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. Author manuscript; available in PMC: 2012 Jul 1.
Published in final edited form as: Med Res Rev. 2010 Feb 4;31(4):483–519. doi: 10.1002/med.20187

Table V.

Inhibition Kinetic Parameters of MPP+-APP Conjugates for Bovine Chromaffin Granule VMAT.a

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Inhibitor Ki (μM)a Km,DA/Ki,Ib Inhibitor Ki (μM)a Km,DA/Ki,Ib
59 38.4 ± 4.2 0.9 64 2.8 ± 0.1 8.7
60 53.0 ± 13.6 0.7 65 0.4 ± 0.1 55
61 16.4 ± 2.7 1.8 66 0.5 ± 0.1 41.5
62 13.4 ± 1.7 2.7 67 4.5 ± 0.5 11.3
63 1.4 ± 0.2 24.1
a

Determined with resealed granule ghosts using non-radioactive substrates with HPLC-EC quantification of catecholamine uptake in the presence of 10 mM ATP, at pH 7.2.

b

Included for comparison purposes (for further details see Table IV foot notes and ref. 55).