Selective inhibition of noradrenaline and serotonin uptake by C 49802-B-Ba and CGP 6085 A

Eur J Pharmacol. 1977 Dec 15;46(4):387-91. doi: 10.1016/0014-2999(77)90234-5.

Abstract

The effects of two new compounds, 1-(1-methylamino-2-hydroxy-3-propyl)-dibenzo[b,e]bicyclo[2,2,2]octadiene-HCl (C 49802-B-Ba) and 4-(5,6-dimethyl-2-benzofuranyl) piperidine HCl (CGP 6085 A), on noradrenaline (NA) and serotonin (5-HT) uptake were investigated in different test systems, CGP 6085 A is a very potent and selective inhibitor of 5-HT uptake in rat brain (ED50 1-4 mg/kg p.o., depending on test system). Doses up to 1000 mg/kg p.o. did not inhibit NA uptake. C 49802-B-Ba is a potent and selective inhibitor of NA uptake in rat brain (ED50 5-10 mg/kg p.o. depending on test system) and heart (ED50 1.5 mg/kg p.o.). At 300 mg/kg p.o., this compound caused no inhibition of 5-HT uptake.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Benzofurans / pharmacology*
  • Brain / drug effects
  • Brain / metabolism
  • Bridged Bicyclo Compounds / pharmacology*
  • Bridged-Ring Compounds / pharmacology*
  • Depression, Chemical
  • Female
  • In Vitro Techniques
  • Myocardium / metabolism
  • Norepinephrine / metabolism*
  • Piperidines / pharmacology*
  • Rats
  • Serotonin / metabolism*

Substances

  • Benzofurans
  • Bridged Bicyclo Compounds
  • Bridged-Ring Compounds
  • Piperidines
  • Serotonin
  • 4-(5,6-dimethyl-2-benzofuranyl)piperidine
  • Norepinephrine