Muscarinic agonists and antagonists in schizophrenia: Recent therapeutic advances and future directions

Handbook of Experimental Pharmacology

Volumn 208, Issue , 2012, Pages 167-190

  Bolbecker, Amanda R ^a   Shekhar, Anantha ^b  

^a INDIANA UNIVERSITY   (United States)

^b INDIANA UNIVERSITY   (United States)

Author keywords

Acetylcholine; Allosteric; Cholinergic; Cognitive; Muscarinic; Psychosis; Schizophrenia

Indexed keywords

4 [3 (4 BUTYLPIPERIDIN 1 YL)PROPYL] 7 FLUORO 4H BENZO[1,4]OXAZIN 3 ONE; AC 260584; AC 42; ARECOLINE; BENZYLQUINOLONE CARBOXYLATE; BIBN 99; CHOLINERGIC RECEPTOR BLOCKING AGENT; CHOLINERGIC RECEPTOR STIMULATING AGENT; CLOZAPINE; LY 2033298; METHOCTRAMINE; MILAMELINE; MUSCARINIC AGENT; MUSCARINIC M1 RECEPTOR; MUSCARINIC M2 RECEPTOR; MUSCARINIC M4 RECEPTOR; MUSCARINIC M5 RECEPTOR; MUSCARINIC RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; NEUROLEPTIC AGENT; OLANZAPINE; PLACEBO; RISPERIDONE; SABCOMELINE; SCH 55790; TPBP; UNCLASSIFIED DRUG; VU 010010; VU 0238429; XANOMELINE; ZIPRASIDONE; ACETYLCHOLINE;

ALLOSTERISM; ALZHEIMER DISEASE; ARTICLE; COGNITIVE DEFECT; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG PENETRATION; DRUG POTENCY; DRUG SAFETY; DRUG TARGETING; EVIDENCE BASED MEDICINE; HUMAN; HYPERACTIVITY; LEARNING DISORDER; MEMORY DISORDER; MOLECULAR PATHOLOGY; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN LOCALIZATION; PSYCHOSIS; SCHIZOPHRENIA; TREATMENT PLANNING; UNSPECIFIED SIDE EFFECT; ANIMAL; BRAIN; METABOLISM; PSYCHOLOGY; REVIEW; SIGNAL TRANSDUCTION; TREATMENT OUTCOME;

ACETYLCHOLINE; ANIMALS; ANTIPSYCHOTIC AGENTS; BRAIN; HUMANS; MUSCARINIC AGONISTS; MUSCARINIC ANTAGONISTS; SCHIZOPHRENIA; SCHIZOPHRENIC PSYCHOLOGY; SIGNAL TRANSDUCTION; TREATMENT OUTCOME;

EID: 84856645717     PISSN: 01712004     EISSN: 18650325     Source Type: Book Series    
DOI: 10.1007/978-3-642-23274-9_8     Document Type: Article

References (165)

1. Abood LG, Biel JH (1962) Anticholinergic psychototmimetic agents. Int Rev Neurobiol 4:217-273
2. Anagnostaras SG, Murphy GG, Hamilton SE et al (2003) Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice. Nat Neurosci 6:51-58 (Pubitemid 36026332)
3. Andersen MB, Fink-Jensen A, Peacock L et al (2003) The muscarinic M1/M4 receptor agonist xanomeline exhibits antipsychotic-like activity in Cebus apella monkeys. Neuropsychopharmacology 28:1168-1175
4. Andreasen NC, O'Leary DS, Flaum M et al (1997) Hypofrontality in schizophrenia: distributed dysfunctional circuits in neuroleptic-naive patients. Lancet 349:1730-1734 (Pubitemid 27252672)
5. Basile AS, Fedorova I, Zapata A et al (2002) Deletion of the M5 muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia. Proc Natl Acad Sci U S A 99:11452-11457 (Pubitemid 34920946)
6. Bellack AS, Gold JM, Buchanan RW (1999) Cognitive rehabilitation for schizophrenia: problems, prospects, and strategies. Schizophr Bull 25:257-274 (Pubitemid 29272504)
7. 2 through a correlation of in vivo microdialysis and in vitro receptor binding data. J Pharmacol Exp Ther 273:273-279
8. Blaha CD, Allen LF, Das S et al (1996) Modulation of dopamine efflux in the nucleus accumbens after cholinergic stimulation of the ventral tegmental area in intact, pedunculopontine tegmental nucleus-lesioned, and laterodorsal tegmental nucleus-lesioned rats. J Neurosci 16:714-722
9. Bodick NC, Offen WW, Levey AI et al (1997) (1997) Effects of xanomeline, a selective muscarinic receptor agonist, on cognitive function and behavioral symptoms in Alzheimer disease. Arch Neurol 54:465-473 (Pubitemid 27172867)
10. Bolden C, Cusack B, Richelson E (1991) Clozapine is a potent and selective muscarinic antagonist at the five cloned human muscarinic acetylcholine receptors expressed in CHO-K1 cells. Eur J Pharmacol 192:205-206
11. Bradley SR, Lameh J, Ohrmund L et al (2010) AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model. Neuropharmacology 58:365-373
12. Brady AE, Jones CK, Bridges TM et al (2008) Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther 327:941-953
13. Braver TS, Cohen JD (2000) On the control of control: the role of dopamine in regulating prefrontal function and working memory. In: Monsell S, Driver J (eds) Control of cognitive processes: attention and performance XVIII. MIT Press, Cambridge
