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

European Journal of Pharmacology
P C WaldmeierL Maitre

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.

Citations

Mar 1, 1980·Naunyn-Schmiedeberg's Archives of Pharmacology·R OrtmannA Delini-Stula
Dec 16, 1983·Pharmaceutisch Weekblad. Scientific Edition·C J GrolJ De Vries
May 15, 1979·European Journal of Pharmacology·P C Waldmeier, A Delini-Stula
Dec 20, 1979·European Journal of Pharmacology·P C Waldmeier
Mar 12, 1985·European Journal of Pharmacology·W A WolfD M Kuhn
Aug 1, 1980·Physiology & Behavior·W KostowskiA Płaźnik
May 1, 1993·Pharmacology, Biochemistry, and Behavior·S F LeibowitzG F Weiss
Sep 1, 1982·Journal of Affective Disorders·J E De Wilde, D P Doogan
Jun 1, 1993·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·A SteigerF Holsboer
Apr 1, 1997·Physiology & Behavior·K InoueS Yamagami
Jan 21, 2000·Brain Research. Molecular Brain Research·Y RenN Saito
Oct 1, 1993·Journal of Basic and Clinical Physiology and Pharmacology·D VaronN V Kaverina
Dec 1, 1982·British Journal of Clinical Pharmacology·O SchmidlinE Weber
Jan 1, 1985·Clinical and Experimental Hypertension. Part A, Theory and Practice·E C KulakowskiW Lovenberg
Apr 1, 1984·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·W DieterleJ Wagner

Related Concepts

Metazoa
Diphenylbenzofuran
Bicyclo Compounds
Brain
Bridged Compounds
Depression, Chemical
Myocardium
Norepinephrine, (+, -)-Isomer
Piperidines
Hydroxytryptamine

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