Purcell W M, Hanahoe T H
Hatfield Polytechnic, Herts, UK.
Agents Actions. 1990 Apr;30(1-2):41-3. doi: 10.1007/BF01968993.
Amitriptyline, at a concentration of 10(-4) M, significantly inhibited the release of histamine from purified peritoneal rat mast cells in response to compound 48/80, but was without effect upon the output of 5-HT. The reduction was not extensive, and concentrations of the drug above or below 10(-4) M were without effect. Amitriptyline (10(-8)-10(-4) M) inhibited uptake of exogenous 5-HT in a concentration dependent manner. Paradoxically, however, histamine uptake was significantly increased in the presence of this drug, but only at a concentration of 10(-4) M. This effect was observed at 4 degrees C for both amines. Concentrations of amitriptyline in excess of 10(-4) M caused lysis of the mast cells. These results suggest that the observed selective inhibitory effect of amitriptyline upon histamine output may be a function of altered amine uptake rather than differential inhibition and 5-HT secretion.
阿米替林在浓度为10⁻⁴ M时，能显著抑制纯化的大鼠腹膜肥大细胞对化合物48/80产生反应时组胺的释放，但对5-羟色胺的释放没有影响。这种减少并不显著，且该药物高于或低于10⁻⁴ M的浓度均无作用。阿米替林（10⁻⁸ - 10⁻⁴ M）以浓度依赖的方式抑制外源性5-羟色胺的摄取。然而，矛盾的是，在该药物存在的情况下，组胺摄取显著增加，但仅在10⁻⁴ M的浓度下。两种胺类在4℃时均观察到这种效应。超过10⁻⁴ M的阿米替林浓度会导致肥大细胞裂解。这些结果表明，观察到的阿米替林对组胺释放的选择性抑制作用可能是胺摄取改变的结果，而非差异抑制和5-羟色胺分泌的结果。
