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Cloperastine fendizoate

Names

[ CAS No. ]:
85187-37-7

[ Name ]:
Cloperastine fendizoate

[Synonym ]:
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)

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
Research Areas >> Inflammation/Immunology

[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.


[Related Small Molecules]

Nigericin sodium salt | Senicapoc | E-4031 | 4-AMINOPYRIDINE | Ginsenoside Rg3 | TRAM-34 | Dofetilide | PAP-1 | Minoxidil | Flufenamic Acid | Flupirtine maleate | NS-1619 | Endoxifen (Z-isomer hydrochloride) | NS309 | Quinine

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℃

Related Compounds