Мы используем файлы cookie.
Продолжая использовать сайт, вы даете свое согласие на работу с этими файлами.
Antitussive
Cloperastine
Другие языки:

Cloperastine

Подписчиков: 0, рейтинг: 0
Cloperastine
Cloperastine.png
Clinical data
Other names HT-11
AHFS/Drugs.com International Drug Names
Routes of
administration		 Oral
ATC code
Identifiers
  • 1-[2-[(4-Chlorophenyl)-phenyl-methoxy]ethyl]piperidine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.020.948
Chemical and physical data
Formula C20H24ClNO
Molar mass 329.87 g·mol−1
3D model (JSmol)
  • Clc1ccc(cc1)C(OCCN2CCCCC2)c3ccccc3
  • InChI=1S/C20H24ClNO/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/h1,3-4,7-12,20H,2,5-6,13-16H2 checkY
  • Key:FLNXBVJLPJNOSI-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Cloperastine (INN) or cloperastin, in the forms of cloperastine hydrochloride (JAN) (brand names Hustazol, Nitossil, Seki) and cloperastine fendizoate (or hybenzoate), is an antitussive and antihistamine that is marketed as a cough suppressant in Japan, Hong Kong, and in some European countries. It was first introduced in 1972 in Japan, and then in Italy in 1981.

Side effects

Adverse effects may include sedation, drowsiness, heartburn, and thickening of bronchial secretions.

Pharmacology

The precise mechanism of action of cloperastine is not fully clear, but several different biological activities have been identified for the drug, of which include: ligand of the σ1 receptor (Ki = 20 nM) (likely an agonist),GIRK channel blocker (described as "potent"),antihistamine (Ki = 3.8 nM for the H1 receptor), and anticholinergic. It is thought that the latter two properties contribute to side effects, such as sedation and somnolence, while the former two may be involved in or responsible for the antitussive efficacy of cloperastine.

Synthesis

Synthesis: Patents: Isomers: China:

The halogenation of 4-Chlorobenzhydrol [119-56-2] (1) with phosphorus tribromide in tetrachloromethane gives 1-(Bromophenylmethyl)-4-chlorobenzene [948-54-9] (2). Treatment with ethylenechlorohydrin (2-Chloroethanol) [107-07-3] (3) gives 1-(4-Chlorobenzhydryl)oxy-2-chloroethane [5321-46-0] (4). Reaction with piperidine (5) completes the synthesis of Cloperastine (6).

See also


Новое сообщение