Table 2.
Competitive inhibition by darifenacin of specific [N-methyl-3H]scopolamine methyl chloride ([3H]NMS) binding in the submandibular gland and bladder of wild type (WT), M2 and M3 knockout (KO) mice
Submandibular gland |
Bladder |
Ki (submandibular gland)/Ki (bladder) | |||
---|---|---|---|---|---|
Ki (nmol·L−1) | nH | Ki (nmol·L−1) | nH | ||
WT | 3.0 ± 0.6* | 0.8 ± 0.1 | 24 ± 7 | 0.6 ± 0.1 | 0.1 |
M2KO | 4.3 ± 0.9## | 1.0 ± 0.1† | 2.5 ± 0.7†,# | 1.0 ± 0.2† | 1.7 |
M3KO | 19 ± 2*,†† | 1.1 ± 0.1† | 43 ± 10† | 0.9 ± 0.1† | 0.4 |
The submandibular gland and bladder were taken from WT and muscarinic acetylcholine receptor (M2, M3) KO mice. Specific [3H]NMS binding in the submandibular gland (0.1 nmol·L−1) and bladder (0.2 nmol·L−1) was measured in the absence and presence of five to six different concentrations (0.3 nmol·L−1–3 µmol·L−1) of darifenacin, and the values of Ki and Hill coefficients (nH) were estimated. Values represent the mean ± SEM of three to six determinations.
Symbols show a significant difference from the values for bladder in the same group of mice
(P < 0.05), a significant difference from the values for the same tissue in WT mice
(P < 0.05,
P < 0.001) and a significant difference from the values for the same tissue in M3KO mice
(P < 0.05,
P < 0.001).