J. Garciacolunga et al., BLOCKAGE OF MUSCLE AND NEURONAL NICOTINIC ACETYLCHOLINE-RECEPTORS BY FLUOXETINE (PROZAC), Proceedings of the National Academy of Sciences of the United Statesof America, 94(5), 1997, pp. 2041-2044
Fluoxetine (Prozac), a widely used antidepressant, is said to exert it
s medicinal effects almost exclusively by blocking the serotonin uptak
e systems. The present study shows that both muscle and neuronal nicot
inic acetylcholine receptors are blocked, in a noncompetitive and volt
age-dependent way, by fluoxetine, which also increases the rate of des
ensitization of the nicotinic receptors. Because these receptors are v
ery widely distributed in the both central and peripheral nervous syst
ems, the blocking action of fluoxetine on nicotinic receptors may play
an important role in its antidepressant and other therapeutical effec
ts. Our findings will help to understand the mode of action of fluoxet
ine, and they may also help to develop more specific medicinal drugs.