TABLE 3

Kd and Bmax for specific [3H]NMS binding in the bladder, submaxillary gland, heart, colon, lung, and brain of rats at 1 to 12 h after the oral administration of imidafenacin (6.26 μmol/kg)

Rats received 6.26 μmol/kg imidafenacin orally and were sacrificed 1 to 12 h later. The specific binding of [3H]NMS (0.06–1.5 nM) in rat tissues was measured. Values in parentheses represent the fold increase in Kd values relative to the control. Values are the mean ± S.E. for sixteen (control) and four to six (imidafenacin) rats.

Tissues and TimeKdBmax
pMfmol/mg protein
Bladder
    Control275 ± 6146 ± 8
    1 h362 ± 13 (1.32)**131 ± 7
    3 h346 ± 30 (1.26)**140 ± 9
    6 h336 ± 21 (1.22)*126 ± 5
    9 h338 ± 13 (1.23)*143 ± 10
    12 h285 ± 23178 ± 1
Submaxillary gland
    Control185 ± 6116 ± 5
    1 h294 ± 19 (1.59)**110 ± 7
    3 h364 ± 39 (1.97)**114 ± 8
    6 h218 ± 597 ± 5
    9 h195 ± 12122 ± 6
    12 h222 ± 9111 ± 9
Heart
    Control423 ± 1064.5 ± 2.3
    1 h505 ± 28 (1.19)**71.2 ± 3.6
    3 h500 ± 24 (1.18)**60.0 ± 1.1
    6 h436 ± 2260.3 ± 2.1
    9 h462 ± 1772.9 ± 3.5
    12 h459 ± 770.7 ± 3.0
Colon
    Control217 ± 790.3 ± 4.7
    1 h369 ± 14 (1.70)**74.3 ± 3.5
    3 h378 ± 46 (1.74)**94.3 ± 10.1
    6 h261 ± 1797.2 ± 5.2
    9 h274 ± 39101.7 ± 4.4
    12 h211 ± 970.6 ± 2.9
Lung
    Control225 ± 108.29 ± 0.44
    1 h325 ± 23 (1.44)*8.91 ± 0.72
    3 h374 ± 74 (1.66)**9.64 ± 0.57
    6 h244 ± 158.25 ± 0.82
    9 h235 ± 589.24 ± 1.62
    12 h264 ± 438.93 ± 0.86
Brain
    Control231 ± 51107 ± 31
    1 h257 ± 34980 ± 17
    3 h252 ± 191034 ± 48
    6 h234 ± 5975 ± 59
    12 h236 ± 71054 ± 69
  • * P < 0.05, significant difference from the control values.

  • ** P < 0.01, significant difference from the control values.