overview | frostidine (fesoterodine, trade name ToviazTM) is a new type of m receptor blocker, which is rapidly metabolized into active metabolites in the body and plays a role. |
use | Frostine was approved by FDA on October 31, 2008 for the treatment of overactive bladder (overactivebladder,OAB). |
Biological activity | Fesoterodine is an orally effective, non-subtype selective, competitive muscarinic receptor (mAChR) antagonist. The pKi values for M1,M2,M3,M4,M5 receptors are 8.0,7.7,7.4,7.3,7.5, respectively. Fesoterodine for overactive bladder (OAB). |
target | pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5) |
Animal Model:
| Bladders from female Sprague-Dawley rats (225-275 g) |
Dosage:
| 0.01, 0.1 and 1 mg/kg |
Administration:
| IV |
Result:
| Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg. |