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编 号：F746552
分子式：C45H47N7O9S3
分子量：926.09
分子式：C45H47N7O9S3
分子量：926.09
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CAS No: 1648550-37-1
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生物活性：
Navafenterol?(AZD-8871) saccharinate?is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3?receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD).?Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
体内研究：
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 μg/kg).Animal Model:Male Dunkin Hartley guinea pigs (body weight 340-600 g)?bearing bronchoconstriction model?
Dosage:10, 30, 100, and 300?μg/mL
Administration:Administered by aerosol
Result:Inhibited the bronchoconstriction in a concentration-response manner with the IC50?value of 2.1?μg/mL.Exhibited the antisialagogue effect with a maximal inhibition of sialorrhea of 65%±11% at 300?μg/mL and an estimated IC50?of 138.4 μg/mL.
Animal Model:Male anesthetized Beagle dogs
Dosage:0.3, 1, 3, or 10?μg/kg
Administration:Administered as nebulized liquid aerosols; the administration volume was 3 mL
Result:Showed significant effects over 24 hours at all the doses tested (0.3-10?μg/kg).Showed long-lasting effects at 10?μg/kg, with a 79% ± 3.6% of bronchoprotection at 24 hours and a calculated half-life longer than 24 hours.?
体外研究：
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.
Navafenterol?(AZD-8871) saccharinate?is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3?receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD).?Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
体内研究：
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 μg/kg).Animal Model:Male Dunkin Hartley guinea pigs (body weight 340-600 g)?bearing bronchoconstriction model?
Dosage:10, 30, 100, and 300?μg/mL
Administration:Administered by aerosol
Result:Inhibited the bronchoconstriction in a concentration-response manner with the IC50?value of 2.1?μg/mL.Exhibited the antisialagogue effect with a maximal inhibition of sialorrhea of 65%±11% at 300?μg/mL and an estimated IC50?of 138.4 μg/mL.
Animal Model:Male anesthetized Beagle dogs
Dosage:0.3, 1, 3, or 10?μg/kg
Administration:Administered as nebulized liquid aerosols; the administration volume was 3 mL
Result:Showed significant effects over 24 hours at all the doses tested (0.3-10?μg/kg).Showed long-lasting effects at 10?μg/kg, with a 79% ± 3.6% of bronchoprotection at 24 hours and a calculated half-life longer than 24 hours.?
体外研究：
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.
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