14. Bridges TM, Marlo JE, Niswender CM (2009) Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem 52:3445-3448
15. Brodde OE, Michel MC (1999) Adrenergic and muscarinic receptors in the human heart. Pharmacol Rev 51:651-690
16. Bymaster FP, Wong DT, Mitch CH et al (1994) Neurochemical effects of the M1 muscarinic agonist xanomeline (LY246708/NNC11-0232). J Pharmacol Exp Ther 269:282-289
17. Bymaster FP, Whitesitt CA, Shannon HE et al (1997) Xanomeline: a selective muscarinic agonist for the treatment of Alzheimers disease. Drug Dev Res 40:158-177
18. Bymaster FP, Shannon HE, Rasmussen K et al (1998) Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo [3.2.1]octane. Eur J Pharmacol 356:109-119
19. Bymaster FP, Felder C, Ahmed S et al (2002) Muscarinic receptors as a target for drugs treating schizophrenia. Curr Drug Targets CNS Neurol Disord 1:163-181
20. Bymaster FP, Felder CC, Tzavara E (2003a) Muscarinic mechanisms of antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry 27:1125-1143 (Pubitemid 37464958)
21. Bymaster FP, McKinzie DL, Felder CC et al (2003b) Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res 28:437-442 (Pubitemid 36314830)
22. Bymaster FP, Carter PA, YamadaM et al (2003c) Role of specific muscarinic receptor subtypes in cholinergic parasympathomimetic responses, in vivo phosphoinositide hydrolysis, and pilocarpine- induced seizure activity. Eur J Neurosci 17:1403-1410 (Pubitemid 36560839)
23. Calabresi P, Centonze D, Gubellini P et al (2000) Acetylcholine-mediated modulation of striatal function. Trends Neurosci 23:120-126 (Pubitemid 30112539)
24. Carey GJ, Billard W, Binch H 3rd et al (2001) SCH 57790, a selective muscarinic M(2) receptor antagonist, releases acetylcholine and produces cognitive enhancement in laboratory animals. Eur J Pharmacol 431:189-200 (Pubitemid 33132125)
25. Carter CS, Perlstein P, Ganguli R et al (1998) Functional hypofrontality and working memory dysfunction in schizophrenia. Am J Psychiatry 155:1285-1287 (Pubitemid 28402528)
26. Caulfield MP (1993) Muscarinic receptors - characterization, coupling and function. Pharmacol Ther 58:319-379 (Pubitemid 23273186)
27. Chan WY, McKinzie DL, Bose S, Mitchell SN, Witkin JM, Thompson RC, Christopoulos A, Lazareno S, Birdsall NJ, Bymaster FP, Felder CC. Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia. Proc Natl Acad Sci USA. 2008 Aug 5;105 (31):10978-10983. Epub 2008 Aug 4. PubMed PMID: 18678919; PubMed Central PMCID: PMC2495016
28. Christie JE, Shering A, Ferguson J et al (1981) Physostigmine and arecoline: effects of intravenous infusions in Alzheimer presenile dementia. Br J Psychiatry 138:46-50 (Pubitemid 11197493)
29. Christopoulos A (2002) Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat Rev Drug Discov 1:198-210 (Pubitemid 37361423)
30. Clader JW, Wang Y (2005) Muscarinic receptor agonists and antagonists in the treatment of Alzheimer's disease. Curr Pharm Des 11:3353-3361 (Pubitemid 41300764)
31. Clarke LA, Cassidy CW, Catalano G et al (2004) Psychosis induced by smoking cessation clinic administered anticholinergic overload. Ann Clin Psychiatry 16:171-175 (Pubitemid 39281277)
32. Conn PJ, Jones CK, Lindsley CW (2009) Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol Sci 30:148-155
33. Crook JM, Tomaskovic-Crook E, Copolov DL et al (2000) Decreased muscarinic receptor binding in subjects with schizophrenia: a study of the human hippocampal formation. Biol Psychiatry 48:381-388
34. Crook JM, Tomaskovic-Crook E, Copolov DL et al (2001) Low muscarinic receptor binding in prefrontal cortex from subjects with schizophrenia: a study of Brodmann's areas 8, 9, 10, and 46 and the effects of neuroleptic drug treatment. Am J Psychiatry 158:918-925 (Pubitemid 32547622)
35. Cui YH, Si W, Yin L et al (2008) A novel derivative of xanomeline improved memory function in aged mice. Neurosci Bull 24:251-257
36. Dean B, Crook JM, Opeskin K et al (1996) The density of muscarinic M1 receptors is decreased in the caudate-putamen of subjects with schizophrenia. Mol Psychiatry 1:54-58 (Pubitemid 126442395)
