Discovery of potential antipsychotic agents possessing pro-cognitive properties

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 385, Issue 3, 2012, Pages 313-323

  Lameh, Jelveh ^a,b   McFarland, Krista ^a   Ohlsson, Jorgen ^a,c   Ek, Fredrik ^a,d   Piu, Fabrice ^e   Burstein, Ethan S ^a   Tabatabaei, Ali ^a,f   Olsson, Roger ^a   Bradley, Stefania Risso ^a,g   Bonhaus, Douglas W ^a,h  

^a ACADIA PHARMACEUTICALS INC   (United States)

^b Genoptix Inc   (United States)

^c ASTRAZENECA R AND D   (Sweden)

^d SPAGO Imaging ^*  (Sweden)

^e Otonomy   (United States)

^f DART NEUROSCIENCE LLC   (United States)

^g MERCK RESEARCH LABORATORIES   (United States)

^h Neuropore Therapies   (United States)

Author keywords

Antipsychotic drug (APD); Dopamine antagonism; Muscarinic agonism; Schizophrenia; Serotonin antagonism

Indexed keywords

4,8 DICHLORO 11 (PIPERAZIN 1 YL) 5H DIBENZO[B,E][1,4]DIAZEPINE; 8 CHLORO 4 METHYL 11 (PIPERAZIN 1 YL) 5H DIBENZO[B,E][1,4]DIAZEPINE; DEXAMPHETAMINE; DIZOCILPINE; DOPAMINE 2 RECEPTOR; KETANSERIN; METHYLSCOPOLAMINE; MUSCARINIC M1 RECEPTOR; NEUROLEPTIC AGENT; RACLOPRIDE; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING ASSAY; COGNITIVE DEFECT; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; HYPERACTIVITY; IN VITRO STUDY; INVERSE AGONISM; LOCOMOTION; MALE; MOUSE; NONHUMAN; RAT; RECOGNITION; SCHIZOPHRENIA;

ANIMALS; ANTIPSYCHOTIC AGENTS; COGNITION; HEK293 CELLS; HUMANS; MALE; MICE; MICROSOMES, LIVER; MOTOR ACTIVITY; NIH 3T3 CELLS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, MUSCARINIC M1; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, DOPAMINE D2; RECOGNITION (PSYCHOLOGY); SEROTONIN ANTAGONISTS;

EID: 84862895922     PISSN: 00281298     EISSN: 14321912     Source Type: Journal    
DOI: 10.1007/s00210-011-0702-2     Document Type: Article

References (47)

