A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning

Molecular Pharmacology

Volumn 76, Issue 2, 2009, Pages 356-368

  Sheffler, Douglas J ^a   Williams, Richard ^a,b   Bridges, Thomas M ^a   Xiang, Zixiu ^a   Kane, Alexander S ^a   Byun, Nellie E ^b   Jadhav, Satyawan ^a,b   Mock, Mathew M ^d   Zheng, Fang ^d   Lewis, L Michelle ^a   Jones, Carrie K ^a,b,c   Niswender, Colleen M ^a,b   Weaver, Charles D ^a,b   Lindsley, Craig W ^a,b   Conn, P Jeffrey ^a,b  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^c DEPARTMENT OF VETERANS AFFAIRS   (United States)

^d UNIVERSITY OF ARKANSAS MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBACHOL; MUSCARINIC AGENT; MUSCARINIC M1 RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; N [3 OXO 3 [4 (PYRIDINE 4 YL)PIPERAZIN 1 YL]PROPYL]BENZO[C][1,2,5]THIADIAZOLE 4 SULFONAMIDE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; PILOCARPINE; RADIOLIGAND; UNCLASSIFIED DRUG; VU 0255035;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN; COGNITIVE DEFECT; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG EFFICACY; DRUG INHIBITION; FREEZING; HIPPOCAMPUS; LEARNING; MALE; MOUSE; MUTAGENESIS; NONHUMAN; PATCH CLAMP; PRIORITY JOURNAL; PYRAMIDAL NERVE CELL; RAT; WHOLE CELL;

ANIMALS; BINDING, COMPETITIVE; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROPHYSIOLOGY; HIPPOCAMPUS; INHIBITORY CONCENTRATION 50; LEARNING; MALE; MICE; MOLECULAR STRUCTURE; MUSCARINIC ANTAGONISTS; PATCH-CLAMP TECHNIQUES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, MUSCARINIC M1; SEIZURES; SENSITIVITY AND SPECIFICITY; SULFONAMIDES; THIADIAZOLES;

EID: 67650837952     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.109.056531     Document Type: Article

References (40)

