Cloperastine fendizoate
o-[(2'-hydroxy[1,1'-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1)
CAS: 85187-37-7
Molecular Formula: C40H38ClNO5
Cloperastine fendizoate - Names and Identifiers
| Name | o-[(2'-hydroxy[1,1'-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1) |
| Synonyms | Cloperastine Febdizoate Cloperastine fendizoate Levocloperastine Fendizoate Levocloperastine Fendizoate Racemic Impurity 1-[2-[(4-Chlorophenyl)phenylmethoxy]ethyl]piperidine Fendizoate 1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine,2-(4-hydroxy-3-phenylbenzoyl)benzoic acid |
| CAS | 85187-37-7 |
| EINECS | 286-126-9 |
| InChI | InChI=1/C20H24ClNO.C20H14O4/c21-19-11-9-18(10-12-19)20(17-7-3-1-4-8-17)23-16-15-22-13-5-2-6-14-22;21-18-11-10-14(12-17(18)13-6-2-1-3-7-13)19(22)15-8-4-5-9-16(15)20(23)24/h1,3-4,7-12,20H,2,5-6,13-16H2;1-12,21H,(H,23,24) |
Cloperastine fendizoate - Physico-chemical Properties
| Molecular Formula | C40H38ClNO5 |
| Molar Mass | 648.18642 |
| Melting Point | 185-187°C |
| Boling Point | 593.9°C at 760 mmHg |
| Flash Point | 327°C |
| Solubility | DMSO: ≥ 30 mg/mL |
| Vapor Presure | 5.95E-15mmHg at 25°C |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Stability | Hygroscopic |
| In vitro study | Cloperastine inhibits the hERG K + currents in a concentrationdependent manner with IC 50 value of 27±3 nM. 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. |
| In vivo study | In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasic action potential (MAP) duration without affecting PR interval or QRS width. 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 LD 50 in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively. |
Cloperastine fendizoate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.543 ml | 7.714 ml | 15.428 ml |
| 5 mM | 0.309 ml | 1.543 ml | 3.086 ml |
| 10 mM | 0.154 ml | 0.771 ml | 1.543 ml |
| 5 mM | 0.031 ml | 0.154 ml | 0.309 ml |
Last Update：2024-01-02 23:10:35
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