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AZD-8871

Product NameAZD-8871
CAS1435519-06-4
MFC38H42N6O6S2
MW742.91
EINECS
MOL File1435519-06-4.mol

Chemical Properties

Boiling point	988.8±65.0 °C(Predicted)
Density	1.45±0.1 g/cm3(Predicted)
pka	8.88±0.20(Predicted)

Usage And Synthesis

Uses

Navafenterol (AZD-8871) 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 can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].

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 μg/kg)^[1].

Animal Model:	Male Dunkin Hartley guinea pigs (body weight 340-600 g)bearing bronchoconstriction model^[1]
Dosage:	10, 30, 100, and 300μg/mL
Administration:	Administered by aerosol
Result:	Inhibited the bronchoconstriction in a concentration-response manner with the IC₅₀value of 2.1μg/mL. Exhibited the antisialagogue effect with a maximal inhibition of sialorrhea of 65%±11% at 300μg/mL and an estimated IC₅₀of 138.4 μg/mL.

Animal Model:	Male anesthetized Beagle dogs^[1]
Dosage:	0.3, 1, 3, or 10μg/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 (0.3-10μg/kg). Showed long-lasting effects at 10μg/kg, with a 79% ± 3.6% of bronchoprotection at 24 hours and a calculated half-life longer than 24 hours.

IC 50

mAChR3

References

[1] Mònica Aparici, et al. Pharmacological Profile of AZD8871 (LAS191351), a Novel Inhaled Dual M3Receptor Antagonist/β2-Adrenoceptor Agonist Molecule with Long-Lasting Effects and Favorable Safety Profile. J Pharmacol Exp Ther.2019 Jul;370(1):127-136. DOI:10.1124/jpet.118.255620

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