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Vol. 295, Issue 1, 321-327, October 2000
Department of Pharmacology and Toxicology, Medical College of
Virginia of Virginia Commonwealth University, Richmond, Virginia
Neuronal nicotinic receptors are ligand-gated ion channels of the
central and peripheral central nervous system that regulate synaptic
activity from both pre- and postsynaptic sites. The present study
establishes the acute interaction of bupropion, an antidepressant agent
that is also effective in nicotine dependence, with nicotine and
nicotinic receptors using different in vivo and in vitro tests. Bupropion was found to block nicotine's antinociception (in two tests), motor effects, hypothermia, and convulsive effects with different potencies in the present investigation, suggesting that bupropion possesses some selectivity for neuronal nicotinic receptors underlying these various nicotinic effects. In addition, bupropion blocks nicotine activation of 
3
2,
42, and 7 neuronal
acetylcholine nicotinic receptors (nAChRs) with some degree of
selectivity. It was ~50 and 12 times more effective in blocking
32 and 42 than 7. This functional blockade was noncompetitive,
because it was insurmountable by increasing concentration of ACh in the nAChRs subtypes tested. Furthermore, bupropion at high concentration failed to displace brain [3H]nicotine binding sites, a
site largely composed of 42 subunit combination. Given the observation that bupropion inhibition of 32 and 42
receptors exhibits voltage-independence properties, bupropion may not
be acting as an open channel blocker. These effects may explain in part
bupropion's efficacy in nicotine dependence. Our present findings
suggest that functional blockade of neuronal nAChRs are useful in
nicotine dependence treatment.
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