1. Abbas A, Roth BL (2008) Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders. Expert Opin Pharmacother 9(18):3251-3259
2. Anagnostaras SG, Murphy GG, Hamilton SE, Mitchell SL, Rahnama NP, Nathanson NM, Silva AJ (2003) Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice. Nat Neurosci 6(1):51-58. doi:10.1038/nn992 (Pubitemid 36026332)
3. Bymaster FP, Felder C, Ahmed S, McKinzie D (2002) Muscarinic receptors as a target for drugs treating schizophrenia. Curr Drug Targets CNS Neurol Disord 1:163-181
4. Bymaster FP, McKinzie DL, Felder CC, Wess J (2003) Use ofM1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res 28(3-4):437-442 (Pubitemid 36314830)
5. Christie JE, Shering A, Ferguson J, Glen AI (1981) Physostigmine and arecoline: effects of intravenous infusions in Alzheimer presenile dementia. Br J Psychiatry 138:46-50 (Pubitemid 11197493)
6. Crook JM, Tomaskovic-Crook E, Copolov DL, Dean B (2000) Decreased muscarinic receptor binding in subjects with schizophrenia: a study of the human hippocampal formation. Biol Psychiatry 48(5):381-388
7. Dean B (2004) M1 receptor agonism, a possible treatment for cognitive deficits in schizophrenia. Neuropsychopharmacology 29(8):1583-1584. doi:10.1038/sj.npp.13005081300508, author reply 1585-1586
8. Dean B, Crook JM, Opeskin K, Hill C, Keks N, Copolov DL (1996) The density of muscarinic M1 receptors is decreased in the caudate-putamen of subjects with schizophrenia. Mol Psychiatry 1(1):54-58 (Pubitemid 126442395)
9. Dean B, McLeod M, Keriakous D, McKenzie J, Scarr E (2002) Decreased muscarinic1 receptors in the dorsolateral prefrontal cortex of subjects with schizophrenia. Mol Psychiatry 7 (10):1083-1091. doi:10.1038/sj.mp.4001199 (Pubitemid 36044267)
10. Drachman DA, Noffsinger D, Sahakian BJ, Kurdziel S, Fleming P (1980) Aging, memory, and the cholinergic system: a study of dichotic listening. Neurobiol Aging 1(1):39-43 (Pubitemid 11065161)
11. Ellis JR, Ellis KA, Bartholomeusz CF, Harrison BJ, Wesnes KA, Erskine FF, Vitetta L, Nathan PJ (2006) Muscarinic and nicotinic receptors synergistically modulate working memory and attention in humans. Int J Neuropsychopharmacol 9(2):175-189. doi:10.1017/S1461145705005407 (Pubitemid 43255831)
12. Fisher A (2008) Cholinergic treatments with emphasis on m1 muscarinic agonists as potential disease-modifying agents for Alzheimer's disease. Neurotherapeutics 5(3):433-442. doi:10.1016/j.nurt.2008.05.002 (Pubitemid 351952486)
13. Friedman JI (2004) Cholinergic targets for cognitive enhancement in schizophrenia: focus on cholinesterase inhibitors and muscarinic agonists. Psychopharmacology (Berl) 174(1):45-53. doi:10.1007/s00213-004-1794-x (Pubitemid 38925090)
14. Gardell LR, Vanover KE, Pounds L, Johnson RW, Barido R, Anderson GT, Veinbergs I, Dyssegaard A, Brunmark P, Tabata-baei A, Davis RE, Brann MR, Hacksell U, Bonhaus DW (2007) ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models. J Pharmacol Exp Ther 322:862-870 (Pubitemid 47105818)
15. Grayson B, Idris NF, NeillJC (2007) Atypical antipsychotics attenuate a sub-chronic PCP-induced cognitive deficit in the novel object recognition task in the rat Behav Brain Res 184(1):31-38. doi:10.1016/j.bbr.2007.06.012 (Pubitemid 47404650)
16. Green M (1996) What are the functional consequences of neuro-cognitive deficits in schizophrenia? Am J Psychiatry 154:799-804
17. Green M, Kern R, Braff D, Mintz J (2000) Neurocognition and functional outcome in schizophrenia: are we measuring the right stuff? Schizoph Bull 26:119-136 (Pubitemid 30317696)
18. Kane J, Honigfeld G, Singer J, Meltzer HY, Group tCCS (1988) Clozapine for the treatment-resistant schizophrenic. Arch Gen Psychiatr 45:789-796
19. Kapur S, Remington G (2001) Atypical antipsychotics: new directions and new challenges in the treatment of schizophrenia. Annu Rev Med 52:503-517. doi:10.1146/annurev.med.52.1.503 (Pubitemid 32195338)
20. Karasawa J, Hashimoto K, Chaki S (2008) D-Serine and a glycine transporter inhibitor improve MK-801-induced cognitive deficits in a novel object recognition test in rats. Behav Brain Res 186 (1):78-83. doi:10.1016/j.bbr.2007.07.033 (Pubitemid 350100896)
21. Kim S, Huang A, Snowman A, Teuscher C, Snyder S (2007) Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation ofhypothalamic AMP-kinase. Proc Nat Acad Sci 104:3456-3459 (Pubitemid 46364180)
22. Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL (2003) H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharm 28:519-526
23. Lepor H, Jones K, Williford W (2000) The mechanism of adverse events associated with terazosin: an analysis of the Veterans Affairs cooperative study. J Urol 163:1134-1137 (Pubitemid 30169378)
24. Li Z, Huang M, Ichikawa J, Dai J, Meltzer HY (2005) N-Desmethylclo- zapine, a major metabolite of clozapine, increases cortical acetylcholine and dopamine release in vivo via stimulation of M1 muscarinic receptors. Neuropsychopharmacology 1(10):1
