Azatadine

Azatadine is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine induces sedation and exhibits topical anesthetic properties. Azatadine can be used for the research of allergic rhinitis^[1][2][3]. In Vitro:Azatadine (3.4 nM-13 nM; 3 minutes) competitively inhibits Histamine (HY-B1204)-induced contractions in isolated guinea-pig ileum segments with an ED₅₀ of 6.5 nM^[1].
Azatadine (6.8 nM-27 nM; 3 minutes) competitively inhibits acetylcholine-induced contractions in isolated guinea-pig ileum segments with an ED₅₀ of 10 nM^[1].
Azatadine (6.8 nM-27 nM; 3 minutes) inhibits Serotonin (HY-B1473A)-induced contractions in isolated unprimed virgin rat uterus segments with an ED₅₀ of 14 nM^[1].
Azatadine (50 μM-1 mM) dose-dependently inhibits anti-IgE-induced Histamine and Leukotriene C4 (HY-113446) release from human lung mast cells, with significantly greater inhibition of Leukotriene C4 release (85% at 1 mM) compared to histamine release (45% at 1 mM)^[3]. In Vivo:Azatadine (p.o.; single dose) exhibits potent in vivo antihistaminic activity in guinea-pigs, with an oral PD₅₀ of 0.009 mg/kg for protection against Histamine-induced lethality^[1].
Azatadine (p.o.; single dose) potently delays the onset of Histamine-induced dyspnea in guinea-pigs, with an oral ED₂₀₀ of 0.01 mg/kg^[1].
Azatadine (p.o.; single dose) delays the onset of acetylcholine-induced dyspnea in guinea-pigs, with an oral ED₂₀₀ of 0.739 mg/kg^[1].
Azatadine (p.o.; single dose) delays the onset of Serotonin-induced dyspnea in guinea-pigs with an oral ED₂₀₀ of 0.860 mg/kg^[1].
Azatadine (p.o.; single dose) exhibits potent antianaphylactic activity in sensitized guinea-pigs, with an oral PD₅₀ of 0.024 mg/kg for protection against anaphylactic shock^[1].
Azatadine (p.o.; single dose) potently protects pertussis-sensitized mice against Histamine-induced lethality, with an oral PD₅₀ of 0.022 mg/kg^[1].
Azatadine (p.o.; single dose) exhibits potent antianaphylactic activity in sensitized mice, with an oral PD₅₀ of 0.019 mg/kg for protection against anaphylactic shock^[1].