WAY-131256 is an orally active, efficacious, and in vivo functionally selective M1 agonist

Drug Development Research

Volumn 40, Issue 2, 1997, Pages 185-192

  Sabb, Annmarie L ^a   Stein, Reinhardt P ^a   Vogel, Robert L ^a   Tasse, Rene ^a   Amburn, Susan ^a   Fairman, Denise K ^a   Kowal, Dianne ^a   Malhotra, Deepa ^a   Boast, Carl A ^a   Bartolomeo, Adam ^a   Morris, Herman ^a   Sailer, Tracy ^a   Moyer, John A ^a   Abou Gharbia, Magid ^a   Ho, Douglas M ^b  

^a PFIZER INC   (United States)

^b PRINCETON UNIVERSITY   (United States)

Author keywords

Alzheimer's disease; Cabamates; Carbachol; Muscarinic receptors; Phophoinositide turnover; Xanomeline

Indexed keywords

AZABICYCLO[2.2.1]HEPTANE 3 METHYLCARBAMATE; CARBACHOL; MUSCARINIC AGENT; MUSCARINIC M1 RECEPTOR; MUSCARINIC RECEPTOR; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG; WAY 131256; XANOMELINE;

ALZHEIMER DISEASE; AMNESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD PRESSURE; CHO CELL; COMPUTER MODEL; CONTROLLED STUDY; DRUG DESIGN; DRUG RECEPTOR BINDING; HEART RATE; HUMAN; IN VITRO STUDY; INTRAPERITONEAL DRUG ADMINISTRATION; LACRIMATION; NONHUMAN; ORAL DRUG ADMINISTRATION; PHOSPHOINOSITIDE METABOLISM; RECEPTOR AFFINITY; RECEPTOR BINDING; RECEPTOR DENSITY; STRUCTURE ACTIVITY RELATION;

EID: 0031011836     PISSN: 02724391     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1098-2299(199702)40:2<185::AID-DDR8>3.0.CO;2-H     Document Type: Article

References (24)

1. Abood LG (1989): Agonists and antagonists to nicotine as smoking deterents. U.S. Patent 4,835,162.
2. Bartus RT, Dean RL III, Beer B, Lippa AS (1982): The cholinergic hypothesis of memory dysfunction. Science 217:408-417.
3. Boelsterli J, Eggnauer U, Pombo-Villar E, Weber H-P, Walkinshaw M, Gould RO (1992): Absolute configuration of 3-substituted 1-azabicyclo[2.2.1]heptanes. Helv Chim Acta 75:507-512.
4. Bonner TI (1989): New subtypes of muscarinic acetylcholine receptors. Subtypes of Muscarinic Receptors. Trends Pharmacol Sci suppl: IV:11-15.
5. Bordley A, Feltz P, Trouslard J (1996): Patch-clamp characterization of nicotinic receptors in a subpopulation of lamina X neurons in rat spinal cord slices. J Physiol (Lond) 490:673-678.
6. Freedman SB, Harley EA, Patel S, Newberry NR, Gilbert MJ, McKnight AT, Tang JK, Maguire JJ, Mudunkotuwa, Baker R, Street LJ, MacLeod AM, Saunders J, Iversen LL (1990): A novel series of non-quaternary oxadiazoles acting as full agonists at muscarinic receptors. Br J Pharmacol 101:575-580.
7. Hu J, Wang S-Z, El-Fakahany EE (1991): Effect of agonist efficacy on desensitization of phosphoinositide hydrolysis mediated by m1 and m3 muscarinic receptors expressed in Chinese hamster ovary cells. J Pharmcol Exp Ther 257:938-945.
8. Hynes RC, Le Page Y (1991): Sucrose, a convenient test crystal for absolute structures. J Appl Crystallogr 24:352-354.
9. Le Page Y, Gabe EJ, Gainsford GJ (1990): A robust alternative to n refinement for assessing the hand of chiral compounds. J Appl Crystallgr 23:406-411.
10. Morris H, Maurer SA, Storch FE, Boast CA (1992) Chronic infusion of muscarinic agonists may be necessary to attenuate AF64A cognitive impairments in rats. Soc Neurosci Abs 18:518-517.
11. Nordvall G, Hacksell U (1993): Binding-site modeling of the muscarinic m1 receptor: A combination of homology-based and indirect approaches. J Med Chem 36:967-976.
12. Peele DB, Baron SD (1988): Effects of selection delays on radial maze performance: Acquisition and effects of scopolamine. Phannacol Biochem Behav 29:143-150.
13. Sabb AL, Stein RP (1995): 1-Azabicycloheptane derivatives. U.S. Patent 5,468,875.
14. Saunders J, Freedman SB (1989): The design of full agonists for the cortical muscarinic receptor. Subtypes of muscarinic receptors. Trends Pharm Sci suppl IV:70-75.
15. Schwarz RD, Davis RE, Jaen JC, Spencer CJ, Tecle H, Thomas AJ (1993): Characterization of muscarinic agonists in recombinant cell lines. Life Sci 52:465-472.
16. Sheldrick GM (1990): SHELXTL-PLUS, Release 4.21. Siemens Analytical X-ray Instruments, Inc., Madison, WI.
17. Sheldrick GM (1993): SHELXL-93. Program for the refinement of Crystal Structures. University of Gottingen, Germany.
18. 14C-3-(3-hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methyl- pyridine (hexyloxy-T2TP) in F344 rats and rhesus monkeys. ISSX Proceedings 2:186.
19. 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.
20. Symons JP, Smith M, Marriott JG, Davis RE (1986): Effects of muscarinic cholinergic agents on spontaneous swimming in rats. Soc Neurosci Abs 12:897.
21. Tecle H, Lauffer DJ, Mirzadegan T, Moos WH, Moreland DW, Pavia MR, Schwarz RD, Davis RE (1992): A rationale for the design and synthesis of m1 selective muscarinic agonists. Bioorg Med Cheni Lett 2:821-826.
22. 3H]quinuclidinyl. Benzilate in rat brain tissue. Life Sci 40:1981-1987.
23. Walsh TJ, Tilson HA, De Haven DL, Mailman RB, Fisher A, Hanin I (1984): AF64A, a cholinergic neurotoxin, selectively depletes acetylcholine in hippocampus and cortex, and produces long-term passive avoidance and radial arm maze deficits in the rat. Brain Res 32191-102.
24. Williams M (1993): Tacrine-recommended for approval. Curr Opin Invest Drugs 2:541-544.