ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: A novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization

Journal of Pharmacology and Experimental Therapeutics

Volumn 285, Issue 2, 1998, Pages 787-794

  Bannon, Anthony W ^a,b   Decker, Michael W ^a,d   Curzon, Peter ^a   Buckley, Michael J ^a   Kim, David J B ^a   Radek, Richard J ^a   Lynch, John K ^a   Wasicak, James T ^a   Lin, Nan Horng ^a   Arnold, William H ^a   Holladay, Mark W ^a   Williams, Michael ^a   Arneric, Stephen P ^a,c  

^a ABBOTT LABORATORIES   (United States)

^b AMGEN INC   (United States)

^c DUPONT COMPANY   (United States)

^d Bldg AP 9A LL ^*

Author keywords

[No Author keywords available]

Indexed keywords

5 (2 AZETIDINYLMETHOXY) 2 CHLOROPYRIDINE; ANALGESIC AGENT; CAFFEINE; CHOLINERGIC RECEPTOR STIMULATING AGENT; MORPHINE; UNCLASSIFIED DRUG;

ANALGESIA; ANIMAL EXPERIMENT; ARTICLE; CHOLINERGIC STIMULATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; DRUG RECEPTOR BINDING; ELECTROENCEPHALOGRAM; INTRAPERITONEAL DRUG ADMINISTRATION; LOCOMOTION; MALE; MOTOR COORDINATION; MOTOR PERFORMANCE; NONHUMAN; PRIORITY JOURNAL; RAT; TASK PERFORMANCE;

ADMINISTRATION, ORAL; ANALGESICS, NON-NARCOTIC; ANIMALS; AZETIDINES; ELECTROENCEPHALOGRAPHY; FORMALDEHYDE; MALE; MORPHINE; MOTOR ACTIVITY; NICOTINIC AGONISTS; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NICOTINIC;

