Azatadine (maleate)

Azatadine is an antihistamine with anticholinergic and antiserotonergic activities., It is a histamine H1 receptor antagonist (Ki = 3.9 nM)., Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT, Cay-14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively). 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). 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.Formal Name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, (2Z)-2-butenedioate. CAS Number: 3978-86-7. Molecular Formula: C20H22N2 . 2C4H4O4. Formula Weight: 522.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20mg/mL, DMSO: 20mg/mL, Ethanol: 5mg/mL, PBS (pH 7.2): 10mg/mL. SMILES: CN(CC/1)CCC1=C2C(N=CC=C3)=C3CCC4=C\2C=CC=C4.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O. InChi Code: InChI=1S/C20H22N2.2C4H4O4/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)19,2*5-3(6)1-2-4(7)8/h2-7,12H,8-11,13-14H2,1H3,2*1-2H,(H,5,6)(H,7,8)/b,2*2-1-. InChi Key: SGHXFFAHXTZRQM-SPIKMXEPSA-N.