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Vol. 283, Issue 3, 1305-1322, 1997
Laboratory of Neuropsychopharmacology, Department of Psychiatry and
Behavioral Sciences, Emory University School of Medicine, Atlanta,
Georgia
Several new antidepressants that inhibit the serotonin (SERT) and
norepinephrine transporters (NET) have been introduced into clinical
practice the past several years. This report focuses on the further
pharmacologic characterization of nefazodone and its metabolites within
the serotonergic and noradrenergic systems, in comparison with other
antidepressants. By use of radioligand binding assays, we measured the
affinity (Ki) of 13 antidepressants and 6 metabolites for the rat and human SERT and NET. The
Ki values for eight of the antidepressants
and three metabolites were also determined for the rat
5-HT1A, 5-HT2A and muscarinic cholinergic receptors, the guinea pig histamine1 receptor and the human
alpha-1 and alpha-2 receptors. These data
are useful for predicting side effect profiles and the potential for
pharmacodynamic drug-drug interactions of antidepressants. Of
particular interest were the findings that paroxetine, generally
thought of as a selective SERT antagonist, possesses moderately high
affinity for the NET and that venlafaxine, which has been described as
a "dual uptake inhibitor", possesses weak affinity for the NET. We
observed significant correlations in SERT (r = 0.965) or NET (r = 0.983) affinity between rat and
human transporters. Significant correlations were also observed between
muscarinic cholinergic and NET affinity. There are several significant
correlations between affinities for the 5-HT1A,
5-HT2A, histamine1, alpha-1 and
alpha-2 receptors. These novel findings, not widely
described previously, suggest that many of the individual drugs studied
in these experiments possess some structural characteristic that
determines affinity for several G protein-coupled, but not muscarinic,
receptors.
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