Effects of sazetidine-A, a selective α4β2* nicotinic receptor desensitizing agent, on body temperature regulation in mice and rats

European Journal of Pharmacology

Volumn 682, Issue 1-3, 2012, Pages 110-117

  Rezvani, Amir H ^a   Timofeeva, Olga ^a   Sexton, Hannah G ^a   Decuir, Damien ^a   Xiao, Yingxian ^b   Gordon, Christopher J ^c   Kellar, Kenneth J ^b   Levin, Edward D ^a  

^a DUKE UNIVERSITY MEDICAL CENTER   (United States)

^b GEORGETOWN UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c U S ENVIRONMENTAL PROTECTION AGENCY   (United States)

Author keywords

Body temperature; DH E; Hypothermia; MLA; Nicotine; Telemetry; Thermoregulation

Indexed keywords

CHOLINERGIC RECEPTOR AFFECTING AGENT; DIHYDRO BETA ERYTHROIDINE; METHYLLYCACONITINE; NICOTINE; NICOTINIC RECEPTOR ALPHA4BETA2; SAZETIDINE A; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CORE TEMPERATURE; DOSE RESPONSE; HYPOTHERMIA; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR DOWN REGULATION; THERMOREGULATION;

ACONITINE; ANIMALS; AZETIDINES; BODY TEMPERATURE REGULATION; DIHYDRO-BETA-ERYTHROIDINE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; MALE; MICE; NICOTINE; NICOTINIC ANTAGONISTS; PYRIDINES; RATS; RECEPTORS, NICOTINIC;

EID: 84859108539     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2012.02.031     Document Type: Article

References (31)

