Desmethylazelastine

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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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Desmethylazelastine Chemical Structure

CAS No. : 47491-38-3

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Other Forms of Desmethylazelastine:

N-Desmethyl Azelastine-d4 Get quote

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Description

In Vivo

1.19 Pharmacokinetic parameters of desmethylazelastine after a single oral administration of 1.0 mg/kg azelastine hydrochloride in guinea pigs^[1].

	Blood	Lung
C_max (ng/mL)^[a]	17.6	2863
T_max (h)	3.0-6.0	4.0-6.0
T_lag (h)	0.25	0.39
AUC_0-24 (ng•h/mL)^[a]	180	28502
t_1/2 (h)	4.24	3.90
CL (L/h)	0.213
Lung-blood ratio^[b]	146	146

^[a] For lung, the unit in grams (g) instead of milliliter (mL). ^[b] Mean value calculated from all time points.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

367.87

Formula

C₂₁H₂₂ClN₃O

CAS No.

47491-38-3

SMILES

O=C1C2=C(C(CC3=CC=C(C=C3)Cl)=NN1C4CCNCCC4)C=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]