Development of M1 subtype selective muscarinic agonists for Alzheimer's disease: Translation of in vitro selectivity into in vivo efficacy

Drug Development Research

Volumn 40, Issue 2, 1997, Pages 133-143

  Schwarz, R D ^a   Callahan, M J ^a   Davis, R E ^a   Jaen, J C ^a   Tecle, H ^a  

^a PFIZER INC   (United States)

Author keywords

Clonal cell lines; Receptor binding; Second messengers; Spatial working memory

Indexed keywords

3 [3 (3 METHOXYPHENYL) 2 PROPYNYLOXYIMINO] 1 AZABICYCLO[2.2.1]HEPTANE; [4 [(3 CHLOROPHENYL)CARBAMOYLOXY] 2 BUTYNYL]TRIMETHYLAMMONIUM; ARECOLINE; CARBACHOL; MUSCARINIC AGENT; MUSCARINIC M1 RECEPTOR; OXOTREMORINE; PILOCARPINE; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; CHOLINERGIC ACTIVITY; CONTROLLED STUDY; DRUG DESIGN; DRUG RECEPTOR BINDING; ELECTROENCEPHALOGRAM; IN VITRO STUDY; MONKEY; NONHUMAN; ORAL DRUG ADMINISTRATION; RAT; REVIEW; SALIVATION; SPATIAL MEMORY;

EID: 0030928436     PISSN: 02724391     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1098-2299(199702)40:2<133::AID-DDR4>3.0.CO;2-M     Document Type: Review

References (67)

