Stereoselective inhibition of renal organic cation transport in human kidney

British Journal of Clinical Pharmacology
L T WongD S Sitar


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.


May 1, 1979·Human Pathology·B F Trump, C C Harris
Jul 1, 1991·Kidney International·J J Grantham
May 1, 1988·Clinical Pharmacology and Therapeutics·E SteinerR Dahlqvist
Nov 1, 1986·Clinical Pharmacology and Therapeutics·D A NottermanM M Reidenberg
Aug 1, 1953·The Biochemical Journal·M DIXON
Aug 1, 1961·The Biochemical Journal·G N WILKINSON

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Jan 1, 1995·Pflügers Archiv : European journal of physiology·S H WrightT P Wunz
Sep 27, 2002·European Journal of Pharmacology·Jeanne FourieDaniel S Sitar
Dec 17, 2003·Clinical Pharmacokinetics·Dion R Brocks, Reza Mehvar
Jun 6, 2006·European Journal of Pharmacology·Kerry B GoralskiDaniel S Sitar
Jan 28, 2014·PloS One·Iqra IshtiaqueAfra Ishtiaque
Jul 23, 2004·Physiological Reviews·Stephen H Wright, William H Dantzler
Dec 11, 2007·Canadian Journal of Physiology and Pharmacology·Daniel S Sitar

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