47491-38-3
Chemical Structure
Desmethylazelastine
- CAS No.: 47491-38-3
- Formula:C21H22ClN3O
- Molecular Weight:367.87
IUPAC Name: 2-(azepan-4-yl)-4-(4-chlorobenzyl)phthalazin-1(2H)-one
InChIKey: WRYCMIFVXDQIKN-UHFFFAOYSA-N
SMILES: O=C1C2=C(C(CC3=CC=C(C=C3)Cl)=NN1C4CCNCCC4)C=CC=C2
Biological Activity: Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4][5].
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Desmethylazelastine | Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2. | |||||||||||||||||||||
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N-Desmethyl Azelastine-d4-1 | N-Desmethyl Azelastine-d4-1 is the deuterium labeled N-Desmethyl Azelastine. | |||||||||||||||||||||
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- [1]. Chand N, et al. Pharmacodynamic and pharmacokinetic studies with azelastine in the guinea pig: evidence for preferential distribution into the lung. Allergy. 1993 Jan;48(1):19-24. [Content Brief]
- [2]. Lieberman P, et al. Management of allergic rhinitis with a combination antihistamine/anti-inflammatory agent. J Allergy Clin Immunol. 1999 Mar;103(3 Pt 2):S400-4. [Content Brief]
- [3]. Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochloridel. Expert Rev Clin Immunol. 2005 Jul;1(2):191-201. [Content Brief]
- [4]. Mohamed M Elseweidy, et al. Azelastine a potent antihistamine agent, as hypolipidemic and modulator for aortic calcification in diabetic hyperlipidemic rats model. Arch Physiol Biochem. 2020 Jul 2;1-8. [Content Brief]
- [5]. Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1-7. [Content Brief]
