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Olopatadine (hydrochloride)

Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis. Target: Histamine Receptor Olopatadine hydrochloride (ALO4943A) is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine hydrochloride (ALO4943A) significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine hydrochloride (ALO4943A) was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of Olopatadine hydrochloride (ALO4943A) accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine hydrochloride (ALO4943A) is one of the few renal clearance drugs in antiallergic drugs. Olopatadine hydrochloride (ALO4943A) was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. Olopatadine hydrochloride (ALO4943A) inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by Olopatadine hydrochloride (ALO4943A) applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].

Product Specifications

CAS Number

[140462-76-6]

Product Name Alternative

ALO4943A; KW4679

UNSPSC

12352005

Hazard Statement

H301, H400

Target

Endogenous Metabolite; Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Olopatadine-hydrochloride.html

Purity

99.71

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 6.67 mg/mL (ultrasonic)

Smiles

O=C(O)CC1=CC=C(C/2=C1)OCC3=CC=CC=C3C2=C\CCN(C)C.Cl

Molecular Formula

C21H24ClNO3

Molecular Weight

373.87

Precautions

H301, H400

References & Citations

[1]Tamura, T., et al., Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology, 2005. 75 (1) : p. 45-52.|[2]Ohmori, K., et al., Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol, 2002. 88 (4) : p. 379-97.|[3]Yanni, J.M., et al., The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther, 1996. 12 (4) : p. 389-400.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Available Sizes

Curated Selection

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