５‐ＨＴ取込に対する新抗うつ薬Ｐａｒｏｘｅｔｉｎｅの特異的薬理作用

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タイトル別名
  • Specific inhibitory action of the novel antidepressant paroxetine on 5-HT uptake.
  • 5-HT トリコミ ニ タイスル シン コウウツヤク Paroxetine ノ

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抄録

Effect of a novel antidepressant, paroxetine, on the uptake of serotonin (5-HT), noradrenaline (NA) and dopamine (DA) as well as on various neuro-receptors were investigated in comparison with those of the tricyclic antidepressants amitriptyline, chlorimipramine and imipramine. Paroxetine showed a potent 5-HT uptake inhibitory action, giving the NA/5-HT ratio of 886 in comparison with the ratios of 1.7, 15 and 1.5 for amitriptyline, chlorimipramine and imipramine, respectively. On the other hand, paroxetine showed almost no inhibitory action on the binding of the [3H]-labeled ligands examined in this study ([3H]quinuclidinyl benzilate, [3H]5-HT, [3H]ketanserine, [3H]pyrilamine, [3H]dihydroalprenolol, [3H]prazosin, [3H]clonidine and [3H]spiroperidol). In contrast, the tricyclic antidepressants showed inhibitory action on a number of bindings and also revealed comparatively high affinities especially for muscarine, histamine-1 and αl-adrenaline receptors responsible for the side effects. From the above findings, it can be concluded that paroxetine has only a weak affinity for various neuro-receptors and inhibits specifically 5-HT uptake.

収録刊行物

  • 日本薬理学雑誌

    日本薬理学雑誌 89 (4), 175-180, 1987

    公益社団法人 日本薬理学会

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