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Inhibition of serotonin uptake by optical isomers of fluoxetine
Author(s) -
Wong David T.,
Bymaster Frank P.,
Reid Leroy R.,
Fuller Ray W.,
Perry Kenneth W.
Publication year - 1985
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430060412
Subject(s) - fluoxetine , serotonin , chemistry , pharmacology , 5 ht receptor , synaptosome , stereochemistry , biochemistry , membrane , receptor , biology
The optical isomers of fluoxetine, a selective inhibitor of serotonin (5‐hydroxytryptamine, 5HT) uptake, have been compared pharmacologically. As inhibitors of 3 H‐5HT uptake in cortical synaptosomes and of 3 H‐fluoxetine binding in cortical membranes, the (+)‐isomer of fluoxetine was slightly more potent than the (−)‐isomer. The potencies to inhibit 3 H‐5HT uptake ex vivo in synaptosomal preparations of cerebral cortex and brain stem were about the same, except that the (−)‐isomer had a much shorter duration of action than the (+)‐isomer in rats.