Azatadine

Names

[ Name ]:
Azatadine

[Synonym ]:
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

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]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

[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.

[Related Small Molecules]

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

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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%

Related Compounds

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