An antihistamine with anticholinergic and antiserotonergic activities; histamine H1 receptor antagonist (Ki = 3.9 nM); inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and 5-HT-induced contractions in isolated rat uterus (EC50s = 6.5

Azatadine (maleate) – 250 mg

Brand:
Cayman
CAS:
3978-86-7
Storage:
-20
UN-No:
De Minimis - 3288 / 6.1

Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}  

 

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Description

An antihistamine with anticholinergic and antiserotonergic activities; histamine H1 receptor antagonist (Ki = 3.9 nM); inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and 5-HT-induced contractions in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively); delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs; prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively); increases survival in guinea pig and mouse models of anaphylactic shock (PD50s = 0.024 and 0.019 mg/kg, respectively)

Formal name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, (2Z)-2-butenedioate

Synonyms: 

Molecular weight: 522.6

CAS: 3978-86-7

Purity: ≥98%

Formulation: A solid

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