Effect of doxepin on uptake and efflux of serotonin in human blood patelets in vitro
- 1 January 1976
- journal article
- research article
- Published by Springer Nature in Psychopharmacology
- Vol. 47 (2) , 183-186
- https://doi.org/10.1007/bf00735819
Abstract
It is shown that the tricyclic antidepressant drug doxepin (comprising 15% of thecis- and 85% of thetrans-isomer) is a moderately potent competitive inhibitor of serotonin uptake in human blood platelets in vitro, with an inhibitory constantKi of about 2×10-7 M. The inhibitory effect was 6 times stronger in an artificial, protein-free medium than in diluted plasma, corresponding to about 85% protein binding. The efflux of serotonin from platelets preloaded with14C-serotonin was not affected by doxepin in concentrations up to 10-6 M, but increased rapidly at concentrations above 10-4 M.Keywords
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