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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 VIII.

VMAT Inhibition Kinetic Parameters of Ketanserin Derivatives

graphic file with name nihms229868u6.jpg
Ki or Kd (nM) Ki or Kd (nM)
Cpd. Chromaffin Gran. Memb. Rat cortex Cpd. Chromaffin Gran. Memb. Rat cortex
7 45.3 ± 2.4(30°)a
6.3 ± 0.4 (0°)a 		1.3d 94 40b 1.4d
91 23b - 95 814b 0.9 d
92 14b 0.7d 96 950b -
93 350b 890d 97 950b 2.3d
a

Kd determined using [3H] ketanserin at 0° and 30 °C 36.

b

Ki for [3H]DTBZOH binding at 22° C93;

c

Kd determined using [3H] ketanserin at 0°C 93.

d

Kd determined using [3H] ketanserin at 37° C36.