Cloperastine fendizoate

Modify Date: 2024-01-18 08:20:55

Cloperastine fendizoate Structure
Cloperastine fendizoate structure
Common Name Cloperastine fendizoate
CAS Number 85187-37-7 Molecular Weight 648.186
Density N/A Boiling Point 593.9ºC at 760 mmHg
Molecular Formula C40H38ClNO5 Melting Point N/A
MSDS N/A Flash Point 327ºC

 Use of Cloperastine fendizoate


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

 Names

Name 1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine,2-(4-hydroxy-3-phenylbenzoyl)benzoic acid
Synonym More Synonyms

 Cloperastine fendizoate Biological Activity

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

27 nM (K+ currents)[1]

In Vitro Cloperastine inhibits the hERG K+ currents in a concentrationdependent manner with IC50 value of 27±3 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 593.9ºC at 760 mmHg
Molecular Formula C40H38ClNO5
Molecular Weight 648.186
Flash Point 327ºC
Exact Mass 647.243835
PSA 87.07000
LogP 8.85820
Storage condition 2-8℃

 Synonyms

cloperastine fendizoate
EINECS 286-126-9
Benzoic acid,2-((6-hydroxy(1,1'-biphenyl)-3-yl)carbonyl)-,compd. with 1-(2-((4-chlorophenyl)phenylmethoxy)ethyl)piperidine (1:1)
Benzoic acid, 2-[(6-hydroxy[1,1'-biphenyl]-3-yl)carbonyl]-, compd. with 1-[2-[(4-chlorophenyl)phenylmethoxy]ethyl]piperidine (1:1)
Cloperastine fendizoate (JAN)
UNII:2M105305SU
o-((2'-Hydroxy(1,1'-biphenyl)-4-yl)carbonyl)benzoic acid,compoundwith 1-(2-(4-chlorobenzhydryloxy)ethyl)piperidine (1:1)
2-[(6-Hydroxy-3-biphenylyl)carbonyl]benzoic acid - 1-{2-[(4-chlorophenyl)(phenyl)methoxy]ethyl}piperidine (1:1)
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