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. 1976 May 28;47(2):183-6.
doi: 10.1007/BF00735819.

Effect of doxepin on uptake and efflux of serotonin human blood patelets in vitro

O Lingjaerde

Effect of doxepin on uptake and efflux of serotonin human blood patelets in vitro

O Lingjaerde. Psychopharmacologia. .

Abstract

It is shown that the tricyclic antidepressant drug doxepin (comprising 15% of the cis- and 85% of the trans-isomer) is a moderately potent competitive inhibitor of serotonin uptake in human blood platelets in vitro, with an inhibitory constant Ki of about 2 X 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 with 14C-serotonin was not affected by doxepin in concentrations up to 10(-6) M, but increased rapidly at concentrations above 10(-4) M.

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