1. B.J. Caldarone, D. Wang, N.E. Paterson, M. Manzano, A. Fedolak, K. Cavino, M. Kwan, T. Hanania, S.K. Chellappan, I.A.P. Kozikowsk, B. Olivier, M.R. Picciotto, and A. Ghavami Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380 Psychopharmacology 217 2011 199 210
2. A.L. Carbone, M. Moroni, P.J. Groot-Kormelink, and I. Bermudez Pentameric concatenated (a4)2(b2)3 and (a4)3(b2)2 nicotinic acetylcholine receptors: subunit arrangement determines functional expression Br. J. Pharmacol. 156 2009 970 981
3. G. Cucchiaro, Y. Xiao, A. Gonzalez-Sulser, and K.J. Kellar Analgesic effects of sazetidine-A, a new nicotinic cholinergic drug Anesthesiology 109 2008 512 519
4. C.M. Flores, S.W. Rogers, L.A. Pabreza, B.B. Wolfe, and K.J. Kellar A subtype of nicotinic cholinergic receptor in rat brain is composed of alpha4 and beta2 subunits and is up-regulated by chronic nicotine treatment Mol. Pharmacol. 41 1992 31 37
5. C.J. Gordon Temperature regulation in laboratory rodents 1993 Cambridge University Press New York
6. C.J. Gordon Thermoregulation in laboratory mammals and human exposed to anticholinestrase agents Neurotoxicol. Teratol. 16 1994 427 453
7. C.J. Gordon The therapeutic potential of regulated hypothermia Emerg. Med. J. 8 2001 81 89
8. C.J. Gordon Temperature and toxicology: an integrative, comparative and environmental approach 2005 Taylor & Francis Group New York
9. C.J. Gordon, F.S. Mohler, W.P. Watkinson, and A.H. Rezvani Temperature regulation in laboratory mammals following acute toxic insult Toxicology 53 1998 161 178
10. C.J. Gordon, P.J. Rowse, and Y.L. Yang Effects of repeated nicotine exposure on core temperature and motor activity in male and female rats J. Therm. Biol. 27 2002 485 492
11. G.H. Hall, and R.D. Myers Temperature changes produced by nicotine injected into the hypothalamus of the conscious monkey Brain Res. 37 1972 241 251
12. G.V. Knox, C. Campbell, and P. Lomax The effects of acetylcholine and nicotine on unit activity in the hypothalamic thermoregulatory centers of the rat Brain Res. 51 1973 215 223
13. A.P. Kozikowski, J.B. Eaton, K.M. Bajjuri, S.K. Chellappan, Y. Chen, S. Karadi, R. He, B. Caldarone, M. Manzano, P.W. Yuen, and R.J. Lukas Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin- 3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression ChemMedChem 4 2009 1279 1291
14. E.D. Levin, A.H. Rezvani, Y. Xiao, S. Slade, M. Cauley, D. Wells, D. Hampton, A. Petro, J.E. Rose, M.L. Brown, M.A. Paige, B.E. McDowell, and K. Kellar Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist reduces nicotine self-administration in rats J. Pharmacol. Exp. Ther. 332 2010 933 939
15. J. Liu, J.B. Eaton, B. Caldarone, R.J. Lukas, and A.P. Kozikowski Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as alpha4beta2-nicotinic acetylcholine receptor-selective partial agonists J. Med. Chem. 53 2010 6973 6985
16. M.J. Marks, L. Miner, J.B. Burch, D.W. Fulker, and A.C. Collins A diallel analysis of nicotine-induced hypothermia Pharmacol. Biochem. Behav. 21 1984 953 959
17. M.J. Marks, J.A. Stitzel, and A.C. Collins Genetic influences on nicotine responses Pharmacol. Biochem. Behav. 33 1989 667 678
18. A. Nordberg, and A. Sundwall Pharmacodynamic effects of nicotine and acetylcholine biosynthesis in mouse brain Acta Pharmacol. Toxicol. 52 1983 341 347
19. D.H. Overstreet Differential effects of nicotine in inbred and selectively bred rodents Behav. Genet. 25 1995 179 185
20. D.H. Overstreet, L.C. Daws, G.D. Schiller, J. Orbach, and D.S. Janowsky Cholinergic/serotonergic interactions in hypothermia: implications for rat models of depression Pharmacol. Biochem. Behav. 59 1998 777 785
21. K.G. Paradiso, and J.H. Steinbach Nicotine is highly effective at producing desensitization of rat alpha4beta2 neuronal nicotinic receptors J. Physiol. (Lond) 15 2003 857 871
22. A.H. Rezvani, S. Slade, C. Wells, A. Petro, T.K. Li, L. Lumeng, Y. Xiao, M.L. Brown, M.A. Paige, B.E. McDowell, K.J. Kellar, J.E. Rose, and E.D. Levin Sazetidine-A, a selective α4β2 nicotinic acetylcholine receptor desensitizing agent and partial agonist reduces both alcohol and nicotine self-administration in selectively-bred alcohol preferring (P) rats Psychopharmacology 211 2010 161 174
23. A.H. Rezvani, M. Cauley, H. Sexton, X. Xiao, M.L. Brown, M.A. Paige, B.E. McDowell, K.L. Kellar, and E.D. Levin Sazetidine-A, a selective α4β2 nicotinic acetylcholine receptor desensitizing agent reverses dizocilpine and scopolamine-induced attentional impairments in rats Psychopharmacology 215 2011 621 630
24. D.N. Ruskin, R. Anand, and G.J. LaHoste Chronic menthol attenuates the effect of nicotine on body temperature in adolescent rats Nicotine Tob. Res. 10 2008 1753 1759
25. R. Sack, A. Gochberg-Sarver, U. Rozovsky, M. Kedmi, S. Rosner, and A. Orr-Urtreger Lower core body temperature and attenuated nicotine-induced hypothermic response in mice lacking the beta4 neuronal nicotinic acetylcholine receptor subunit Brain Res. Bull. 66 2005 30 36
26. O. Salminen, and L. Ahtee The effects of acute nicotine on the body temperature and striatal dopamine metabolism of mice during chronic nicotine infusion Neurosci. Lett. 284 2000 37 40
27. J.R. Turner, L.M. Castellano, and J.A. Blendy Parallel anxiolytic-like effects and upregulation of neuronal nicotinic acetylcholine receptors following chronic nicotine and varenicline Nicotine Tob. Res. 13 2011 41 46
28. Y. Xiao, H. Fan, J.L. Musachio, Z.L. Wei, S.K. Chellappan, A.P. Kozikowski, and K.J. Kellar Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them Mol. Pharmacol. 70 2006 1454 1460
29. Y. Xiao, R.P. Yasuda, N. Sahibzada, L. Horton, J.R. DiPietro, A.F. Iwueze, M.A. Paige, B. McDowell, M.L. Brown, B.B. Wolfe, and K.J. Kellar Pharmacological properties of sazetidine-A, a selective ligand of α4β2 nicotinic acetylcholine receptor Society for Neuroscience 38th Annual MeetingWashington, DC 2008
30. M.R. Zarrindast, S. Barghi-Lashkari, and M. Shafizadeh The possible cross-tolerance between morphine- and nicotine-induced hypothermia in mice Pharmacol. Biochem. Behav. 68 2001 283 289
31. R. Zwart, A.L. Carbone, M. Moroni, I. Bermudez, A.J. Mogg, E.A. Folly, L.M. Broad, A.C. Williams, D. Zhang, C. Ding, B.A. Heinz, and E. Sher Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors Mol. Pharmacol. 73 2008 1838 1843