抗炎症薬に関する研究(第18報) : 2-Amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine(Y-3642)のHistamine遊離に対する作用

抄録

2-Amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) hydrochloride showed 50% inhibition of histamine release from rat mast cells by polymixin B sulfate in vitro at a concentration of 40 μM. The activity was more potent than fulfenamic acid or phenylbutazone. At 50 μM, the compound inhibited histamine release from rat mast cells in vitro by dextran or lung thromboplastin of a rabbit. Y-3642 inhibited the delay of tissue clearance by polymixin B sulfate and protected the death by polymixin B shock in rats. These results may suggest that Y-3642 inhibits the release of mast cell histamine which plays a role as one of chemical mediators in the process of inflammation.