Abstract
The cephalosporin antibiotics cephaloridine and cefazolin were examined for their effects on the transport of a prototype anion, [3H]p-aminohippurate (PAH) and a prototype cation, N1-[3H] methylnicotinamide (NMN) in basolateral membrane vesicles and brush border membrane vesicles (BBMV). Cefazolin inhibited transport of 50 microM PAH in both membranes and had no effect on transport of 50 microM NMN transport. Under identical conditions, cephaloridine, a zwitterion, inhibited PAH transport in both membranes and NMN transport in BBMV but not in basolateral membrane vesicles. Cephaloridine was less effective than cefazolin in inhibiting PAH transport in BBMV. The results demonstrate the organic transport systems in the basolateral membrane vesicles differ from those in the BBMV. Furthermore, a zwitterionic drug can interact with both systems in the BBMV. An explanation for the intracellular accumulation of cephaloridine is presented.
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