1. Alexander DA (1973): Attention dysfunction in senile dementia. Psychol Rep 32:229-230.
2. Bartus RT, Dean RL, Beer B, Lippa AS (1982): The cholinergic hypothesis of geriatric memory dysfunction. Science 217:408-417.
3. Beattv WW, Bierley RA (1986): Scopolamine impairs encoding and retrieval of spatial working memory in rats. Physiol Psychol 14:82-86.
4. Bonner TI, Buckley J, Young A, Brann MR (1987): Identification of a family of muscarinic receptor genes. Science 237:527-532.
5. Bonner TI, Young AC, Brann MR, Buckley NJ (1988): Cloning and expression of the human and rat m5 muscarinic receptor genes. Neuron 1:403-410.
6. Brann MR, Buckley NJ, Bonner TI (1988): The striatum and cerebral cortex express different muscarinic receptor mRNAs. FEBS Lett 230:90-94.
7. Brauner-Osborne H, Ebert B, Brann MR, Falch E, Krogsgaard Larsen P (1995): Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. J Med Chem 38:2188-2195.
8. Bruno G, Mohr E, Gillespie M, Fedio P, Chase TN (1986): Muscarinic agonist therapy of Alzheimer's disease: a clinical trial of RS-86. Arch Neurol 43:659-661.
9. Buckley NJ, Bonner TI, Buckley CM, Brann MR (1989): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells. Mol Pharmacol 35:469-476.
10. Burstein ES, Spalding TA, Hill Eubanks D, Brann MR (1995): Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins. J Biol Chem 270:3141-3146.
11. Caine ED (1980): Cholinomimetic treatment fails to improve memory disorders. N Engl J Med 303:585-586.
12. Callahan MJ, Kinsora JJ, Harbaugh RE, Reeder TM, Davis RE (1993): Continuous ICV infusion of scopolamine impairs sustained attention of rhesus monkeys. Neurobiol Aging 14:147-151.
13. Caulfield MP (1993): Muscarinic receptors-characterization, coupling, and function. Pharmacol Ther 58:319-379.
14. 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.
15. Davis KL, Hollander E, Davidson M, Davis BM, Mohs RC, Horvath TB (1987): Induction of depression with oxotremorine in patients with Alzheimer's disease. Am J Psychiatry 144:468-471.
16. Davis RE, Raby C, Callahan MJ, Lipinski W, Schwarz R, Dudley D, Lauffer D, Reece P, Jaen J, Tecle H (1993): Subtype selective muscarinic agonists: potential therapeutic agents for Alzheimer's disease. Prog Brain Res 98:439-445.
17. Davis RE, Doyle PD, Carroll RT, Emmerling MR, Jaen JC (1995): Cholinergic therapies for Alzheimer's disease: palliative or disease altering? Arzneim Forsch 45:425-431.
18. Dilsaver SC, Alessi NE. (1988): Temperature as a dependent variable in the study of cholinergic mechanisms. Prog Neuropsychopharmacol Biol Psychiatry 12:1-32.
19. Gauthier S, Leblanc R, Robitaille Y, Quirion R, Carlsson G, Beaulieu M, Bouchard R, Dastoor D, Ervin F, Gauthier L, et al. (1986): Transmitter-replacement therapy in Alzheimer's disease using intracerebroventricular infusions of receptor agonists [published erratum appears in Can J Neurol Sci 1987;14:189]. Can J Neurol Sci 13:394-402.
20. Harbaugh RE, Roberts DW, Coombs DW, Saunders RL, Reeder TM (1984): Preliminary report: intracranial cholinergic drug infusion in patients with Alzheimer's disease. Neurosurgery 15:514-518.
21. Harbaugh RE, Reeder TM, Senter HJ, Knopman DS, Baskin DS, Pirozzolo F, Chui HC, Shetter AG, Bakay RA, Leblanc R, et al. (1989): Intracerebroventricular bethanechol chloride infusion in Alzheimer's disease: results of a collaborative double-blind study. J Neurosurg 71:481-186.
22. Hollander E, Davidson M, Mohs RC, Horvath TB, Davis BM, Zemishlany Z, Davis KL (1987): RS86 in the treatment of Alzheimer's disease: cognitive and biological effects. Biol Psychiatry 22:1067-1078.
23. Horowitz ZP, Chow MI (1962): Effects of centrally acting drugs on the correlation of electro cortical activity and wakefulness of cats. J Pharmacol Exp Ther 137:127-132.
24. Hulme EC, Birdsall NJM, Buckley NJ (1990): Muscarinic receptor subtypes. Annu Rev Pharmacol Toxicol 30:633-673.
25. Jaen J, Schwarz RD (1997): Development of muscarinic agonists for the symptomatic treatment of Alzheimer's disease. In Brioni JD, Decker MW (eds): Pharmacological Treatment of Alzheimer's Disease. John Wiley & Sons, NY.
