Azatadine dimaleate |
| Catalog No.GC15776 |
Histamine and cholinergic inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3978-86-7
Sample solution is provided at 25 µL, 10mM.
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Azatadine dimaleate is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.Target: Histamine ReceptorAzatadine, a new antihistamine, was evaluated for its efficacy in 20 patients with chronic allergic rhinitis. Eighty percent of patients had symptomatic relief with a twice daily dosage of 2 mg. Sedation was volunteered as a side effect by six of the patients and was admitted by two further patients after specific questioning. A choice reaction time test gave slowing of motor function in these sedated patients. Four of the previously sedated patients experienced good symptomatic control with minimal sedation when the azatadine dose was reduced to 1 mg twice daily; slowing of motor function was not observed at this, the normal recommended dose.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.
References:
[1]. Wilson JD, et al. Azatadine maleate (Zadine): evaluation in the management of allergic rhinitis. N Z Med J. 1981 Aug 12;94(689):79-81.
[2]. Tozzi S, et al. The pharmacology of azatadine, a potential antiallergy drug. Agents Actions. 1974 Oct;4(4):264-70.
| Cas No. | 3978-86-7 | SDF | |
| Chemical Name | (Z)-but-2-enedioic acid;11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine | ||
| Canonical SMILES | CN1CCC(=C2C3=CC=CC=C3CCC4=C2N=CC=C4)CC1.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O | ||
| Formula | C28H30N2O8 | M.Wt | 522.55 |
| Solubility | DMF: 20mg/mL,DMSO: 20mg/mL,Ethanol: 5mg/mL,PBS (pH 7.2): 10mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9137 mL | 9.5685 mL | 19.1369 mL |
| 5 mM | 0.3827 mL | 1.9137 mL | 3.8274 mL |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9137 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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