ^a   Schechter, Lee E ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; DONEPEZIL; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; N [2 METHYL(4 INDOLYL 1 PIPERAZINYL)ETHYL] N (2 PYRIDINYL)CYCLOHEXANE CARBOXAMIDE; SCOPOLAMINE; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; TRITIUM; UNCLASSIFIED DRUG; WAY 101405;

AMNESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COGNITIVE DEFECT; CONDITIONING; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG TARGETING; FEAR; FEMALE; HIPPOCAMPUS; IN VIVO STUDY; LEARNING; MALE; MAZE TEST; MICRODIALYSIS; NEUROPHARMACOLOGY; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR INTRINSIC ACTIVITY; RECEPTOR OCCUPANCY; RODENT;

AMINOPYRIDINES; ANIMALS; BIOLOGICAL AVAILABILITY; BRAIN; COGNITION; CYCLOHEXANES; MEMORY; MODELS, ANIMAL; PIPERAZINES; RADIOLIGAND ASSAY; RATS; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN ANTAGONISTS;

EID: 41149099114     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.107.133082     Document Type: Article

References (38)

1. 1A receptor antagonists on hippocampal 5-hydroxytryptamine levels: (S)-WAY100135, but not WAY100635, has partial agonist properties. Eur J Pharmacol 304:15-21.
2. 1A receptor antagonist WAY-100635. Psychopharmacology 167:28-36.
3. Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
4. 1A binding in rat brain-a combined in situ hybridisation/in vitro receptor autoradiographic study. Brain Res 561:51-60.
5. 4 receptor agonist. Psychopharmacology 188:244-251.
6. 1A antagonists: the discovery of Lecozotan. J Med Chem 48:3467-3470.
7. Day M and Langston RF (2006) Post-training N-methyl-D-aspartate receptor blockade offers protection from retrograde interference but does not affect consolidation of weak or strong memory traces in the water maze. Neuroscience 137:19-28.
8. 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.
9. 1A receptors. Eur J Pharmacol 237:283-291.
10. 1A receptor antagonist, WAY-100635. Eur J Pharmacol 281:81-88.
11. 1A antagonist, WAY-100635, ameliorates the cognitive impairment induced by fornix transection in the marmoset. Psychopharmacology 127:245-254.
12. B2 receptor subunits. Biochem Pharmacol 65:1103-1113.
13. 6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. Eur J Pharmacol 553:109-119.
14. Hoyer D, Hannon JP, and Martin GR (2002) Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav 71:533-554.
15. 1A receptors in rat brain. Eur J Pharmacol 271:515-523.
16. Johansson L, Sohn D, Thorberg SO, Jackson DM, Kelder D, Larsson LG, Renyi L, Ross SB, Wallsten C, Eriksson H, et al. (1997) The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299. J Pharmacol Exp Ther 283:216-225.
17. Kia HK, Brisorgueil MJ, Hamon M, Calas A, and Verge D (1996) Ultrastructural localization of 5-hydroxytryptamine1A receptors in the rat brain. J Neurosci Res 46:697-708.
18. 1A receptors in spatial and aversive learning in the rat. Neuropharmacology 48:830-852.
19. Madjid N, Tottie EE, Lüttgen M, Meister B, Sandin J, Kuzmin A, Stiedl O, and Ogren SO (2006) 5-Hydroxytryptamine 1A receptor blockade facilitates aversive learning in mice: interactions with cholinergic and glutamatergic mechanisms. J Pharmacol Exp Ther 316:581-591.
20. Martin SJ and Clark RE (2007) The rodent hippocampus and spatial memory: from synapses to systems. Cell Mol Life Sci 64:401-431.
21. Meltzer CC, Smith G, DeKosky ST, Pollock BG, Mathis CA, Moore RY, Kupfer DJ, and Reynolds CF (1998) Serotonin in aging, late-life depression, and Alzheimer's disease: the emerging role of functional imaging. Neuropsychopharmacology 18:407-430.
22. Millan MJ, Gobert A, Roux S, Porsolt R, Meneses A, Carli M, Di Cara B, Jaffard R, Rivet JM, Lestage P, et al. (2004) The serotonin1A receptor partial agonist S15535 [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine] enhances cholinergic transmission and cognitive function in rodents: a combined neurochemical and behavioral analysis. J Pharmacol Exp Ther 311:190-203.
23. Morris RG, Garrud P, Rawlins JN, and O'Keefe J (1982) Place-navigation impaired in rats with hippocampal lesions. Nature 297:681-683.
24. Myhrer T (2003) Neurotransmitter systems involved in learning and memory in the rat: a meta-analysis based on studies of four behavioral tasks. Brain Res Rev 41:268-287.
25. Paxinos G and Watson C (1986) The Rat Brain in Stereotaxic Coordinates, Academic Press, New York.
26. 1A receptors in human brain with PET and [11C]WAY-100635. Eur J Pharmacol 283:R1-R3.
27. 1A receptor antagonist WAY-100635 improves rats performance in different models of amnesia evaluated by the object recognition task. Brain Res 983:215-222.
28. 1A receptors in healthy young and elderly subjects, and in patients with Alzheimer's disease. Clin Pharmacol Ther 83:86-96.
29. Rasmussen K, Calligaro DO, Czachura JF, Dreshfield-Ahmad LJ, Evans DC, Hemrick-Luecke SK, Kallman MJ, Kendrick WT, Leander JD, Nelson DL, et al. (2000) The novel 5-hydroxytryptamine(1A) antagonist LY426965: effects on nicotine withdrawal and interactions with fluoxetine. J Pharmacol Exp Ther 294:688-700.
30. 1A receptor antagonists in the treatment of cognitive dysfunction associated with Alzheimer's disease. Curr Pharm Des 8:139-145.
31. Schechter LE, Smith DL, Rosenzweig-Lipson S, Sukoff SJ, Dawson LA, Marquis K, Jones D, Piesla M, Andree T, Nawoschik S, et al. (2005) Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. J Pharmacol Exp Ther 314:1274-1289.
32. Steckler T and Sahgal A (1995) The role of serotonergic-cholinergic interactions in the mediation of cognitive behaviour. Behav Brain Res 67:165-199.
33. 1A receptors in classical fear conditioning in C57BL/6J mice. J Neurosci 20:8515-8527.
34. 1A receptor binding potential declines with age as measured by [11C]WAY-100635 and PET. Neuropsychopharmacology 24:522-530.
35. 1A receptor ligands on rat dorso-lateral septal neurones in vitro. Br J Pharmacol 106:893-899.
36. 2 receptor occupancy predicts catalepsy and the suppression of conditioned avoidance response behavior in rats. Psychopharmacology 150:422-429.
37. 1A receptors on human explicit memory. Am J Psychiatry 160:334-340.
38. Zhang MY, Hughes ZA, Lin Q, Kerns EH, and Beyer CE (2007) Development of a liquid chromatography/tandem mass spectrometry method for the quantitation of acetylcholine and related neurotransmitters in brain microdialysates from freely moving rats. J Pharm Biomed Anal 44:586-593.