Blockade by antidepressants and related compounds of biogenic amine uptake into rat brain synaptosomes: Most antidepressants selectively block norepinephrine uptake

Elliott Richelson, Michael Pfenning

Research output: Contribution to journalArticle

474 Scopus citations

Abstract

Inhibitor constants (Ki's) for blocking uptake of [3H]norepinephrine, [3H]serotonin, and [3H]dopamine into synaptosomal preparations of rat brain were determined for 25 antidepressants and putative antidepressants, some neuroleptics, stimulants, antihistamines and other monoamines. With Ki's we could directly and definitely compare the relative potencies of a drug at the three processes. Eighteen or 72% of the antidepressants (including tertiary amine tricyclics) were more potent at blocking uptake of norepinephrine than at blocking uptake of serotonin. Considering all three biogenic amines, 17 antidepressants were selective for blocking [3H]norepinephrine uptake, one (bupropion) was selective although weak for blocking [3H]dopamine uptake, and the remainder were selective for blocking [3H]serotonin uptake. The neuroleptics chlorpromazine and promazine were relatively potent at blocking uptake of [3H]norepinephrine and some tricyclic antidepressants (notably, trimipramine and butriptyline) were very weak at blocking any biogenic amine uptake.

Original languageEnglish (US)
Pages (from-to)277-286
Number of pages10
JournalEuropean Journal of Pharmacology
Volume104
Issue number3-4
DOIs
StatePublished - Sep 17 1984

Keywords

  • Antihistaminics
  • Dopamine uptake
  • Neuroleptics
  • Norepinephrine uptake
  • Re-uptake
  • Serotonin uptake
  • Stimulants

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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