EID: 7144264420     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. Aceto MD, Awaya H, Martin BR and May EL (1983) Antinociceptive action of nicotine and its methiodide derivatives in mice and rats. Br J Pharmacol 79:869-876.
2. Arneric SP (1998) Neurobiology of neuronal nicotinic acetylcholine receptors (nAChRs), in Nicotine: Neurotropic and Neurotoxic Effects. (Newhouse P and Piasecki M, eds) American Psychiatric Press, Inc., Washington, D.C., pp 1-20.
3. Badio B, Garraffo HM, Spande TF and Daly JW (1994) Epibatidine: Discovery and definition as a potent analgesic and nicotinic agonist. Med Chem Res 4:440-448.
4. Bannon AW, Decker MW, Holladay MW, Curzon P, Donnelly-Roberts D, Puttfarcken PS, Bitner RS, Pauly JL, Diaz A, Dickenson AH, Williams M and Arneric SP (1998) Broad spectrum, non-opioid analgesic activity by selective modulation of nicotinic acetylcholine receptors. Science 279:77-81.
5. Bauer G. (1987) EEG, drug effects, and central nervous system poisoning, in Electroencephalography: Basic principles, Clinical Applications and Related Fields (Niedermeyer E and Lopes De Silva F, eds) 2nd ed, pp 567-578, Urban and Schwarzenberg, Baltimore, MD.
6. Benowitz NL (1992) Nicotine and coronary heart disease. Trends Cardiovasc Med 1:315-321.
7. Bitner RS, Nikkel AL, Bannon AW, Arneric SP and Decker MW (1997) Supraspinal c-fos induction produced by a novel cholinergic channel modulator analgesic, ABT-594. Soc Neurosci Abstr 23:1200, 477.14.
8. Caggiula AR, Epstein LH, Perkins KA and Saylor S (1995) Different methods of assessing nicotine-induced antinociception may engage different neural mechanisms. Psychopharmacology 122:310-306.
9. Changeux JP, Galzi JL, Devillers-Thiery A and Bertrand D (1992) The functional architecture of the acetylcholine nicotinic receptor explored by affinity labeling and site-directed mutagenesis. Q Rev Biophys 25:395-432.
10. Cherny NI (1996) Opioid Analgesics: Comparative features and prescribing guide-lines. Drugs 51:713-737.
11. Cooper E, Couturier S and Ballivet M (1991) Pentameric structure and subunit stoichiometry of a neuronal acetylcholine receptor. Nature 350:235-238.
12. Curzon P, Bitner RS, Nikkel AL, Bannon AW, Arneric SP and Decker MW (1997) Central mechanism involved in ABT-594 antinociception. Soc Neurosci Abstr 23: 1200, 477.13.
13. Davis L, Pollock LJ and Stone TT (1932) Visceral pain. Surg Gynecol Obstet 55:418-427.
14. Decker MW, Bannon AW, Buckley MJ, Kim DJB, Holladay MW, Ryther KB, Lin N-H, Wasicak JT, Williams M and Arneric SP (1998) Antinociceptive effects of the novel cholinergic channel modulator, ABT-594, in mice. Eur J Pharmacol, in press.
15. Dirig DM and Yaksh TL (1995) Differential right shifts in the dose-response curve for intrathecal morphine and sufentanil as a function of stimulus intensity. Pain 62:321-328.
16. Donnelly-Roberts DL, Puttfarcken PS, Kunztweiler TA, Briggs CA, Anderson DJ, Campbell JE, Manelli A, Piatonni-Kaplan M, Mckenna DG, Wasciak J, Holladay MW, Williams M and Arneric SP (1998) ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: A novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization. J Pharmacol Exp Ther 285: 777-786.
17. Ferger B and Kuschinsky K (1995) Effects of morphine on EEG in rats and their possible relations to hypo- and hyperkinesia. Psychopharmacology 117:200-207.
18. Flores CM, DeCamp RM, Kilo S, Rogers SW and Hargreaves KM (1996) Neuronal nicotinic receptor expression in sensory neurons of the rat trigeminal ganglion: Demonstration of α3β4, a novel subtype in the mammalian nervous system. J Neurosci 16:7892-7901.
19. Flores CM, Rogers SW, Pabreza LA, Wolfe B and Kellar KJ (1992) A subtype of nicotinic cholinergic receptor is composed of α4 and β2 subunits and is upregulated by chronic nicotine treatment. Mol Pharmacol 41:31-37.
20. Hargreaves K, Dubner R, Brown F, Flores C and Joris J (1988) A new and sensitive method for measuring thermal nociception in cutaneous hyperalgesia. Pain 32: 77-88.
21. Holladay MW, Wasicak JT, Lin N-H, He Y, Ryther KB, Bannon AW, Buckley MJ, Kim DJB, Decker MW, Anderson DJ, Campbell JE, Kuntzweiler TA, Donnelly-Roberts DL, Piattoni-Kaplan M, Briggs CA, Williams M and Arneric SP (1998) Identification and initial structure-activity relationships of [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine] (0ABT-594), a potent, orally active non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. J Med Chem 41:407-412.
22. Martin WR and Kay DC (1977) Effects of opioid analgesics and antagonists on the EEG, in Handbook of Electroencephalography and Clinical Neurophysiology (Remond A, ed) pp 97-109, Elsevier, Amsterdam.
23. McGehee DS and Role LW (1996) Neurobiology: Memories of nicotine. Nature 383: 670-671.
24. Nikkel AL, Curzon P, Decker MW, Bannon AW, Holladay MW and Arneric SP (1997) Antinociceptive effects of two potent nicotinic receptor ligands, (±)-epibatidine and A-85380. Soc Neurosci Abstr 23:669, 266.10.
25. Qian C, Li T, Shen TY, Libertine-Garahan L, Eckman J, Biftu T and Ip S (1993) Epibatidine is a nicotinic analgesic. Eur J Pharmacol, 250:R13-R14.
26. Radek RJ, Briggs CA, Sullivan J, Kang CH and Arneric SA (1996) Effects of the cholinergic channel activator ABT-418 on cortical EEG: comparison with ( - )-nicotine. Drug Dev Res 37:73-79.
27. Seguela P, Wadiche J, Dineley-Miller K, Dani JA and Patrick JW (1993) Molecular cloning, functional properties and distribution of rat brain α7; a nicotinic cation channel highly permeable to calcium. J Neurosci 13:596-604.
28. Singh G, Ramey D, Morfeld D and Fries JF (1994) Comparative toxicity of non-steroidal anti-inflammatory agents. Pharmacol Ther 62:175-191.
29. Spande TF, Garraffo HM, Edwards MW, Yeh HJC, Pannell L and Daly JW (1992) Epibatidine: a novel (chloropyridyl)azabicycloheptane with potent analgesic activity from an Ecuadoran poison frog. J Am Chem Soc 114:3475-3478.
30. Sullivan JP and Bannon AW (1995) Epibatidine: Pharmacological properties of a novel analgesic agent. CNS Drug Rev 2:21-39.
31. Sullivan JP, Briggs CA, Donnelly-Roberts D, Brioni JD, Radek RJ, McKenna DG, Campbell JE, Arneric SP, Decker MW and Bannon AW (1994a) (±)-Epibatidine can differentially evoke responses mediated by putative subtypes of nicotinic acetylcholine receptors (nAChRs). Med Chem Res 4:502-516.
32. Sullivan JP, Decker MW, Brioni JD, Donnelly-Roberts D, Anderson DJ, Bannon AW, Kang C-H, Adams P, Piattoni-Kaplan M, Buckley MJ, Gopalakrishnan M, Williams M and Arneric SP (1994b) (±)-Epibatidine elicits a diversity of in vitro and in vivo effects mediated by nicotinic acetylcholine receptors. J Pharmacol Exp Ther 271:1-8.
33. Wada E, McKinnon D, Heinemann S, Patrick J and Swanson LW (1990) The distribution of mRNA encoded by a new member of the neuronal nicotinic acetylcholine receptor gene family (α5) in the rat central nervous system. Brain Res 526:45-53.
34. Wada E, Wada K, Boulter J, Deneris E, Heinemann S, Patrick JW and Swanson LW (1989) Distribution of alpha-2, alpha-3, alpha-4. and beta-2 neuronal nicotinic receptor subunit mRNAs in the central nervous system: A hybridization histochemical study in the rat. J Comp Neurol 284:314-335.