37. Dean B, Crook JM, Pavey G et al (2000) Muscarinic1 and 2 receptor mRNA in the human audateputamen: no change in m1 mRNA in schizophrenia. Mol Psychiatry 5:203-207 (Pubitemid 30229437)
38. Dean B, McLeod M, Keriakous D et al (2002) Decreased muscarinic1 receptors in the dorsolateral prefrontal cortex of subjects with schizophrenia. Mol Psychiatry 7:1083-1091 (Pubitemid 36044267)
39. Dean B, Bymaster FP, Scarr E (2003) Muscarinic receptors in schizophrenia. Curr Mol Med 3:419-426 (Pubitemid 36975101)
40. Deng C, Huang XF. Decreased density of muscarinic receptors in the superior temporal gyrusin schizophrenia. J Neurosci Res 2005 Sep 15;81(6):883-890. PubMed PMID: 16041805 (Pubitemid 41532154)
41. Dickinson D, Coursey RD (2002) Independence and overlap among neurocognitive correlates of community functioning in schizophrenia. Schizophr Res 56:161-170 (Pubitemid 34655478)
42. 2 and M3 receptors. J Pharmacol Exp Ther 242:257-262 (Pubitemid 17112288)
43. Eglen RM (2005) Muscarinic receptor subtype pharmacology and physiology. Prog Med Chem 43:105-136 (Pubitemid 40605496)
44. Felder CC, Bymaster FP, Ward J et al (2000) Therapeutic opportunities for muscarinic receptors in the central nervous system. J Med Chem 43:4333-4353 (Pubitemid 32046857)
45. Fink-Jensen A, Kristensen P, Shannon HE et al (1998) Muscarinic agonists exhibit functional dopamine antagonism in unilaterally 6-OHDA lesioned rats. Neuroreport 9:3481-3486 (Pubitemid 28566134)
46. Fink-Jensen A, Fedorova I, Wortwein G (2003) Role for M5 muscarinic acetylcholine receptors in cocaine addiction. J Neurosci Res 74:91-96 (Pubitemid 37176671)
47. Fisher CM (1991) Visual hallucinations on eye closure associated with atropine toxicity. A neurological analysis and comparison with other visual hallucinations. Can J Neurol Sci 18:18-27
48. Fisher A (2008) Cholinergic treatments with emphasis on M1 muscarinic agonists as potential disease-modifying agents for Alzheimer's disease. Neurotherapeutics 5:433-442 (Pubitemid 351952486)
49. Fisahn A, Yamada M, Duttaroy A, Gan JW, Deng CX, McBain CJ, Wess J. Muscarinic induction of hippocampal gamma oscillations requires coupling of the M1 receptor to two mixed cation currents. Neuron 2002 Feb 14;33(4):615-624. PubMed PMID:11856534 (Pubitemid 34188436)
50. Forster GL, Blaha CD (2003) Pedunculopontine tegmental stimulation evokes striatal dopamine efflux by activation of acetylcholine and glutamate receptors in the midbrain and pons of the rat. Eur J Neurosci 17:751-762 (Pubitemid 36315245)
51. Forster GL, Yeomans JS, Takeuchi J et al (2002) M5 muscarinic receptors are required for prolonged accumbal dopamine release after electrical stimulation of the pons in mice. J Neurosci 22:RC190
52. Fredrickson A, Snyder PJ, Cromer J (2008) The use of effect sizes to characterize the nature of cognitive change in psychopharmacological studies: an example with scopolamine. Hum Psychopharmacol 23:425-436
53. Friedman JI (2004) Cholinergic targets for cognitive enhancement in schizophrenia: focus on cholinesterase inhibitors and muscarinic agonists. Psychopharmacology (Berl) 174:45-53 (Pubitemid 38925090)
54. Frommann I, Pukrop R, Brinkmeyer J et al (2011) Neuropsychological profiles in different at-risk states of psychosis: executive control impairment in the early - and additional memory dysfunction in the late - prodromal state. Schizophr Bull 37(4):861-873
55. Gerber DJ, Sotnikova TD, Gainetdinov RR et al (2001) Hyperactivity, elevated dopaminergic transmission, and response to amphetamine in M1 muscarinic acetylcholine receptor-deficient mice. Proc Natl Acad Sci U S A 98:15312-15317 (Pubitemid 34014011)
56. Gershon S, Olariu J (1960) JB 329 degrees-a new spychotomimetic, its antagonism by tetrahydroaminacrin and its comparison with LSD, mescaline and sernyl. J Neuropsychiatr 1:283-292
57. Giovannini MG (2006) The role of the extracellular signal-regulated kinase pathway in memory encoding. Rev Neurosci 17:619-634 (Pubitemid 46144732)
58. Gold JM, Goldberg RW, McNary SW et al (2002) Cognitive correlates of job tenure among patients with severe mental illness. Am J Psychiatry 159:1395-1402 (Pubitemid 34832723)
