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Olopatadine hydrochloride

CAS No.140462-76-6
Chemical Name:Olopatadine hydrochloride
CBNumber:CB0144403
Molecular Formula:C21H24ClNO3
Formula Weight:373.88
MOL File:140462-76-6.mol

Olopatadine hydrochloride Property

Melting point 242-245?C
storage temp. Inert atmosphere,Room Temperature
solubility H2O: ≥20mg/mL
form solid
color White to Light yellow
Water Solubility H2O: ≥20mg/mL
Merck 14,6840
BCS Class 3(CLogP), 1 (LogP)
InChI InChI=1S/C21H23NO3.ClH/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24;/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24);1H/b18-8-;
InChIKey HVRLZEKDTUEKQH-NOILCQHBSA-N
SMILES C(=C1/C2=CC=CC=C2COC2C=CC(CC(=O)O)=CC/1=2)\CCN(C)C.Cl
CAS DataBase Reference 140462-76-6(CAS DataBase Reference)
FDA UNII 2XG66W44KF
UNSPSC Code 41116107
NACRES NA.77

Safety

Hazard Codes :T,N
Risk Statements :25-50
Safety Statements :45-61
RIDADR :UN 2811 6.1 / PGIII
WGK Germany :3
RTECS :HQ4135060
HS Code :29329990

NFPA 704:

	0
2		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordDanger
Hazard statements H301-H400
Precautionary statements P273-P301+P310+P330

Olopatadine hydrochloride Price More Price(3)

Brand: Sigma-Aldrich(India)
Product number: O0391
Product name : Olopatadine hydrochloride
Purity: ≥98% (HPLC)
Packaging: 10MG
Price: ₹8183.7
Updated: 2022/06/14
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Brand: Sigma-Aldrich(India)
Product number: O0391
Product name : Olopatadine hydrochloride
Purity: ≥98% (HPLC)
Packaging: 50MG
Price: ₹34943.1
Updated: 2022/06/14
Buy: Buy

Brand: TCI Chemicals (India)
Product number: O0361
Product name : Olopatadine Hydrochloride
Purity:
Packaging: 1G
Price: ₹19500
Updated: 2022/05/26
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Olopatadine hydrochloride Chemical Properties,Usage,Production

Description Olopatadine hydrochloride is an ophthalmic antihistamine that inhibits release of histamine from mast cells and is a relatively selective histamine H1 antagonist. It inhibits type 1 immediate hypersensitivity reactions. Olopatadine hydrochloride is indicated in the temporary relief of itching caused by allergic conjunctivitis. H1 antagonists have an established and valued place in the symptomatic treatment of various immediate hypersensitivity reactions. In addition, the central properties of some of the series are of therapeutic value for suppressing motion sickness or for sedation.
Chemical Properties White Solid
Originator Kyowa Hakko (Japan)
Uses Dual acting histamine H1-receptor antagonist and mast cell stabilizer. Antiallergic; antihistaminic.
Uses Olopatadine hydrochloride is a potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively). It blocks histamine-induced phosphoinositide turnover in isolated cells (IC50 = 9.5-39.9 nM) and prevents passive cutaneous anaphylaxis in rats (ED50 = 49 μg/kg) and anaphylactic bronchoconstriction in guinea pigs (ID50 = 30 μg/kg). Olopatadine is effective in treating allergic rhinitis and conjunctivitis. It also suppresses itch in patients with well-controlled chronic urticaria. In humans, this antihistamine does not cause cognitive or psychomotor impairment at therapeutic doses.[Cayman Chemical]
Preparation Olopatadine hydrochloride can be prepared in five steps from the sodium salt of phydroxyphenylacetic acid methyl ester with phthalide.
Definition ChEBI: Olopatadine hydrochloride is a dibenzooxazepine.
brand name Patanol (Alcon).
Pharmacokinetics Olopatadine hydrochloride was launched in the US for use in allergic conjunctivitis. It has a fast onset of action with a long duration of action (due to slow dissociation kinetics) that combines the ability to prevent human conjunctival mast cell mediator release with selective H1-receptor antangonistic activity (greater H3:H1 selectivity than H2:H1 selectivity). In addition, Olopatadine hydrochloride had no inhibition of 5-lipoxygenase, PAF acetyltransferase and thromboxane synthase while interfering with phospholipase A2. It has a presynaptic inhibition of tachykinin release and inhibits bronchial sensory nerves through activation of small conductance calcium activated potassium channels. It was more potent than ketotifen and terfenadine and was effective at inhibition of PAF, LTC4 induced conjunctivitis and TXB2 production. It does not accumulate in the CNS, has a low affinity for H1-receptors in the brain, and significantly inhibits allergen induce sneezing. Olopatadine hydrochloride was more effective in conjuctival than in corneal or the trabecuiar meshwork cells.
Veterinary Drugs and Treatments Olopatadine HCl is a selective H₁ receptor antagonist and inhibitor of histamine release from mast cells. It is marketed for topical use to alleviate symptoms of allergic conjunctivitis in humans and is thought to be safe for use in children three years of age and older. Olopatadine, upon topical application in humans, was shown to have very limited systemic absorption. It was detectable in the milk of nursing rats, after topical application, and like most medications should be avoided in pregnant or nursing animals.
storage Desiccate at RT