Are positive allosteric modulators of α7 nAChRs clinically safe?

Journal of Neurochemistry

Volumn 136, Issue 2, 2016, Pages 217-219

  Uteshev, Victor ^a  

^a UNIVERSITY OF NORTH TEXAS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (5 CHLORO 2,4 DIMETHOXYPHENYL) 3 (5 METHYL 3 ISOXAZOLYL)UREA; BUNGAROTOXIN RECEPTOR; NIFEDIPINE; OMEGA CONOTOXIN; VOLTAGE GATED CALCIUM CHANNEL; CALCIUM;

ADULT; ALLOSTERISM; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRAIN ISCHEMIA; CALCIUM CELL LEVEL; CALCIUM TRANSPORT; CELL PROTECTION; CELL VIABILITY; CONTROLLED STUDY; CYTOTOXICITY; DRUG ACTIVITY; DRUG ANTAGONISM; ENZYME ACTIVATION; GLIOSIS; HUMAN; HUMAN CELL; MIDDLE CEREBRAL ARTERY OCCLUSION; MORTALITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; TRAUMATIC BRAIN INJURY; YOUNG ADULT; AGONISTS; ANIMAL; ENDOPLASMIC RETICULUM; MALE; METABOLISM; PHYSIOLOGY;

ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR; ANIMALS; CALCIUM; ENDOPLASMIC RETICULUM; HUMANS; MALE;

EID: 84954369733     PISSN: 00223042     EISSN: 14714159     Source Type: Journal    
DOI: 10.1111/jnc.13236     Document Type: Article

References (13)

1. Gatson J. W., Simpkins J. W., and, Uteshev V. V., (2015) High therapeutic potential of positive allosteric modulation of alpha7 nAChRs in a rat model of traumatic brain injury: proof-of-concept. Brain Res. Bull. 112C, 35-41.
2. Gourlay S. G., and, Benowitz N. L., (1997) Arteriovenous differences in plasma concentration of nicotine and catecholamines and related cardiovascular effects after smoking, nicotine nasal spray, and intravenous nicotine. Clin. Pharmacol. Ther. 62, 453-463.
3. Guerra-Alvarez M., Moreno-Ortega A. J., Navarro E., Fernandez-Morales J. C., Egea J., Lopez M. G., and, Cano-Abad M. F., (2015) Positive allosteric modulation of alpha-7 nicotinic receptors promotes cell death by inducing Ca(2+) release from the endoplasmic reticulum. J. Neurochem. 133, 309-319.
4. Hurst R. S., Hajos M., Raggenbass M., et al,. (2005) A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J. Neurosci. 25, 4396-4405.
5. Kalappa B. I., and, Uteshev V. V., (2013) The dual effect of PNU-120596 on alpha7 nicotinic acetylcholine receptor channels. Eur. J. Pharmacol. 718, 226-234.
6. Kalappa B. I., Sun F., Johnson S. R., Jin K., and, Uteshev V. V., (2013) A positive allosteric modulator of alpha7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischaemia. Br. J. Pharmacol. 169, 1862-1878.
7. McLean S. L., Idris N. F., Grayson B., Gendle D. F., Mackie C., Lesage A. S., Pemberton D. J., and, Neill J. C., (2012) PNU-120596, a positive allosteric modulator of alpha7 nicotinic acetylcholine receptors, reverses a sub-chronic phencyclidine-induced cognitive deficit in the attentional set-shifting task in female rats. J. Psychopharmacol. 26, 1265-1270.
8. Ng H. J., Whittemore E. R., Tran M. B., Hogenkamp D. J., Broide R. S., Johnstone T. B., Zheng L., Stevens K. E., and, Gee K. W., (2007) Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc. Natl Acad. Sci. USA 104, 8059-8064.
9. Rose J. E., Mukhin A. G., Lokitz S. J., Turkington T. G., Herskovic J., Behm F. M., Garg S., and, Garg P. K., (2010) Kinetics of brain nicotine accumulation in dependent and nondependent smokers assessed with PET and cigarettes containing 11C-nicotine. Proc. Natl Acad. Sci. USA 107, 5190-5195.
10. Russell M. A., Jarvis M., Iyer R., and, Feyerabend C., (1980) Relation of nicotine yield of cigarettes to blood nicotine concentrations in smokers. Br. Med. J. 280, 972-976.
11. Sun F., Jin K., and, Uteshev V. V., (2013) A Type-II Positive Allosteric Modulator of alpha7 nAChRs Reduces Brain Injury and Improves Neurological Function after Focal Cerebral Ischemia in Rats. PLoS ONE 8, e73581.
12. Walker D. P., Wishka D. G., Piotrowski D. W., et al,. (2006) Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists. Bioorg. Med. Chem. 14, 8219-8248.
13. Williams D. K., Peng C., Kimbrell M. R., and, Papke R. L., (2012) Intrinsically low open probability of alpha7 nicotinic acetylcholine receptors can be overcome by positive allosteric modulation and serum factors leading to the generation of excitotoxic currents at physiological temperatures. Mol. Pharmacol. 82, 746-759.