Cloperastine hydrochloride

Modify Date: 2024-01-07 09:58:15

Cloperastine hydrochloride Structure
Cloperastine hydrochloride structure
Common Name Cloperastine hydrochloride
CAS Number 14984-68-0 Molecular Weight 366.325
Density N/A Boiling Point 84°C 35mm
Molecular Formula C20H25Cl2NO Melting Point N/A
MSDS Chinese USA Flash Point 210.2ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Cloperastine hydrochloride


Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM[1].

 Names

Name Cloperastine hydrochloride
Synonym More Synonyms

 Cloperastine hydrochloride Biological Activity

Description Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM[1].
Related Catalog
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.

 Chemical & Physical Properties

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

 Toxicological Information

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

 Safety Information

Symbol GHS07
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

 Customs

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%

 Articles14

More Articles
[Novel antidepressant-like action of drugs possessing GIRK channel blocking action in rats].

Yakugaku Zasshi 130(5) , 699-705, (2010)

We have previously found that antitussive drugs inhibit G protein-coupled inwardly rectifying potassium (GIRK) channel currents in brain neurons. Potassium efflux through GIRK channels causes membrane...

Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs.

J. Pharmacol. Sci. 120(3) , 165-75, (2012)

Cloperastine is an antitussive drug, which can be received as an over-the-counter cold medicine. The chemical structure of cloperastine is quite similar to that of the antihistamine drug diphenhydrami...

Levocloperastine in the treatment of chronic nonproductive cough: comparative efficacy versus standard antitussive agents.

Drugs Exp. Clin. Res. 30(4) , 133-41, (2004)

The medical and social impact of cough is substantial. Current antitussive agents at effective doses have adverse events such as drowsiness, nausea and constipation that limit their use. There is also...

 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
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