Azatadine (dimaleate)
CAS No. : 3978-86-7
(Synonyms: Azatadine maleate)
| Size | Price | Stock |
|---|---|---|
| 25mg | $30 | In-stock |
| 50mg | $45 | In-stock |
| 100mg | $73 | In-stock |
| 200mg | $107 | In-stock |
| 500mg | $210 | In-stock |
| 1g | $295 | In-stock |
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| Cat. No. : | HY-B0170A |
| M.Wt: | 522.55 |
| Formula: | C28H30N2O8 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 100 mg/mL;H2O : ≥ 100 mg/mL |
Azatadine dimaleate (Azatadine maleate) is an orally active histamine H1 receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis[1][2][3].
In Vitro:Azatadine dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (p.o.; single dose) potently protects pertussis-sensitized mice against Histamine-induced lethality, with an oral PD50 of 0.022 mg/kg[1].
Azatadine dimaleate (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].
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