Cloperastine
Cloperastine or cloperastin, in the forms of cloperastine hydrochloride and cloperastine fendizoate, is an antitussive and antihistamine that is marketed as a cough suppressant in Japan, Hong Kong, Brazil and in some European countries. It was first introduced in 1972 in Japan, and then in Italy in 1981.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 , GIRK channel blocker, antihistamine, 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
The halogenation of 4-Chlorobenzhydrol with phosphorus tribromide in tetrachloromethane gives 1--4-chlorobenzene . Treatment with ethylenechlorohydrin gives 1-oxy-2-chloroethane . Reaction with piperidine completes the synthesis of Cloperastine.