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Product Name: Cloperastine hydrochloride
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Dayang Chem (Hangzhou) Co., Ltd.
China
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Henan Tianfu Chemical Co., Ltd.
China
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14984-68-0

14984-68-0 structure

14984-68-0 structure

Name: Cloperastine hydrochloride
Chemical Name: Cloperastine hydrochloride
CAS Number: 14984-68-0
Molecular Formula: C₂₀H₂₅Cl₂NO
Molecular Weight: 366.325
Catalog: API Antiallergic Antihistamine
Create Date: 2018-06-16 18:24:35
Modify Date: 2024-01-07 09:58:15
Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM[1].

Name	Cloperastine hydrochloride
Synonyms	1-(2-((p-chloro-a-phenylbenzyl)oxy)ethyl)piperidine hydrochloride MFCD00079012 1-[2-[(4-Chlorophenyl)(phenyl)methoxy]ethyl]piperidine Hydrochloride Piperidine, 1-(2-((4-chlorophenyl)phenylmethoxy)ethyl)-, hydrochloride (9CI) Piperidine, 1-[2-[(4-chlorophenyl)phenylmethoxy]ethyl]-, hydrochloride (1:1) Cloperastine hydrochloride 4-Chlorobenzhydryl 2-(1-Piperidyl)ethyl Ether Hydrochloride 1-{2-[(4-Chlorophenyl)(phenyl)methoxy]ethyl}piperidine hydrochloride (1:1) 1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine,hydrochloride EINECS 239-067-8

Description	Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM[1].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
Target	27 nM (K+ currents)[1]
In Vitro	Cloperastine inhibits the hERG K+ currents in a concentrationdependent manner with an IC50 value of 27 nM[1]. Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also relaxes the bronchial musculature. Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects[2].
In Vivo	In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasicaction potential (MAP) duration without affecting PR interval or QRS width[1]. Cloperastine hydrochloride shows relatively low acute toxicity when administered by the intraperitoneal route in rats and mice, and shows minor toxicity by the oral route when administered as Cloperastine fendizoate, the LD50 in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively[2].
References	[1]. Takahara A, et al. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. J Pharmacol Sci. 2012;120(3):165-75. [2]. Catania MA, et al. Pharmacological and clinical overview of cloperastine in treatment of cough. Ther Clin Risk Manag. 2011;7:83-92.

Boiling Point	84°C 35mm
Molecular Formula	C₂₀H₂₅Cl₂NO
Molecular Weight	366.325
Flash Point	210.2ºC
Exact Mass	365.131317
PSA	12.47000
LogP	5.67180
Vapour Pressure	2.15E-07mmHg at 25°C
Index of Refraction	1.414

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM6491500

CHEMICAL NAME :: Piperidine, 1-(2-((p-chloro-alpha-phenylbenzyl)oxy)ethyl)-, hydrochloride

CAS REGISTRY NUMBER :: 14984-68-0

LAST UPDATED :: 199706

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C20-H24-Cl-N-O.Cl-H

MOLECULAR WEIGHT :: 366.36

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1986 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 553 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 140 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 80,1759,1960

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn:Harmful;
Risk Phrases	R22
Safety Phrases	S36
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	TM6491500
HS Code	2933399090

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%