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Stereoselective inhibition of renal organic cation transport in human kidney.
Author(s) -
Wong LT,
Smyth DD,
Sitar DS
Publication year - 1992
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1992.tb05653.x
Subject(s) - stereoselectivity , diastereomer , quinidine , chemistry , kidney , quinine , human kidney , stereochemistry , pharmacology , biochemistry , endocrinology , biology , malaria , immunology , catalysis
Amantadine was found to be concentrated by human cortical slices, with apparent Km and Vmax values of 187 +/‐ 11 microM and 1.37 +/‐ 0.28 nmol mg‐1 min‐1 respectively (mean +/‐ s.e. mean, n = 4). Addition of quinine (8S, 9R‐(−)−isomer) or quinidine (8R, 9S‐(+)‐isomer) competitively inhibited this accumulation (apparent Ki values of 261 +/‐ 44 (n = 4) and 586 +/‐ 68 microM (n = 3), respectively). The stereoselectivity of this inhibition is the reverse of that seen with respect to the renal clearances of the diastereoisomers.