CAS 140462-76-6|Olopatadine Hydrochloride

Introduction：Basic information about CAS 140462-76-6|Olopatadine Hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Olopatadine Hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Articles35
7. Synonyms

Common Name	Olopatadine Hydrochloride
CAS Number	140462-76-6	Molecular Weight	373.873
Density	1.221 g/cm3	Boiling Point	523ºC at 760mmHg
Molecular Formula	C₂₁H₂₄ClNO₃	Melting Point	242-245ºC
MSDS	ChineseUSA	Flash Point	270.1ºC
Symbol	GHS06, GHS09	Signal Word	Danger

Names

Name	Olopatadine Hydrochloride
Synonym	More Synonyms

Olopatadine Hydrochloride BiologicalActivity

Description	Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine 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 was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A 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 AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology
References	[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.

Description

Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine 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 was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A 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 AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology

References

[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.

Chemical & Physical Properties

Density	1.221 g/cm3
Boiling Point	523ºC at 760mmHg
Melting Point	242-245ºC
Molecular Formula	C₂₁H₂₄ClNO₃
Molecular Weight	373.873
Flash Point	270.1ºC
Exact Mass	373.144470
PSA	49.77000
LogP	4.39150
Vapour Pressure	9.65E-13mmHg at 25°C
InChIKey	HVRLZEKDTUEKQH-NOILCQHBSA-N
SMILES	CN(C)CCC=C1c2ccccc2COc2ccc(CC(=O)O)cc21.Cl
Storage condition	Refrigerator

Safety Information

Symbol	GHS06, GHS09
Signal Word	Danger
Hazard Statements	H301-H400
Precautionary Statements	P273-P301 + P310
Hazard Codes	T,N
Risk Phrases	25-50
Safety Phrases	45-61
RIDADR	UN 2811 6.1 / PGIII
HS Code	2932999099

Customs

HS Code	2932999099
Summary	2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles35

Topical cyclosporine a 1% for the treatment of chronic ocular surface inflammation.

Eye Contact Lens 40(5) , 283-8, (2014)

To evaluate the use of topical cyclosporine A (CsA) 1% emulsion in the treatment of chronic ocular surface inflammation (OSI).We conducted a retrospective chart review of patients with various forms o...

Histamine suppresses regulatory T cells mediated by TGF-β in murine chronic allergic contact dermatitis.

Exp. Dermatol. 24(4) , 280-4, (2015)

Regulatory T cells (Tregs) suppress effector T cells and ameliorate contact hypersensitivity (CH); however, the role of Tregs in chronic allergic contact dermatitis (CACD) has not been assessed. Repea...

Chromatographic analysis of olopatadine in hydrophilic interaction liquid chromatography.

J. Chromatogr. Sci. 53 , 680-6, (2015)

In this paper, chromatographic analysis of active substance olopatadine hydrochloride, which is used in eye drops as antihistaminic agent, and its impurity E isomer by hydrophilic interaction liquid c...

Synonyms

AL 4943A

MFCD00875716

Olopatadine hydrochloride

Dibenz[b,e]oxepin-2-acetic acid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, (11Z)-, hydrochloride (1:1)

{(11Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}acetic acid hydrochloride

{(11Z)-11-[3-(Dimethylamino)propyliden]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}essigsäurehydrochlorid

{(11Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}acetic acid hydrochloride (1:1)

dibenz[b,e]oxepin-2-acetic acid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, (11Z)-, hydrochloride

acide {(11Z)-11-[3-(diméthylamino)propylidène]-6,11-dihydrodibenzo[b,e]oxépin-2-yl}acétique chlorhydrate

Olopatadine (hydrochloride)

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