59. Gomeza J, Zhang L, Kostenis E et al (1999) Enhancement of D1 dopamine receptor-mediated locomotor stimulation inM4 muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci U S A 96:10483-10488 (Pubitemid 29422585)
60. Granacher RP, Baldessarini RJ (1975) Physostigmine. Its use in acute anticholinergic syndrome with antidepressant and antiparkinson drugs. Arch Gen Psychiatry 32:375-380
61. Gray JA, Moran PM, Grigoryan G (1997) Latent inhibition: the nucleus accumbens connection revisited. Behav Brain Res 88:27-34 (Pubitemid 27459689)
62. Green MF (1996) What are the functional consequences of neurocognitive deficits in schizophrenia? Am J Psychiatry 153:321-330 (Pubitemid 26074706)
63. Hamilton SE, Loose MD, Qi M et al (1997) Disruption of the M1 receptor gene ablates muscarinic receptor-dependent M current regulation and seizure activity in mice. Proc Natl Acad Sci U S A 94:13311-13316 (Pubitemid 27518518)
64. Han M, Newell K, Zavitsanou K et al (2008) Effects of antipsychotic medication on muscarinicM1 receptor mRNA expression in the rat brain. J Neurosci Res 86:457-464 (Pubitemid 351196751)
65. Harries MH, Samson NA, Cilia J et al (1998) The profile of sabcomeline (SB-202026), a functionally selective M1 receptor partial agonist, in the marmoset. Br J Pharmacol 124:409-415 (Pubitemid 28248033)
66. Heinrich JN, Butera JA, Carrick T et al (2009) Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists. Eur J Pharmacol 605:53-56
67. Hemstapat K, Da Costa H, Nong Y et al (2007) A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors. J Pharmacol Exp Ther 322:254-264 (Pubitemid 46956377)
68. Hill K, Mann L, Laws KR et al (2004) Hypofrontality in schizophrenia: a meta-analysis of functional imaging studies. Acta Psychiatr Scand 110:243-256 (Pubitemid 39278982)
69. Hirsch S, Barnes TRE (1995) The clinical treatment of schizophrenia with antipsychotic medication. In: Hirsch SR, Weinberger DR (eds) Schizophrenia. Blackwell Science, Oxford
70. Hoffman DC, Donovan H (1995) Catalepsy as a rodent model for detecting antipsychotic drugs with extrapyramidal side effect liability. Psychopharmacology 120:128-133
71. Howes OD, Kapur S (2009) The dopamine hypothesis of schizophrenia: version III - the final common pathway. Schizophr Bull 35:549-562
72. Hulme EC, Birdsall NJ, Buckley NJ (1990) Muscarinic receptor subtypes. Annu Rev Pharmacol Toxicol 30:633-673 (Pubitemid 20139559)
73. Ichikawa J, Dai J, O'Laughlin IA et al (2002) Atypical, but not typical, antipsychotic drugs increase cortical acetylcholine release without an effect in the nucleus accumbens or striatum. Neuropsychopharmacology 26:325-339 (Pubitemid 34159210)
74. Jones CK, Eberle EL, Shaw DB et al (2005) Pharmacologic interactions between the muscarinic cholinergic and dopaminergic systems in the modulation of prepulse inhibition in rats. J Pharmacol Exp Ther 312:1055-1063 (Pubitemid 40293764)
75. Jones CK, Brady AE, Davis AA et al (2008) Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychoticlike activity in rats. J Neurosci 28:10422-10433
76. Joseph MH, Peters SL, Moran PM et al (2000) Modulation of latent inhibition in the rat by altered dopamine transmission in the nucleus accumbens at the time of conditioning. Neuroscience 101:921-930
77. Joyce EM, Koob GF (1981) Amphetamine-, scopolamine- and caffeine-induced locomotor activity following 6-hydroxydopamine lesions of the mesolimbic dopamine system. Psychopharmacology (Berl) 73:311-313 (Pubitemid 11114112)
78. Kaiser J, Lutzenberger W (2005) Cortical oscillatory activity and the dynamics of auditory memory processing. Rev Neurosci 16:239-254 (Pubitemid 41648184)
79. 2, but not M4, receptor supports its role as autoreceptors in the rat hippocampus. Brain Res Mol Brain Res 67:98-106 (Pubitemid 29170073)
80. Kitaichi K, Day JC et al (1999b) A novel muscarinic M(4) receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M(2) receptor sub-type. Eur J Pharmacol 383:53-56 (Pubitemid 29509822)
