CAS NO: | 864750-70-9 |
规格: | 98% |
分子量: | 597.75 |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Background:
Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
The Kis of revefenacin are 0.42, 0.32, 0.18, 0.56, and 6.7 nM at human M1, M2, M3, M4 and M5 receptors, respectively. In a functional assay, revefenacin is shown to be a functional antagonist with inhibition constants similar to binding Ki’s. Revefenacin also inhibits agonist-induced contraction of guinea pig isolated tracheal ring preparation with an affinity of 0.1 nM, similar to the measured M3 biding Ki[1].
In anesthetized dogs, revefenacin, along with tiotropium and glycopyrronium, produce sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled revefenacin exhibits dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency is 45.0 µg/mL and the bronchoprotective potencies are maintained after 7 days of once-daily dosing[2].
[1]. Steinfeld T, et al. In vitro characterization of TD-4208, a lung-selective and long-acting muscarinic antagonist bronchodilator (Abstract). Am J Respir Crit Care Med 179:A4553. [2]. Pulido-Rios MT, et al. In vivo pharmacological characterization of TD-4208, a novel lung-selective inhaled muscarinic antagonist with sustained bronchoprotective effect in experimental animal models. J Pharmacol Exp Ther. 2013 Aug;346(2):241-50.