Azatadine dimaleate

SKU: orb1310807

Description

Azatadine dimaleate

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 3978-86-7
• MW: 522.55
• Purity: 99.70%
• Formula: C₂₈H₃₀N₂O₈
• SMILES: OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CN1CC\C(CC1)=C1\c2ccccc2CCc2cccnc12
• Target: AChR,Histamine Receptor,5-HT Receptor
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:97 mg/mL (185.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.32 mM);H2O:96 mg/mL (183.71 mM)

Bioactivity

• Target IC50:
  Cholinergic:10 nM|Histamine receptor:6.5 nM
• In Vivo:
  Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a Cmax of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation, demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine (8.8 mg oral) in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis.
• In Vitro:
  95% of Azatadine is biotransformed in Sabouraud dextrose broth within 72 hours treatment with two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cholinergic, 5HT Receptor, 5HTReceptor, Azatadine, Azatadine dimaleate, Azatadine Dimaleate, Azatadine Maleate, inhibit, HT, HistamineReceptor, Histamine Receptor, Inhibitor, SCH 10649, SCH10649, SCH-10649

Compound Identifiers

PubChem CID

5281066