81. Kuroki T, Meltzer HY, Icikawa J (1999) Effects of antipsychotic drugs on extracellular dopamine levels in rat medial prefrontal cortex and nucleus accumbens. J Pharmacol Exp Ther 288:774-781 (Pubitemid 29119694)
82. 2 muscarinic antagonist, SCH 72788. Life Sci 2001 Apr 27;68(22-23):2585-2592. PubMed PMID: 11392630 (Pubitemid 32455698)
83. Lazaris A, Bertrand F, Lazarus C, Galani R, Stemmelin J, Poirier R, Kelche C, Cassel JC. Baseline and 8-OH-DPAT-induced release of acetylcholine in the hippocampus of aged rats with different levels of cognitive dysfunction. Brain Res 2003 Mar 28;967(1-2):181-190. PubMed PMID: 12650979 (Pubitemid 36329162)
84. Langmead CJ, Austin NE, Branch CL (2008a) Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1. Br J Pharmacol 154:1104-1115 (Pubitemid 351915055)
85. Langmead CJ, Watson J, Reavill C (2008b) Muscarinic acetylcholine receptors as CNS drug targets. Pharmacol Ther 117:232-243
86. Leach K, Loiacono RE, Felder CC,McKinzie DL, Mogg A, Shaw DB, Sexton PM, Christopoulos A. Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology. 2010 Mar; 35(4):855-869. Epub 2009 Nov 25. PubMed PMID: 19940843; PubMed Central PMCID: PMC3055367
87. Levey AI (1993) Immunological localization of M1-M5 muscarinic acetylcholine receptors in peripheral tissues and brain. Life Sci 52:441-448
88. Levey AI, Kitt CA, Simonds WF et al (1991) Identification and localization of muscarinic acetylcholine receptor proteins in brain with subtype-specific antibodies. J Neurosci 11:3218-3226
89. Li Z, Huang M, Ichikawa J et al (2005) N-desmethylclozapine, a major metabolite of clozapine, increases cortical acetylcholine and dopamine release in vivo via stimulation of M1 muscarinic receptors. Neuropsychopharmacology 30:1986-1995 (Pubitemid 43093499)
90. Li Z, Bonhaus DW, Huang M et al (2007) AC260584 (4-[3-(4-butylpiperidin- 1-yl)-propyl]-7- fluoro-4H-benzo[1,4]oxazin-3-one), a selective muscarinic M1 receptor agonist, increases acetylcholine and dopamine release in rat medial prefrontal cortex and hippocampus. Eur J Pharmacol 572:129-137 (Pubitemid 47429641)
91. Li Z, Snigdha S, Roseman AS et al (2008) Effect of muscarinic receptor agonists xanomeline and sabcomeline on acetylcholine and dopamine efflux in the rat brain; comparison with effects of 4-[3-(4-butylpiperidin-1-yl)-propyl]-7- fluoro-4H-benzo[1,4]oxazin-3-one (AC260584) and Ndesmethylclozapine. Eur J Pharmacol 596:89-97
92. Ma L, Seager MA, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, Regan C, Flick R, Pascarella D, Garson S, Doran S, Kreatsoulas C, Veng L, Lindsley CW, Shipe W, Kuduk S, Sur C, Kinney G, Seabrook GR, Ray WJ. Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proc Natl Acad Sci USA 2009 Sep 15;106 (37):15950-15955. Epub 2009 Aug 26. Erratum in: Proc Natl Acad Sci USA 2009 Oct 20;106(42):18040. Seager, Matthew [corrected to Seager, Matthew A]. PubMed PMID: 19717450; PubMed Central PMCID:PMC2732705
93. Mancama D, Arranz MJ, Landau S et al (2003) Reduced expression of the muscarinic 1 receptor cortical subtype in schizophrenia. Am J Med Genet B Neuropsychiatr Genet 119B:2-6 (Pubitemid 37064044)
94. Marino MJ, Conn PJ (2002) Direct and indirect modulation of the N-methyl D-aspartate receptor. Curr Drug Target CNS Neurol Disord 1:1-16
95. Marino MJ, Rouse ST, Levey AI et al (1998) Activation of the genetically defined M1 muscarinic receptor potentiates N-methyl-D-aspartate (NMDA) receptor currents in hippocampal pyramidal cells. Proc Natl Acad Sci U S A 95:11465-11470 (Pubitemid 28450152)
96. McBain CJ, Mayer ML (1994) N-methyl-D-aspartic acid receptor structure and function. Physiol Rev 74:723-760
97. Mego DM, Omori JM, Hanley JF (1988) Transdermal scopolamine as a cause of transient psychosis in two elderly patients. South Med J 81:394-395
98. Meyer EM, Otero DH (1985) Pharmacological and ionic characterizations of the muscarinic receptors modulating [3H]acetylcholine release from rat cortical synaptosomes. J Neurosci 5:1202-1207 (Pubitemid 15098430)
99. Minzenberg MJ, Poole JH, Benton C et al (2004) Association of anticholinergic load with impairment of complex attention and memory in schizophrenia. Am J Psychiatry 161:116-124 (Pubitemid 38419316)
