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Effect of varenicline on the acute and repeated locomotor responses to nicotine in rats
Author(s) -
Zaniewska Magdalena,
Mccreary Andrew C.,
Stefański Roman,
Przegaliński Edmund,
Filip Małgorzata
Publication year - 2008
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.20564
Subject(s) - varenicline , nicotine , pharmacology , agonist , partial agonist , sensitization , nicotinic agonist , smoking cessation , medicine , chemistry , anesthesia , receptor , pathology , immunology
The objective of this study was to evaluate the efficacy of varenicline, a novel partial agonist at α4β2 and full agonist at α7 nicotinic acetylcholine receptor (nAChR) subtypes, in blocking the locomotor effects of acute or repeated treatments with nicotine (0.4 mg/kg, s.c.) in rats. Varenicline (0.3–3 mg/kg, s.c.) by itself enhanced the basal locomotor activity in naive rats while it had an inhibitory effect on acute nicotine‐induced hyperlocomotion. Varenicline (0.3–3 mg/kg) did not change the nicotine‐evoked conditioned locomotion, but when administered to nicotine‐sensitized rats (0.1 and 1 mg/kg), reduced the expression of nicotine sensitization. In another set of experiments, varenicline (1 mg/kg) administered during the second withdrawal period (days 11–14) to nicotine‐treated rats, attenuated the reestablishment of the expression of nicotine sensitization. Our pharmacological analyses further support the hypothesis that varenicline might be a useful treatment for smoking cessation considering its actions on the locomotor and reinforcing effects of nicotine without inhibition of conditioned locomotion. Synapse 62:935–939, 2008. © 2008 Wiley‐Liss, Inc.