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Navafenterol saccharinate

CAS No. : 1648550-37-1

MCE 站：Navafenterol saccharinate

产品活性：Navafenterol?(AZD-8871) 是一种吸入型的双效、选择性和持久的 M3-拮抗剂/β2-激动剂 (MABA)，具有持久作用和良好的安全性。对人 M3 受体的 pIC₅₀ 为 9.5，β2-肾上腺素受体的 pEC₅₀ 为 9.5。Navafenterol 可用于慢性阻塞性肺疾病 (COPD) 的研究。具有支气管保护和抗唾液分泌作用，且具有良好的心血管特征。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mAChR  |  Adrenergic Receptor

In Vitro: The pIC₅₀?values of Navafenterol?(AZD-8871) at the human M1, M2, M3, M4, and M5?receptor are 9.9, 9.9, 9.5, 10.4, and 8.8, respectively.
pEC₅₀?values of Navafenterol at theβ1, β2, and β3 adrenoceptor are 9.0, 9.5, and 8.7, respectively. It is selective for the?β2-adrenoceptor over the?β1?and?β3?subtypes (3- and 6-fold, respectively).
Navafenterol shows kinetic selectivity for the M3?(half-life: 4.97 hours) over the M2?receptor (half-life: 0.46 hour).
Navafenterol?shows dual antimuscarinic and?β2-adrenoceptor functional activity in isolated guinea pig tissue (pIC₅₀?in electrically stimulated trachea: 8.6; pEC₅₀?in spontaneous tone isolated trachea: 8.8, respectively), which are sustained over time.

In Vivo: Navafenterol?(AZD-8871) prevents acetylcholine-induced bronchoconstriction in both guinea pig and dog with minimal effects on salivation and heart rate at doses with bronchoprotective activity. Moreover, AZD8871 shows long-lasting effects in dog, with a bronchoprotective half-life longer than 24 hours. Navafenterol?shows dose-proportional bronchoprotective effect, with a nonsignificantly different potency (ID₄₀?of 0.40 ?g/kg).

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