Sugawara M, Sasaki M, Iseki K, Miyazaki K
Department of Pharmacy, Hokkaido University Hospital, School of Medicine, Sapporo, Japan.
Biochim Biophys Acta. 1992 Nov 9;1111(2):145-50. doi: 10.1016/0005-2736(92)90304-5.
The effect of membrane potential on the uptake of tryptamine, an organic cation, by rat intestinal brush-border membrane vesicles was studied. In the presence of an outwardly directed H(+)-gradient, the initial uptake of tryptamine was stimulated remarkably and the overshoot phenomenon was observed. In contrast, the uptake was depressed by an inwardly-directed H(+)-gradient. The effect of H(+)-gradient on the uptake of tryptamine was maintained in the presence of FCCP, whereas it vanished when voltage-clamped vesicles were used. Moreover, the uptake of tryptamine was linearly augmented with increase of the valinomycin-induced inside-negative K+ diffusion potential. These results suggest that tryptamine is taken up into intestinal brush-border membrane vesicles depends upon the ionic diffusion potential. The effect of several indole derivatives and amine compounds on the uptake of tryptamine was also examined. The uptake of tryptamine was inhibited by all amine compounds used, but anionic and zwitterionic compounds had no effect, suggesting that these amines interact on brush-border membrane and cause an inhibitory effect.
研究了膜电位对大鼠肠道刷状缘膜囊泡摄取有机阳离子色胺的影响。在存在外向H⁺梯度的情况下,色胺的初始摄取显著受到刺激,并观察到过冲现象。相反,内向H⁺梯度会抑制摄取。在存在羰基氰化物间氯苯腙(FCCP)的情况下,H⁺梯度对色胺摄取的影响得以维持,而当使用电压钳制的囊泡时,这种影响消失。此外,随着缬氨霉素诱导的内向负K⁺扩散电位的增加,色胺的摄取呈线性增加。这些结果表明,色胺被摄取到肠道刷状缘膜囊泡中取决于离子扩散电位。还研究了几种吲哚衍生物和胺类化合物对色胺摄取的影响。所用的所有胺类化合物均抑制色胺的摄取,但阴离子和两性离子化合物没有影响,这表明这些胺类在刷状缘膜上相互作用并产生抑制作用。