26. Jaen J, Barrett S, Brann M, Callahan M, Davis R, Doyle P, Eubanks D, Lauffer D, Lauffer L, Lipinski W, Moreland D, Nelson C, Raby C, Schwarz R, Spencer C, Tecle H (1995): In vitro and in vivo evaluation of the subtype selective muscarinic agonist PD151832. Life Sci 56:845-852.
27. Knapp MJ, Knopman DS, Soloman PR, Pendlebury WW, Davis CS, Gracon SI, and the Tacrine Study Group (1994): A 30 week randomized controlled trial of high-dose tacrine in patients with Alzheimer's disease. JAMA 271:985-991.
28. Kumar V, Calache M (1991): Treatment of Alzheimer's disease with cholinergic drugs. Int J Clin Pharmacol Ther Toxicol 29:23-37.
29. Kubo T, Fukuda K, Mikami A, Maeda A, Takahashi H, Mishina M, Haga K, Ichiyama A, Kangawa K, Kojima M, Matsuo H, Hirose T, Numa S (1986a): Cloning, sequencing and expression of complementary DNA encoding the muscarinic acetylcholine receptor. Nature 323:411-416.
30. Kubo T, Maeda A, Sugimoto K, Akiba I, Mikami A, Takahashi H, Haga T, Haga K, Ichiyama A, Kangawa K, Matsuo H, Mishina M, Hirose T, Numa S (1986b): Primary structure of porcine cardiac muscarinic acetylcholine receptor deduced from the cDNA sequence. FEBS Lett 209:367-372.
31. Lazareno S, Farries T, Birdsall NJ (1993): Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors m1-m4. Life Sci 52:449-456.
32. Levey AI, Kitt CA, Simonds WF, Price DL, Brann MR (1991): Identification and localization of muscarinic acetylcholine receptor proteins in brain with subtype-specific antibodies. J Neurosci 11:3218-3226.
33. Li M, RP Yasuda, Wall SJ, Wellstein A, Wolfe BB (1991): Distribution of m2 muscarinic receptors in rat brain using antisera selective for m2 receptors. Mol Pharmacol 40:28-35.
34. Mash DC, Flynn DD, Potter LT (1985): Loss of M2 muscarine receptors in the cerebral cortex in Alzheimer's disease and experimental denervation. Science 228:1115-1117.
35. Mouradian MM, Mohr E, Williams JA, Chase TN (1988): No response to high-dose muscarinic agonist therapy in Alzheimer's disease. Neurology 38:606-608.
36. Nabeshima T, Ogawa SI, Nishimura H, Fuji K, Kameyama T, Sasaki Y (1991): Stauro sporine facilitates recovery from the basal forebrain-lesion-induced impairment of learning and deficit of cholinergic neuron in rats. J Pharmacol Exp Ther 257:562-566.
37. Nathanson NM (1987): Molecular properties of the muscarinic acetylcholine receptor. Annu Rev Neurosci 10:195-236.
38. Natori K, Okazaki Y, Irie T, Katsube J (1990): Pharmacological and biochemical assessment of SM-10888, a novel cholinesterase inhibitor. Jpn J Pharmacol 53:145-155.
39. Palacios JM, Bolliger G, Glosse A, Enz A, Gmelin G, Malanowski J (1986): The pharmacological assessment of RS-86 (2-ethyl-8-methyl2,8-diazaspiro-[4,5]-decan-1,3-dion hydrobromide). A potent, specific muscarinic acetylcholine receptor agonist. Eur J Pharmacol 125:45-62.
40. Pearce B, Potter LT (1991): Coupling of m1 muscarinic receptors to G-proteins in Alzheimer's disease. Alzheimer Dis Assoc Disord 5:163-172.
41. Parrott AC (1986): The effects of transdermal scopolamine and four dose levels of oral scopolamine (0.15, 0.3, 0.6 and 1.2 mg) upon psychological performance. Psychopharmacology 89:347-354.
42. Penn RD, Martin EM, Wilson RS, Fox JH, Savoy SM (1988): Intraventricular bethanechol infusion for Alzheimer's disease: results of double-blind and escalating-dose trials. Neurology 38:219-222.
43. Peralta EG, Ashkenazi A, Winslow JW, Smith DH, Ramachandran J, Capon DJ (1987a): Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J 6:3923-3929.
44. Peralta EG, Winslow JW, Peterson GL, Smith DH, Ashkenazi A, Ramachandran J, Schimerlick MI, Capon DJ (1987b): Primary structure and biochemical properties of an M2 muscarinic receptor. Science 236:600-605.
45. Peralta EG, Ashkenazi A, Winslow JW, Ramachandran J, Capon DJ (1988): Differential regulation of PI hydrolysis and adenylyl cyclase by muscarinic receptor subtypes. Nature 334:434-137.
46. Perry EK, Tomlinson BE, Blessed G, Bergmann K, Gibson P, Perry RH (1978): Correlation of cholinergic abnormalities with senile plaques and mental test scores in dementia. Br Med J 2:1457-1459.
