Pharmacology of the new H1-receptor antagonist setastine hydrochloride

J. Porszasz, F. Varga, K. G. Porszasz, J. Szolscanyi, L. Barthó, L. Petocz, L. Kapolnai

Research output: Contribution to journalArticle

3 Citations (Scopus)

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 sleping 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.

Original languageEnglish
Pages (from-to)1340-1345
Number of pages6
JournalArzneimittel-Forschung
Volume40
Issue number12
Publication statusPublished - 1990

Fingerprint

Histamine H1 Receptors
Pharmacology
Clemastine
Guinea Pigs
Histamine Antagonists
Rats
Central Nervous System Depressants
Histamine H1 Antagonists
Pyrilamine
Hexobarbital
Stupor
Bronchial Spasm
Fumarates
Adrenergic Antagonists
Cholinergic Antagonists
Neurology
Anaphylaxis
Amphetamine
setastine
Ileum

Keywords

  • antiallergic drugs
  • CAS 64294-95-7
  • clemastine
  • H-receptor antagonists
  • Loderix®
  • sentastine, pharmacology

ASJC Scopus subject areas

  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

Cite this

Porszasz, J., Varga, F., Porszasz, K. G., Szolscanyi, J., Barthó, L., Petocz, L., & Kapolnai, L. (1990). Pharmacology of the new H1-receptor antagonist setastine hydrochloride. Arzneimittel-Forschung, 40(12), 1340-1345.

Pharmacology of the new H1-receptor antagonist setastine hydrochloride. / Porszasz, J.; Varga, F.; Porszasz, K. G.; Szolscanyi, J.; Barthó, L.; Petocz, L.; Kapolnai, L.

In: Arzneimittel-Forschung, Vol. 40, No. 12, 1990, p. 1340-1345.

Research output: Contribution to journalArticle

Porszasz, J, Varga, F, Porszasz, KG, Szolscanyi, J, Barthó, L, Petocz, L & Kapolnai, L 1990, 'Pharmacology of the new H1-receptor antagonist setastine hydrochloride', Arzneimittel-Forschung, vol. 40, no. 12, pp. 1340-1345.
Porszasz J, Varga F, Porszasz KG, Szolscanyi J, Barthó L, Petocz L et al. Pharmacology of the new H1-receptor antagonist setastine hydrochloride. Arzneimittel-Forschung. 1990;40(12):1340-1345.
Porszasz, J. ; Varga, F. ; Porszasz, K. G. ; Szolscanyi, J. ; Barthó, L. ; Petocz, L. ; Kapolnai, L. / Pharmacology of the new H1-receptor antagonist setastine hydrochloride. In: Arzneimittel-Forschung. 1990 ; Vol. 40, No. 12. pp. 1340-1345.
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