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Olopatadine hydrochloride

Product Name
Olopatadine hydrochloride
CAS No.
140462-76-6
Chemical Name
Olopatadine hydrochloride
Synonyms
OLOPATADINE HCL;Patanol;Olopatadin HCL;OLAPATADINE HCL;Olopatadine Hydrochlorde;ALO4943A;AL-4943A;Opatanol;OLOPATDINEHYDROCHLORIDE;Olatadine hydrochloride
CBNumber
CB0144403
Molecular Formula
C21H24ClNO3
Formula Weight
373.88
MOL File
140462-76-6.mol
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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
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)
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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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
O0391
Product name
Olopatadine hydrochloride
Purity
≥98% (HPLC)
Packaging
10mg
Price
$86
Updated
2024/03/01
Sigma-Aldrich
Product number
1478403
Product name
Olopatadine hydrochloride
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
150mg
Price
$598
Updated
2024/03/01
TCI Chemical
Product number
O0361
Product name
Olopatadine Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$284
Updated
2024/03/01
Cayman Chemical
Product number
11999
Product name
Olopatadine (hydrochloride)
Purity
≥98%
Packaging
10mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
11999
Product name
Olopatadine (hydrochloride)
Purity
≥98%
Packaging
25mg
Price
$81
Updated
2024/03/01
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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

Olopatadine hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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Olopatadine hydrochloride Suppliers

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View Lastest Price from Olopatadine hydrochloride manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Olopatadine hydrochloride 140462-76-6
Price
US $0.00-0.00/KG
Min. Order
100g
Purity
98%-102%
Supply Ability
10KGS
Release date
2021-06-07
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Olopatadine Hydrochloride 140462-76-6
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
50kg/Month
Release date
2024-09-19
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Olopatadine Hydrochloride. 140462-76-6
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-11-15

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