PMID: 8593281Jan 31, 1996Paper

Characterisation of penicillin-G uptake in rabbit small-intestinal brush-border membrane vesicles

Biochimica Et Biophysica Acta
J F PoschetP D Fairclough

Abstract

Uptake of penicillin-G has been studied in rabbit intestinal brush-border membrane vesicles (BBMV). Penicillin-G was transported into the lumen of BBMV via an H+-dependent, Na+-independent uptake system. This was a saturable carrier-mediated process, which adhered to Michaelis-Menten kinetics, having a pH optimum of 4.5 and resulting in a net-negative charge transfer. Vmax was 59 nmol penicillin-G (mg protein)-1 (30s)-1 and Km 22.7 mM. Ampicillin, penicillin-V, cefadroxil, cephalexin, cephalothin, cephradine, L-carnosine, glycyl-L-alanine, glycyl-L-tyrosine and glycylglycylglycine inhibited the uptake of penicillin-G. However, glycylsarcosine stimulated uptake by 92%. Countertransport experiments suggested that this effect took place at the active site of the transporter. Penicillin-G uptake appeared to be mediated via a common transport system shared by penicillins, cephalosporins and peptides.

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Citations

Mar 22, 2005·International Journal of Pharmaceutics·Kouki ObataYosinori Aso
Jul 5, 2005·Expert Opinion on Investigational Drugs·V Y Alakhov, A V Kabanov

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