Preferential inhibition of type B-MAO by new compounds, 1-[3-(dimethylamino)propyl]-5-methyl-3-phenyl-1H-indazole(FS32) and its N-desmethylated derivative (FS97)

2区 · 医学

Article

作者: T. Koide ; K. Uyemura

FS32 (I, R = Me) [57614-23-0] and FS97 (I, R = H) [61365-76-2] effectively inhibited rat brain mitochondrial monoamine oxidase (EC 1.4.3.4) (II) [9001-66-5] type B (K_i = 0.9 × 10^-5 and 0.8 × 10^-5M, resp.) but inhibited type A II (K_i = 34.5 × 10^-5 and 20.0 × 10^-5M, resp.) to a lesser extent.II type B was also more susceptible than type A to inhibition by classical tricyclic antidepressants, e.g. imipramine [50-49-7].FS32 and FS97 were competitive, reversible inhibitors of types A and B II.

1980-04-01·Neuropharmacology2区 · 医学

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

2区 · 医学

Article

作者: T. Koide ; K. Uyemura

FS32 (I, R = H) [57614-23-0] and FS97 (I, R = Me) [61365-76-2], new nontricyclic amine uptake inhibitors, competitively inhibited ³H-labeled norepinephrine [50-67-9] uptake into hypothalamic synaptosomes with K_i values of 6.5 × 10^-7 and 3.8 × 10^-7M resp.The potencies of FS32 and FS97 were similar to those observed for clomipramine and imipramine resp.Competitive inhibition of ³H-labeled 5-hydroxytryptamine [51-41-2] uptake into whole brain synaptosomes by FS32 and FS97 was also observed (K_i 2.9 × 10^-6 and 5.9 × 10^-6M); the former was equipotent with nortriptyline and the latter was twice as potent as iprindole.

1980-03-01·European Journal of Pharmacology3区 · 医学

Inhibition of (3H)-dopamine uptake into rat brain synaptosomes by the new non-tricyclic antidepressants, FS32 and FS97

3区 · 医学

Article

作者: Uyemura, Keiichi ; Koide, Tohru

The effects of new non-tricyclic antidepressants, FS32 and its desmethylated compound (FS97), on the uptake of (3H)-dopamine (DA) by rat purified whole brain synaptosomes and the striatal synaptosomes were studied. The uptake into synaptosomes was time- and temperature-dependent and was saturable with a Km value of 9.1 X 10(-8) M. The inhibiting activities of both compounds were comparable to those of amitriptyline, nortriptyline and iprindole, and were nearly twice the activity of imipramine and desipramine. The kinetic constants indicated that both FS32 and FS97 were competitive inhibitors of (3H)-DA uptake. Neither drug caused a significant release of (3H)-DA from the synaptosomes.

100 项与 FS-032 相关的药物交易

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