{"title":"Effect of doxepin on uptake and efflux of serotonin human blood patelets in vitro.","authors":"O Lingjaerde","doi":"10.1007/BF00735819","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":20715,"journal":{"name":"Psychopharmacologia","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1976-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/BF00735819","citationCount":"2","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Psychopharmacologia","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1007/BF00735819","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 2
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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