100. Mirza N, Peters D, Sparks RG (2003) Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists. CNS Drug Rev 9:159-186 (Pubitemid 36903890)
101. Miyakawa T, Yamada M, Duttaroy A, Wess J. Hyperactivity and intact hippocampus-dependent learning in mice lacking the M1 muscarinic acetylcholine receptor. J Neurosci 2001 Jul 15;21 (14):5239-5250. PubMed PMID: 11438599 (Pubitemid 32622949)
102. Moser PC, Hitchcock JM, Lister SD et al (2000) The pharmacology of latent inhibition as an animal model of schizophrenia. Brain Res Rev 33:275-307
103. Neubauer H, Gershon S, Sundland DM (1966) Differential responses to an anticholinergic psychotomimetic (Ditran) in a mixed psychiatric population. Psychiatr Neurol (Basel) 151:65-80
104. Newell KA, Zavitsanou K, Jew SK et al (2007) Alterations of muscarinic and GABA receptor binding in the posterior cingulate cortex in schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 31:225-233 (Pubitemid 44959255)
105. Olianas MC, Maullu C, Onali P (1999) Mixed agonist-antagonist properties of clozapine at different human cloned muscarinic receptor subtypes expressed in Chinese hamster ovary cells. Neuropsychopharmacology 20:263-270 (Pubitemid 29067405)
106. Perlstein WM, Carter CS, Noll DC et al (2001) Relation of prefrontal cortex dysfunction to working memory and symptoms in schizophrenia. Am J Psychiatry 158:1105-1113 (Pubitemid 32623115)
107. Perry EK, Perry RH (1995) Acetylcholine and hallucinations: disease-related compared to druginduced alterations in human consciousness. Brain Cogn 28:240-258
108. Perry KW, Nisenbaum LK, George CA et al (2001) The muscarinic agonist xanomeline increases monoamine release and immediate early gene expression in the rat prefrontal cortex. Biol Psychiatry 49:716-725 (Pubitemid 32328121)
109. Quirion R, Wilson A, Rowe W et al (1995) Facilitation of acetylcholine release and cognitive performance by an M(2)-muscarinic receptor antagonist in aged memory-impaired. J Neurosci 15:1455-1462
110. Raedler TJ, Knable MB, Jones DW et al (2003) In vivo determination of muscarinic acetylcholine receptor availability in schizophrenia. Am J Psychiatry 160:118-127 (Pubitemid 36042435)
111. Raedler TJ, Bymaster FP, Tandon R et al (2007) Towards a muscarinic hypothesis of schizophrenia. Mol Psychiatry 12:232-246 (Pubitemid 46328501)
112. Raffa RB (2009) The M5 muscarinic receptor as possible target for treatment of drug abuse. J Clin Pharm Ther 34:623-629
113. Rasmussen T, Fink-Jensen A, Sauerberg P et al (2001) The muscarinic receptor agonist BuTAC, a novel potential antipsychotic, does not impair learning and memory in mouse passive avoidance. Schizophr Res 49:193-201 (Pubitemid 32434325)
114. Reichenberg A, Caspi A, Harrington H et al (2010) Static and dynamic cognitive deficits in childhood preceding adult schizophrenia: a 30-year study. Am J Psychiatry 167:160-169
115. Riehemann S, Volz HP, StÜtzer P (2001) Hypofrontality in neuroleptic-naive schizophrenic patients during the Wisconsin card sorting test - a fMRI study. Eur Arch Psychiatry Clin Neurosci 251(2):66-71 (Pubitemid 32488034)
116. Rodriguez AL, Nong Y, Sekaran NK (2005) A close structural analog of 2-methyl-6- (phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol Pharmacol 68:1793-1802 (Pubitemid 41654362)
117. Rouse ST, Marino MJ, Potter LT et al (1999) Muscarinic receptor subtypes involved in hippocampal circuits. Life Sci 64:501-509 (Pubitemid 29066699)
118. Rouse ST, Edmunds SM, Yi H (2000) Localization of M(2) muscarinic acetylcholine receptor protein in cholinergic and non-cholinergic terminals in rat hippocampus. Neurosci Lett 284:182-186 (Pubitemid 30204543)
119. 2 receptor antagonist, on improving spatial memory performance in aged cognitively impaired rats. Behav Brain Res 145:171-178 (Pubitemid 37188642)
120. Russig H, Murphy CA, Feldon J (2002) Clozapine and haloperidol reinstate latent inhibition following its disruption during amphetamine withdrawal. Neuropsychopharmacology 26:765-777 (Pubitemid 34455029)
121. Scarr E, Sundram S, Keriakous D (2007) Altered hippocampal muscarinic M4, but not M1, receptor expression from subjects with schizophrenia. Biol Psychiatr 61:1161-1170 (Pubitemid 46669465)
