抗炎症薬に関する研究(第17報) : 2-Amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine(Y-3642)Hydrochlorideのラット肝ミトコンドリアの酸化的リン酸化, 膨化およびAdenosine Triphosphataseに対する影響

概要

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Oxidative phosphorylation (expressed as ADP/O ratio) in liver mitochondria of rats was uncoupled by 2-amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno [2,3-c] pyridine (Y-3642) hydrochloride in vitro. The concentration of 20% inhibition of the compound was about 90 μM, which is lower than that of acetylsalicylic acid or Ibufenac, but higher than that of phenylbutazone, Indomethacin, or flufenamic acid. The ADP/O ratio of the mitochondria obtained from rats after oral administration of Y-3642 in a dose of 100 mg/kg was not different from that of untreated control. Y-3642 showed a reverse action on mitochondria swelling ; it promoted at 1000 μM and inhibited the swelling at 500 μM. Activation of mitochondria ATPase in the presence of Y-3642 at a concentration of 100 μM was only 12%, against 227% at 5 μM of flufenamic acid. These results may suggest that Y-3642 produces a functional change in the mitochondria without a structural change and that production or hydrolysis of ATP does not play an important role in the mechanism of anti-inflammatory activity of this compound.
公益社団法人日本薬学会の論文
1971-07-25