Selective inhibition of noradrenaline and serotonin uptake by C 49802-B-Ba and CGP 6085 A.
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.
D000818:Animals; D001572:Benzofurans / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology*; D001952:Bridged-Ring Compounds / Q000494:pharmacology*; D003864:Depression, Chemical; D005260:Female; D066298:In Vitro Techniques; D009206:Myocardium / Q000378:metabolism; D009638:Norepinephrine / Q000378:metabolism*; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D012701:Serotonin / Q000378:metabolism*
D001572:Benzofurans; D001643:Bridged Bicyclo Compounds; D001952:Bridged-Ring Compounds; D010880:Piperidines; D012701:Serotonin; C015613:4-(5,6-dimethyl-2-benzofuranyl)piperidine; D009638:Norepinephrine