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In vitro and in vivo studies of the non-sedating antihistamine epinastine.
Arzneimittelforschung. 1988 Oct; 38(10):1446-53.A

Abstract

Epinastine (3-amino-9,13b-dihydro-1H-dibenz [c,f]imidazo[1,5-a]azepine hydrochloride, WAL 801 CL) was tested in vitro and in vivo in comparison with other H1-receptor antagonists. In the guinea pig ileum and in receptor binding studies the test substance showed a high affinity to H1-receptors. The following rank order was determined: WAL 801 CL greater than astemizole greater than terfenadine. These results were confirmed in vivo. The studies were carried out with oral and intravenous administration of WAL 801 CL to assess the inhibition of histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. 10- to 100fold antihistaminic doses of WAL 801 CL showed no effect on the sleeping-waking behaviour of cats. From this and other results it is suggested that the compound does not penetrate in the central nervous system. The action pattern of WAL 801 CL as a non-sedating antihistamine corresponds more to that of terfenadine than that of ketotifen.

Authors+Show Affiliations

Department of Pharmacology, Boehringer Ingelheim K.G. Ingelheim/Rhein, Fed. Rep. of Germany.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

2461715

Citation

Fügner, A, et al. "In Vitro and in Vivo Studies of the Non-sedating Antihistamine Epinastine." Arzneimittel-Forschung, vol. 38, no. 10, 1988, pp. 1446-53.
Fügner A, Bechtel WD, Kuhn FJ, et al. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung. 1988;38(10):1446-53.
Fügner, A., Bechtel, W. D., Kuhn, F. J., & Mierau, J. (1988). In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittel-Forschung, 38(10), 1446-53.
Fügner A, et al. In Vitro and in Vivo Studies of the Non-sedating Antihistamine Epinastine. Arzneimittelforschung. 1988;38(10):1446-53. PubMed PMID: 2461715.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro and in vivo studies of the non-sedating antihistamine epinastine. AU - Fügner,A, AU - Bechtel,W D, AU - Kuhn,F J, AU - Mierau,J, PY - 1988/10/1/pubmed PY - 1988/10/1/medline PY - 1988/10/1/entrez SP - 1446 EP - 53 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 38 IS - 10 N2 - Epinastine (3-amino-9,13b-dihydro-1H-dibenz [c,f]imidazo[1,5-a]azepine hydrochloride, WAL 801 CL) was tested in vitro and in vivo in comparison with other H1-receptor antagonists. In the guinea pig ileum and in receptor binding studies the test substance showed a high affinity to H1-receptors. The following rank order was determined: WAL 801 CL greater than astemizole greater than terfenadine. These results were confirmed in vivo. The studies were carried out with oral and intravenous administration of WAL 801 CL to assess the inhibition of histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. 10- to 100fold antihistaminic doses of WAL 801 CL showed no effect on the sleeping-waking behaviour of cats. From this and other results it is suggested that the compound does not penetrate in the central nervous system. The action pattern of WAL 801 CL as a non-sedating antihistamine corresponds more to that of terfenadine than that of ketotifen. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/2461715/In_vitro_and_in_vivo_studies_of_the_non_sedating_antihistamine_epinastine_ L2 - https://www.lens.org/lens/search/patent/list?q=citation_id:2461715 DB - PRIME DP - Unbound Medicine ER -