Azatadine

Modify Date: 2024-01-04 11:55:05

Azatadine Structure
Azatadine structure
Common Name Azatadine
CAS Number 3964-81-6 Molecular Weight 290.40
Density 1.127 g/cm3 Boiling Point 450.1ºC at 760 mmHg
Molecular Formula C20H22N2 Melting Point 124-126ºC
MSDS N/A Flash Point 226ºC

 Use of Azatadine


Azatadine 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.

 Names

Name azatadine
Synonym More Synonyms

 Azatadine Biological Activity

Description Azatadine 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.
Related Catalog
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.

 Chemical & Physical Properties

Density 1.127 g/cm3
Boiling Point 450.1ºC at 760 mmHg
Melting Point 124-126ºC
Molecular Formula C20H22N2
Molecular Weight 290.40
Flash Point 226ºC
PSA 16.13000
LogP 3.64560
Storage condition 2-8℃

 Safety Information

HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

11-(1-methyl-piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
11-(1-methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2Z)-but-2-enedioate (1:2)
Azatadinum [INN-Latin]
Azatadina [INN-Spanish]
11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine
Azatadina
Optimine
Azatadinum
Azatidine
5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2)
11-(1-Methyl-4-piperidinylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2Z)-2-butenedioate (1:2)
Azatadine [INN:BAN]
6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
6,11--dihydro-11-(N-methyl-4-piperidylidene)-5H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridine
Azatadine maleate
Zadine
AZATADINE