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.
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- No. CAS: 3964-81-6
- Fòrmula: C20H22N2
- Peso molecular:290.40
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Actividad biológica
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3964-81-6
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Peso molecular 290.40
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Fòrmula C20H22N2
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SMILES
CN1CC/C(CC1)=C2C3=CC=CC=C3CCC4=CC=CN=C4\2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Tozzi S, et al. The pharmacology of azatadine, a potential antiallergy drug. Agents Actions. 1974 Oct;4(4):264-70. [Content Brief]
[2]. Katelaris C, et al. Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. Asian Pac J Allergy Immunol. 1990;8(2):103-107. [Content Brief]
[3]. Togias AG, et al. Demonstration of inhibition of mediator release from human mast cells by azatadine base. In vivo and in vitro evaluation. JAMA. 1986 Jan 10;255(2):225-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Azatadine Related Classifications
HY-B0170 Related Classifications
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