A comparison of the inhibitory effects of new non-tricyclic amine uptake inhibitors on the uptake of norepinephrine and 5-hydroxytryptamine into synaptosomes of the rat brain

Abstract

Listen

Translate article

The effects of new non-tricyclic amine uptake inhibitors, FS32 and FS97, on the uptake of [ 3H]-norepinephrine (NE) into the hypothalamic synaptosomes and [ 3H]-5-hydroxytryptamine (5-HT) into whole brain synaptosomes were studied. Their effects were compared with those of tricyclic antidepressants. The uptake of [ 3H]-NE was inhibited competitively by FS32 and FS97 with a respective K i value of 6.5 × 10 −7 M and 3.8 × 10 −7 M. The potency of FS32 and FS97 to inhibit this uptake was almost comparable to that of clomipramine and imipramine, respectively. In the case of [ 3H]-5-HT uptake, FS32 and FS97 also showed competitive inhibition with a respective K i value of 2.9 × 10 −6 M and 5.9 × 10 −6M. The ability of FS32 to inhibit [ 3H]-5-HT uptake was almost equal to that of nortriptyline, while FS97 was two times more potent than iprindole in inhibiting this uptake.