25. Lieberman J, Stroup T, McEvoy J, Swartz M, Rosenheck R, Perkins D, Keefe R, Davis S, Davis C, Lebowitz B, Severe J, Hsiao J, Investigators CAToEC (2005) Effectiveness of antipsychotic drugs in patients with chronic schizophrenia. N Engl J Med 353:1209-1223 (Pubitemid 41345943)
26. Mancama D, Arranz MJ, Landau S, Kerwin R (2003) Reduced expression of the muscarinic 1 receptor cortical subtype in schizophrenia. Am J Med Genet B Neuropsychiatr Genet 119B (1):2-6. doi:10.1002/ajmg.b.20020 (Pubitemid 37064044)
27. McArthur RA, Gray J, Schreiber R (2010) Cognitive effects of muscarinic M1 functional agonists in non-human primates and clinical trials. Curr Opin Investig Drugs 11(7):740-760
28. Meller E, Helmer-Matyjek E, Bohmaker K, Adler CH, Friedhoff AJ, Goldstein M (1986) Receptor reserve at striatal dopamine autoreceptors: implications for selectivity of dopamine agonists. Eur J Pharmacol 123(2):311-314 (Pubitemid 16055467)
29. Meltzer H, Matsubara S, Lee J (1989) Classification oftypical and atypical antipsychotic drugs on the basis of dopamine, D-1, D-2 and serotonin2 pKi values. J Pharmacol Exp Ther 251:238-246
30. 2C receptors tonically inhibit dopamine (DA) release and noradrenaline (NA), but not 5-HT, release in the frontal cortex in vivo. Neurophar-macology 37:953-955
31. Miller KJ (2005) Serotonin 5-ht2c receptor agonists: potential for the treatmentofobesity MolInterv5(5):282-291. doi:10.1124/mi.5.5.8 (Pubitemid 41595460)
32. Mizoguchi H, Takuma K, Fukakusa A, Ito Y, Nakatani A, Ibi D, Kim HC, Yamada K (2008) Improvement by minocycline of methamphetamine-induced impairment of recognition memory in mice. Psychopharmacology (Berl) 196(2):233-241. doi:10.1007/s00213-007-0955-0
33. 2A receptors in antipsychotic activity. Life Sci 56:2209-2222
34. Seeman P (1992) Elevated D2 in schizophrenia: role of endogenous dopamine and cerebellum. Commentary on "The current status of PET scanning with respect to schizophrenia". Neuropsychopharm 7:55-57
35. Sellin AK, Shad M, Tamminga C (2008) Muscarinic agonists for the treatmentof cognition in schizophrenia. CNS Spectr 13(11):985-996
36. Shekhar A, Potter WZ, Lightfoot J, Lienemann J, Dube S, Mallinckrodt C, Bymaster FP, McKinzie DL, Felder CC (2008) Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry 165 (8):1033-1039. doi:10.1176/appi.ajp.2008.06091591
37. Sitaram N, Weingartner H, Gillin JC (1978) Human serial learning: enhancement with arecholine and choline impairment with scopolamine. Science 201(4352):274-276 (Pubitemid 8396756)
38. Snigdha S, Neill JC (2008) Efficacy of antipsychotics to reverse phencyclidine-induced social interaction deficits in female rats- a preliminary investigation. Behav Brain Res 187(2):489-494. doi:10.1016/j.bbr.2007.10.012
39. Spalding TA, Trotter C, Skjaerbaek N, Messier TL, Currier EA, Burstein ES, Li D, Hacksell U, Brann MR (2002) Discovery of an ectopic activation site on the M(1) muscarinic receptor. Mol Pharmacol 61(6):1297-1302 (Pubitemid 34575739)
40. Stanhope KJ, Mirza NR, Bickerdike MJ, Bright JL, Harrington NR, Hesselink MB, Kennett GA, Lightowler S, Sheardown MJ, Syed R, Upton RL, Wadsworth G, Weiss SM, Wyatt A (2001) The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J Pharmacol Exp Ther 299(2):782-792
41. Stroup T, Alves W, Hamer R, Lieberman J (2006a) Clinical trials for antipsychotic drugs: design conventions, dilemmas and innova-tions. Nature Reviews, Drug Discovery 5:133-146
42. Stroup T, Lieberman J, McEvoy J, Swartz M, Davis S, Rosenheck R, Perkins D, Keefe R, Davis C, Severe J, Hsiao J, Investigators C (2006b) Effectiveness of olanzapine, quetiapine, risperidone, and ziprasidone in patients with chronic schizophrenia following discontinuation of a previous atypical antipsychotic. Am J Psychiatry 163:611-622 (Pubitemid 44464570)
43. Takata Y, Kurihara J, Suzuki S, Okubo Y, Kato H (1999) A rabbit model for evaluation of chlorpromazine-induced orthostatic hypotension. Biol Pharm Bull 22:457-462 (Pubitemid 29252217)
44. Vanover KE, Veinbergs I, Davis RE (2008) Antipsychotic-like behavioral effects and cognitive enhancement by a potent and selective muscarinic M-sub-1 receptor agonist, AC-260584. Behav Neurosci 122(3):570-575. doi:10.1037/0735- 7044.122.3.570 (Pubitemid 351787835)
45. Weiner DM, Burstein ES, Nash N, Croston GE, Currier EA, Vanover KE, Harvey SC, Donohoue E, Hansen HC, Andersson CM, Spalding TA, Gibson DFC, Krebs-Thomson K Powell SB, Geyey MA, Hacksell U, Brann MR (2001) 5-Hydroxytryptamine2A receptor inverse agonists as antipsychotics. J Pharmacol Exp Therapeut 299:268-276 (Pubitemid 32905144)
46. Wong AH, Tol HHV (2003) Schizophrenia: from phenomenology to neurobiology Neurosci Biobehav Rev 27:269-306 (Pubitemid 36681541)
47. Wood MD, Heidbreder C, Reavill C, Ashby CR, Middlemiss DN (2001) 5-HT2C receptor antagonists: potential in schizophrenia. Drug Dev Res 54:88-94 (Pubitemid 34041810)