47. Raffaele KC, Berardi A, Morris PP, Asthana S, Haxby JV, Schapiro MB, Rapoport SI and Soncrant TT (1991): Effects of acute infusion of the muscarinic cholinergic agonist arecoline on verbal memory and visuo-spatial function in dementia of the Alzheimer type. Prog Neuropsychopharmacol Biol Psychiatry 15:643-648.
48. Richards MH (1991): Pharmacology and second messenger interactions of cloned muscarinic receptors. Biochem Pharmacol 42:1645-1653.
49. Richards MH, van Giersbergen PLM (1995): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists. Br J Pharmacol. 114:1241-1249.
50. Schwarz RD, Davis RE, Jaen JC, Spencer CJ, Tecle H, Thomas AJ (1993): Characterization of muscarinic agonists in recombinant cell lines. Life Sci 52:465-172.
51. Sedman AJ, Bockbrader H, Schwarz RD (1995): Preclinical and phase I clinical characterization of CI-979/RU35926, a novel muscarinic agonist for the treatment of Alzheimer's disease. Life Sci 56:877-882.
52. Shannon HE, Bymaster FP, Calligaro DO, Greenwood B, Mitch CH, Sawyer BD, Ward JS, Wong DT, Olesen PH, Sheardown MJ, Swedberg MDB, Suzdak PD, Sauerberg P (1994): Xanomeline: a novel muscarinic receptor agonist with functional selectivity for m1 receptors. J Pharmacol Exp Ther 269:271-281.
53. Soncrant TT, Raffaele KC, Asthana S, Berardi A, Morris PP, Haxby JV (1993): Memory improvement without toxicity during chronic, low dose intravenous arecoline in Alzheimer's disease. Psychopharmacology 112:421-427.
54. Spencer PSJ (1965): Activity of centrally acting and other drugs against tremor and hypothermia induced in mice by tremorine. Br J Pharmacol 25:442-455.
55. Starke K, Gothert M, Kilbinger H (1989): Modulation of neurotransmitter release by pre synaptic autoreceptors. Physiol Rev 69:865-962.
56. Stewart BR, Jenner P, Marsden CD (1989): Assessment of the muscarinic receptor sub type involved in the mediation of pilocarpine-induced purposeless chewing behaviour. Psychopharmacology 97:1228-1234.
57. Symons JP, Davis RE, Marriott JG (1988): Water maze learning and effects of cholinergic drugs in mouse strains with high and low hippocampal pyramidal cell counts. Life Sci 42:375-383.
58. Tariot PN, Cohen RM, Welkowitz JA, Sunderland T, Newhouse PA, Murphy DL, Weingartner H (1988): Multiple-dose arecoline infusions in Alzheimer's disease. Arch Gen Psychiatry 45:901-905.
59. Wall SJ, Yasuda RP, Hory F, Flagg S, Martin BM, Ginnis EI, Wolfe BB (1991): Production of antisera selective for ml muscarinic receptors using fusion proteins: distribution of m1 receptors in rat brain. Mol Pharmacol 39:643-649.
60. Wang SZ, El-Fakahany EE (1993): Application of transfected cell lines in studies of functional receptor subtype selectivity of muscarinic agonists. J Pharmacol Exp Ther 266:237-243.
61. Wei J, Walton EA, Milici A, Buccafusco JJ (1994): m1-m5 Muscarinic receptor distribution in rat CNS by RT-PCR and HPLC. J Neurochem 63:815-821.
62. Wesnes K, Warburton DM (1983): Effects of scopolamine on stimulus sensitivity and response bias in a visual vigilance task. Neuropsychobiology 9:154-157.
63. Wesnes K, Warburton DM (1984): Effects of scopolamine and nicotine on human rapid information processing performance. Psychopharmacology 82:147-150.
64. Wettstein A, Spiegel R (1984): Clinical trials with the cholinergic drug RS 86 in Alzheimer's disease (AD) and senile dementia of the Alzheimer type (SDAT). Psychopharmacology 84:572-573.
65. Whishaw IQ, O'Connor WT, Dunnett SB (1985): Disruption of central cholinergic systems in the rat by basal forebrain lesions or atropine: effects on feeding, sensorimotor behaviour, locomotor activity and spatial navigation. Behav Brain Res 17:103-115.
66. Whitehouse P, Price D, Strubble R, Clark A, Coyle J, DeLong M (1982): Alzheimer's disease and senile dementia: loss of neurons in the basal forebrain. Science 215:1237-1239.
67. Yamamoto J (1988): Roles of cholinergic, dopaminergic, noradrenergic, serotonergic and GABAergic systems in changes of the EEG power spectra and behavioral states in rabbits. Jpn J Pharmacol 47:123-134.