122. Schwarz RD, Callahan MJ, Coughenour LL et al (1999) Milameline (CI-979/RU35926): a muscarinic receptor agonist with cognition-activating properties: biochemical and in vivo characterization. J Pharmacol Exp Ther 291:812-822 (Pubitemid 29503557)
123. 2 muscarinic acetylcholine receptor knock-out mice show deficits in behavioral flexibility, working memory, and hippocampal plasticity. J Neurosci 24:10117-10127 (Pubitemid 39492037)
124. Sellin AK, Shad M, Tamminga C (2008) Muscarinic agonists for the treatment of cognition in schizophrenia. CNS Spectr 13:985-996
125. Senda T, Matsuno K, Kobayashi T et al (1997) Reduction of scopolamine-induced impairment of passive-avoidance performance by s-receptor agonist in mice. Physiol Behav 61:257-264 (Pubitemid 27085557)
126. Shannon HE, Hart JC, Bymaster FP et al (1999) Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats. J Pharmacol Exp Ther 290:901-907 (Pubitemid 29355112)
127. Shannon HE, Rasmussen K, Bymaster FP et al (2000) Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice. Schizophr Res 42:249-259 (Pubitemid 30216536)
128. Shekhar A, Potter WZ, Lightfoot J et al (2008) Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry 165:1033-1039
129. Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol Pharmacol 2009 Aug;76(2):356-368. Epub 2009 Apr 30. PubMed PMID: 19407080; PubMed Central PMCID: PMC2713127
130. Shirey JK, Xiang Z, Orton D et al (2008) An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat Chem Biol 4:42-50 (Pubitemid 350273654)
131. Shirey JK, Brady AE, Jones PJ et al (2009) A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. J Neurosci 29:14271-14286
132. Shinoe T, Matsui M, Taketo MM, Manabe T. Modulation of synaptic plasticity by physiological activation of M1 muscarinic acetylcholine receptors in the mouse hippocampus. J Neurosci 2005 Nov 30;25(48):11194-11200. PubMed PMID: 16319319 (Pubitemid 43089564)
133. Schmitt GJ, Meisenzahl EM, Dresel S, Tatsch K, Rossmuller B, Frodl T, Preuss UW, Hahn K, Moller HJ. Striatal dopamine D2 receptor binding of risperidone in schizophrenic patients as assessed by 123I-iodobenzamide SPECT: a comparative study with olanzapine. J Psychopharmacol 2002 Sep;16(3):200-206. PubMed PMID: 12236625 (Pubitemid 34983073)
134. Spalding TA, Ma J-N, Ott TR et al (2006) Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and Ndesmethylclozapine: evidence for three distinct modes of receptor activation. Mol Pharmacol 70:1974-1983 (Pubitemid 44771913)
135. Spencer KM, Nestor PG, Niznikiewicz MA et al (2003) Abnormal neural synchrony in schizophrenia. J Neurosci 23:7407-7411 (Pubitemid 36999532)
136. Spencer KM, Nestor PG, Perlmutter R et al (2004) Neural synchrony indexes disordered perception and cognition in schizophrenia. Proc Natl Acad Sci U S A 101:17288-17293 (Pubitemid 39627812)
137. Stanhope KJ, Mirza NR, Bickerdike MJ et al (2001) The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J Pharmacol Exp Ther 299:782-792
138. Stoll C, Schwarzwälder U, Johann S et al (2003) Characterization of muscarinic autoreceptors in the rabbit hippocampus and caudate nucleus. Neurochem Res 28:413-417 (Pubitemid 36314826)
139. Stahl E, Ellis J. Novel allosteric effects of amiodarone at the muscarinic M5 receptor. J Pharmacol Exp Ther 2010 Jul;334(1):214-222. Epub 2010 Mar 26. PubMed PMID: 20348203; PubMed Central PMCID: PMC2912050
140. Sur C, Kinney GG (2005) Selective Targeting of Muscarinic Receptors: Novel Therapeutic Approaches for Psychotic Disorders. Current Neuropharmacology 3:63-71 (Pubitemid 40246719)
141. Sur C, Mallorga PJ, Wittmann M et al (2003) N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate
142. Tzavara ET, Bymaster FP, Davis RJ et al (2004)M4 muscarinic receptors regulate the dynamics of cholinergic and dopaminergic neurotransmission: relevance to the pathophysiology and treatment of related CNS pathologies. FASEB J 18:1410-1412 (Pubitemid 39561597)
143. Vannucchi MG, Pepeu G. Muscarinic receptor modulation of acetylcholine release from rat cerebral cortex and hippocampus. Neurosci Lett 1995 Apr 28;190(1):53-56. PubMed PMID: 7624055