1. Anagnostaras SG, Maren S, and Fanselow MS (1995) Scopolamine selectively disrupts the acquisition of contextual fear conditioning in rats. Neurobiol Learn Mem 64:191-194.
2. Anagnostaras SG, Murphy GG, Hamilton SE, Mitchell SL, Rahnama NP, Nathanson NM, and Silva AJ (2003) Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice. Nat Neurosci 6:51-58. (Pubitemid 36026332)
3. Arunlakshana O and Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol Chemother 14:48-58.
4. Brocks DR (1999) Anticholinergic drugs used in Parkinson's disease: An overlooked class of drugs from a pharmacokinetic perspective. J Pharm Pharm Sci 2:39-46.
5. Bymaster FP, Carter PA, Yamada M, Gomeza J, Wess J, Hamilton SE, Nathanson NM, McKinzie DL, and Felder CC (2003a) 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)
6. Bymaster FP and Falcone JF (2000) Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium. Eur J Pharmacol 390:245-248.
7. Bymaster FP, Felder CC, Tzavara E, Nomikos GG, Calligaro DO, and Mckinzie DL (2003b) Muscarinic mechanisms of antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry 27:1125-1143.
8. Conn PJ, Jones CK, and Lindsley CW (2009) Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol Sci 30:148-155.
9. Conn PJ and Sanders-Bush E (1986) Biochemical characterization of serotonin stimulated phosphoinositide turnover. Life Sci 38:663-669.
10. Drachman DA and Leavitt J (1974) Human memory and the cholinergic system. A relationship to aging? Arch Neurol 30:113-121.
11. Felder CC, Bymaster FP, Ward J, and DeLapp N (2000) Therapeutic opportunities for muscarinic receptors in the central nervous system. J Med Chem 43:4333-4353. (Pubitemid 32046857)
12. Fornari RV, Moreira KM, and Oliveira MG (2000) Effects of the selective M1 muscarinic receptor antagonist dicyclomine on emotional memory. Learn Mem 7:287-292. (Pubitemid 30783670)
13. Hagan JJ, Jansen JH, and Broekkamp CL (1987) Blockade of spatial learning by the M1 muscarinic antagonist pirenzepine. Psychopharmacology (Berl) 93:470-476.
14. Hamilton SE, Loose MD, Qi M, Levey AI, Hille B, McKnight GS, Idzerda RL, and Nathanson NM (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)
15. Hersch SM, Gutekunst CA, Rees HD, Heilman CJ, and Levey AI (1994) Distribution of m1-m4 muscarinic receptor proteins in the rat striatum: light and electron microscopic immunocytochemistry using subtype-specific antibodies. J Neurosci 14:3351-3363.
16. Holden M and Kelly C (2002) Use of cholinesterase inhibitors in dementia. Adv Psychiatr Treatment 8:89-96.
17. Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, et al. (2008) Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci 28:10422-10433.
18. Karlsson E, Jolkkonen M, Mulugeta E, Onali P, and Adem A (2000) Snake toxins with high selectivity for subtypes of muscarinic acetylcholine receptors. Biochimie 82:793-806. (Pubitemid 30843361)
19. Kennedy JP, Williams L, Bridges TM, Daniels RN, Weaver D, and Lindsley CW (2008) Application of combinatorial chemistry science on modern drug discovery. J Comb Chem 10:345-354.
20. Langmead CJ, Watson J, and Reavill C (2008) Muscarinic acetylcholine receptors as CNS drug targets. Pharmacol Ther 117:232-243.
21. Leister W, Strauss K, Wisnoski D, Zhao Z, and Lindsley C (2003) Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries. J Comb Chem 5:322-329. (Pubitemid 37140578)
22. Levey AI, Kitt CA, Simonds WF, Price DL, and Brann MR (1991) Identification and localization of muscarinic acetylcholine receptor proteins in brain with subtype-specific antibodies. J Neurosci 11:3218-3226.
23. Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, et al. (2008) Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorg Med Chem Lett 18:885-890. (Pubitemid 351179367)
24. Maresca A and Supuran CT (2008) Muscarinic acetylcholine receptors as therapeutic targets for obesity. Expert Opin Ther Targets 12:1167-1175.
25. Marino MJ, Rouse ST, Levey AI, Potter LT, and Conn PJ (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.
26. Messer WS Jr. (2002) The utility of muscarinic agonists in the treatment of Alzheimer's disease. J Mol Neurosci 19:187-193. (Pubitemid 35013354)
27. Miyakawa T, Yamada M, Duttaroy A, and Wess J (2001) Hyperactivity and intact hippocampus-dependent learning in mice lacking the M1 muscarinic acetylcholine receptor. J Neurosci 21:5239-5250. (Pubitemid 32622949)
28. Phillips RG and LeDoux JE (1992) Differential contribution of amygdala and hippocampus to cued and contextual fear conditioning. Behav Neurosci 106:274-285.
29. Pisani A, Bernardi G, Ding J, and Surmeier DJ (2007) Re-emergence of striatal cholinergic interneurons in movement disorders. Trends Neurosci 30:545-553. (Pubitemid 47513239)
30. Porter AC, Bymaster FP, DeLapp NW, Yamada M, Wess J, Hamilton SE, Nathanson NM, and Felder CC (2002) M1 muscarinic receptor signaling in mouse hippocampus and cortex. Brain Res 944:82-89. (Pubitemid 34775011)
31. Potter LT, Flynn DD, Liang JS, and McCollum MH (2004) Studies of muscarinic neurotransmission with antimuscarinic toxins. Prog Brain Res 145:121-128.
32. Potter LT and Purkerson SL (1995) Pharmacology of striatal muscarinic receptors, in Molecular and Cellular Mechanisms of Neostriatal Function (Ariano M and Surmeier J eds) pp 241-254, R.G. Landes Co., New York.
33. Rouse ST, Hamilton SE, Potter LT, Nathanson NM, and Conn PJ (2000) Muscarinic-induced modulation of potassium conductances is unchanged in mouse hippocampal pyramidal cells that lack functional M1 receptors. Neurosci Lett 278:61-64.
34. Rouse ST, Marino MJ, Potter LT, Conn PJ, and Levey AI (1999) Muscarinic receptor subtypes involved in hippocampal circuits. Life Sci 64:501-509. (Pubitemid 29066699)
35. Santiago MP and Potter LT (2001) Biotinylated m4-toxin demonstrates more M4 muscarinic receptor protein on direct than indirect striatal projection neurons. Brain Res 894:12-20.
36. Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, et al. (2008) An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat Chem Biol 4:42-50. (Pubitemid 350273654)
37. Spalding TA, Ma JN, Ott TR, Friberg M, Bajpai A, Bradley SR, Davis RE, Brann MR, and Burstein ES (2006) Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation. Mol Pharmacol 70:1974-1983. (Pubitemid 44771913)
38. Sur C, Mallorga PJ, Wittmann M, Jacobson MA, Pascarella D, Williams JB, Brandish PE, Pettibone DJ, Scolnick EM, and Conn PJ (2003) N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc Natl Acad Sci U S A 100:13674-13679. (Pubitemid 37444798)
39. Wess J (2004) Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implications. Annu Rev Pharmacol Toxicol 44:423-450.
40. Wess J, Eglen RM, and Gautam D (2007) Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development. Nat Rev Drug Discov 6:721-733. (Pubitemid 47342315)