These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Pharmacology of the new H1-receptor antagonist setastine hydrochloride.
    Author: Porszász J, Varga F, Porszász KG, Szolscányi J, Barthó L, Petöcz L, Kápolnai L.
    Journal: Arzneimittelforschung; 1990 Dec; 40(12):1340-5. PubMed ID: 1982751.
    Abstract:
    Setastine HCl (N-(1-phenyl-1-[4-chlorophenyl])-etoxy-ethylene-perhydroazepine hydrochloride, Loderix; CAS 64294-95-7) is a potent antagonist of histamine H1-receptor mediated responses. The antihistamine activity of the compound is similar to that of clemastine fumarate in the following assays: histamine-induced lethality and bronchospasm in guinea-pigs, plasma extravasation in rats, and contractile action in isolated guinea-pig ileum. Setastine HCl inhibits anaphylactic shock in guinea-pigs sensitized by horse serum. No antiserotonin, anticholinergic and antiadrenergic effect of the compound can be detected. Setastine HCl has a long lasting (up to 16 h) antihistamine effect with a good oral effectiveness. It shows no cardiovascular effects in cats. Setastine HCl shows a much weaker CNS depressant activity than clemestine fumarate measuring inhibition of amphetamine-induced hypermotility, rotarod performance, potentiation of ethanol-narcosis in mice, and prolongation of hexobarbital sleeping time in rats. In displacement studies (3H-mepyramine) setastine HCl had significantly weaker affinity for the central nervous system (CNS) H1-receptors than clemastine fumarate. It is concluded that setastine HCl is a non-sedative highly active H1-antagonist.
    [Abstract] [Full Text] [Related] [New Search]