144. Vannucchi MG, Scali C, Kopf SR et al (1997) Selective muscarinic antagonists differentially affect in vivo acetylcholine release and memory performances of young and aged rats. Neuroscience 79:837-846 (Pubitemid 27292679)
145. 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 122:570-575 (Pubitemid 351787835)
146. Vilaro MT, Palacios JM, Mengod G (1994) Multiplicity of muscarinic autoreceptor subtypes? Comparison of the distribution of cholinergic cells and cells containing mRNA for five subtypes of muscarinic receptors in the rat brain. Brain Res Mol Brain Res 21:30-46
147. Vilaró MT, Palacios JM, Mengod G (1990) Localization of M5 muscarinic receptor mRNA in rat brain examined by in situ hybridization histochemistry. Neurosci Lett 114:154-159 (Pubitemid 20188950)
148. Wall SJ, Yasuda RP, Hory F (1991) Production of antisera selective for M1 muscarinic receptors using fusion proteins: distribution of M1 receptors in rat brain. Mol Pharmacol 39:643-649
149. 2 muscarinic receptor antagonists. J Med Chem 45:5415-5418 (Pubitemid 35424957)
150. Wang H, Ng K, Hayes D et al (2004) Decreased amphetamine-induced locomotion and improved latent inhibition in mice mutant for the M5 muscarinic receptor gene found in the human 15q schizophrenia region. Neuropsychopharmacology 29:2126-2139 (Pubitemid 39578903)
151. Weinberger DR, Berman KF, Zec RF (1986) Physiologic dysfunction of dorsolateral prefrontal cortex in schizophrenia: I. Regional cerebral blood flow evidence. Arch Gen Psychiatry 43:114-124 (Pubitemid 16163530)
152. Weiner DM, Levey AI, Brann MR (1990) Expression of muscarinic acetylcholine and dopamine receptor mRNAs in rat basal ganglia. Proc Natl Acad Sci U S A 87:7050-7054
153. Weiner DM, Meltzer HY, Veinbergs I et al (2004) The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine. Psychopharmacol 177:207-216 (Pubitemid 40109932)
154. Wess J (1996) Molecular biology of muscarinic acetylcholine receptors. Crit Rev Neurobiol 10:69-99 (Pubitemid 26283956)
155. Wess J, Duttaroy A, Zhang W et al (2003) M1-M5 muscarinic receptor knockout mice as novel tools to study the physiological roles of the muscarinic cholinergic system. Receptors Channels 9:279-290 (Pubitemid 37069448)
156. Wienrich M, Ceci A, Ensinger HA et al (2002) Talsaclidine (WAL 2014 FU): a muscarinic M1 receptor agonist for the treatment of Alzheimer's disease. Drug Develop Res 56:321-334 (Pubitemid 35168309)
157. Williams LM, Whitford TJ, Flynn G et al (2008) General and social cognition in first episode schizophrenia: identification of separable factors and prediction of functional outcome using the IntegNeuro test battery. Schizophr Res 99:182-191 (Pubitemid 351255579)
158. Winkler J, Thal LJ, Gage FH et al (1998) Cholinergic strategies for Alzheimer's disease. J Mol Med 76:555-567
159. Wolkin A, Sanfilipo M, Wolf AP et al (1992) Negative symptoms and hypofrontality in chronic schizophrenia. Arch Gen Psychiatry 49:959-965
160. Yeomans JS (1995) Role of tegmental cholinergic neurons in dopaminergic activation, antimuscarinic psychosis and schizophrenia. Neuropsychopharmacology 12:3-16
161. Yeomans JS, Forster G, Blaha C (2001) M5 muscarinic receptors are needed for slow activation of dopamine neurons and for rewarding brain stimulation. Life Sci 68:2449-2456 (Pubitemid 32455681)
162. Zavitsanou K, Katsifis A, Mattner F et al (2004) Investigation of M1/M4 muscarinic receptors in the anterior cingulate cortex in schizophrenia, bipolar disorder, and major depression disorder. Neuropsychopharmacology 29:619-625
163. 2/M4 muscarinic receptor binding in the anterior cingulate cortex in schizophrenia and mood disorders. Brain Res Bull 65:397-403
164. Zhang W, Yamada M, Gomeza J et al (2002a) Multiple muscarinic acetylcholine receptor subtypes modulate striatal dopamine release, as studied with M1-M5 muscarinic receptor knockout mice. J Neurosci 22:6347-6352 (Pubitemid 35386389)
165. Zhang W, Basile AS, Gomeza J et al (2002b) Characterization of central inhibitory muscarinic autoreceptors by the use of muscarinic acetylcholine receptor knock-out mice. J Neurosci 22:1709-1717 (Pubitemid 35386289)