Temperature-sensitive high affinity [3H]serotonin binding: Characterization and effects of antidepressant treatment |
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Authors: | Daiga M. Helmeste Siu W. Tang |
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Affiliation: | Psychopharmacology Unit, Clarke Institute of Psychiatry, 250 College Street, Toronto, Ontario, Canada M5T 1R8 |
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Abstract: | Characterization of temperature-sensitive [3H]serotonin (5-HT) binding sites (1 and 4 nM Kd sites) revealed complex inhibition by neuroleptics and serotonin antagonists. There was no simple correlation with affinities for S1 and S2 receptors. pretreatment (48 h before) with mianserin did not alter Bmax or Kd for the 1 nM Kd [3H]5-HT site, although [3H]ketanserin (S2) densities were decreased by 50%. This suggested that possible S2 components of [3H]5-HT binding must be negligeable, even though ketanserin competed with high affinity (IC50 = 3 nM) for a portion of the 1 nM Kd [3H]5-HT site. Low concentrations of mianserin inhibited the 1 nM Kd [3H]5-HT site in a non-competitive manner, as shown by a decrease in Bmax with no change in Kd after incubation. The complex inhibition data may therefore represent indirect interactions through another site. |
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