| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorbed well after oral administration. Metabolism/Metabolites Liver. |
|---|---|
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Occasional use of low-dose atazatta during lactation may be acceptable. Higher doses or prolonged use may cause infant drowsiness and other adverse reactions, or reduce milk production, especially when used in combination with sympathomimetic drugs (such as pseudoephedrine) or before lactation is fully established. Non-sedating antihistamines are a better alternative. ◉ Effects on Breastfed Infants As of the revision date, no published information was found regarding atazatta. In a telephone follow-up study, mothers reported irritability and colic in 10% of their infants after taking various antihistamines, and drowsiness in 1.6% of their infants. All reactions did not require medical attention. ◉ Effects on Lactation and Breast Milk Higher doses of injectable antihistamines can lower baseline serum prolactin levels in non-lactating women and early postpartum women. However, pre-natal administration of antihistamines by postpartum mothers does not affect suckling-induced prolactin secretion. Whether lower doses of oral antihistamines have the same effect on serum prolactin, and whether their effect on prolactin has any impact on breastfeeding success, is currently unstudied. For mothers who have already established lactation, their prolactin levels may not affect their ability to breastfeed. |
| Additional Infomation |
Atazatidine is a benzo[5,6]cycloheptano[1,2-b]pyridine compound with a 1-methylpiperidin-4-subunit linked at position 11. It is an H1 receptor antagonist and an antihistamine. It is a benzo[5,6]cycloheptanopyridine compound and also a tertiary amine. Antihistamines (such as atazatidine) appear to compete with histamine for histamine H1 receptor sites on effector cells. Antihistamines antagonize histamine by activating H1 receptor sites, thereby reducing the intensity of allergic reactions and tissue damage reactions involving histamine release. See also: Atazatidine maleate; Pseudoephedrine sulfate (note moved to).
Drug Indications For the relief of upper respiratory tract mucosal congestion caused by perennial and allergic rhinitis, and for the relief of nasal congestion and Eustachian tube congestion. Mechanism of Action Antihistamines such as atazattadine appear to compete with histamine for histamine H1 receptor sites on effector cells. Antihistamines antagonize histamine through pharmacological effects mediated by activation of H1 receptor sites, thereby reducing the intensity of allergic reactions and tissue damage reactions involving histamine release. Pharmacodynamics Atazattadine is an antihistamine associated with cyproheptadine and possesses antiserotonin, anticholinergic (dryness), and sedative effects. Atazattadine belongs to the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike other drugs in its class, atazattadine is not used clinically as an antipsychotic. Antihistamines antagonize the vasodilatory effects of endogenously released histamine, particularly in small vessels, and reduce histamine-induced increases in capillary permeability and edema formation. Due to these effects, antihistamines can antagonize the physiological manifestations of histamine release in the nasal cavity after antigen-antibody interaction, such as nasal congestion, mucosal edema, and copious watery secretions caused by vascular congestion, as well as stimulation and sneezing caused by histamine acting on afferent nerve endings. |
| Molecular Formula |
C20H22N2
|
|---|---|
| Molecular Weight |
290.40208
|
| Exact Mass |
290.178
|
| CAS # |
3964-81-6
|
| Related CAS # |
Azatadine dimaleate;3978-86-7
|
| PubChem CID |
19861
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.127 g/cm3
|
| Boiling Point |
450.1ºC at 760 mmHg
|
| Melting Point |
124-126ºC
|
| Flash Point |
226ºC
|
| LogP |
3.645
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
22
|
| Complexity |
417
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CC/C(CC1)=C2C3=CC=CC=C3CCC4=CC=CN=C4\2
|
| InChi Key |
SEBMTIQKRHYNIT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H22N2/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19/h2-7,12H,8-11,13-14H2,1H3
|
| Chemical Name |
2-(1-methylpiperidin-4-ylidene)-4-azatricyclo[9.4.0.03,8]pentadeca-1(15),3(8),4,6,11,13-hexaene
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4435 mL | 17.2176 mL | 34.4353 mL | |
| 5 mM | 0.6887 mL | 3.4435 mL | 6.8871 mL | |
| 10 mM | 0.3444 mL | 1.7218 mL | 3.4435 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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