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Comparison of pharmacological properties of optical isomers and a racemic mixture of epinastine.
Arzneimittelforschung. 1991 Mar; 41(3):219-23.A

Abstract

Some pharmacological effects of d- and l-isomers of epinastine (WAL 801 CL, 3-amino-9,13b-dihydro-1H-dibenz [c,f]imidazo[1,5-a]azepine hydrochloride; CAS 80012-43-7) were studied in comparison with that of dl-epinastine. Although no significant difference was detected, d-epinastine is slightly more active than the l-isomer in the depressant actions of the central nervous system. However, in EEG power spectra recorded at the frontal cortex, occipital cortex, hippocampus and amygdala in conscious rats, no appreciable differences were recognized between two optical isomers and a racemic mixture. Furthermore, the extents of compound 48/80-induced lethality, antagonism on histamine-induced contraction of guinea pig ileum and histamine release from rat peritoneal mast cells were almost the same among the racemate and optical isomers of epinastine. In addition, two stereoisomers caused an almost equal degree of inhibition in antigen-induced histamine release from the lung pieces of sensitized guinea-pigs and the equivalent level of inhibition was exerted by the racemate.

Authors+Show Affiliations

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

1714277

Citation

Tasaka, K, et al. "Comparison of Pharmacological Properties of Optical Isomers and a Racemic Mixture of Epinastine." Arzneimittel-Forschung, vol. 41, no. 3, 1991, pp. 219-23.
Tasaka K, Kamei C, Izushi K, et al. Comparison of pharmacological properties of optical isomers and a racemic mixture of epinastine. Arzneimittelforschung. 1991;41(3):219-23.
Tasaka, K., Kamei, C., Izushi, K., Tsujimoto, S., & Yoshida, T. (1991). Comparison of pharmacological properties of optical isomers and a racemic mixture of epinastine. Arzneimittel-Forschung, 41(3), 219-23.
Tasaka K, et al. Comparison of Pharmacological Properties of Optical Isomers and a Racemic Mixture of Epinastine. Arzneimittelforschung. 1991;41(3):219-23. PubMed PMID: 1714277.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparison of pharmacological properties of optical isomers and a racemic mixture of epinastine. AU - Tasaka,K, AU - Kamei,C, AU - Izushi,K, AU - Tsujimoto,S, AU - Yoshida,T, PY - 1991/3/1/pubmed PY - 1991/3/1/medline PY - 1991/3/1/entrez SP - 219 EP - 23 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 41 IS - 3 N2 - Some pharmacological effects of d- and l-isomers of epinastine (WAL 801 CL, 3-amino-9,13b-dihydro-1H-dibenz [c,f]imidazo[1,5-a]azepine hydrochloride; CAS 80012-43-7) were studied in comparison with that of dl-epinastine. Although no significant difference was detected, d-epinastine is slightly more active than the l-isomer in the depressant actions of the central nervous system. However, in EEG power spectra recorded at the frontal cortex, occipital cortex, hippocampus and amygdala in conscious rats, no appreciable differences were recognized between two optical isomers and a racemic mixture. Furthermore, the extents of compound 48/80-induced lethality, antagonism on histamine-induced contraction of guinea pig ileum and histamine release from rat peritoneal mast cells were almost the same among the racemate and optical isomers of epinastine. In addition, two stereoisomers caused an almost equal degree of inhibition in antigen-induced histamine release from the lung pieces of sensitized guinea-pigs and the equivalent level of inhibition was exerted by the racemate. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/1714277/Comparison_of_pharmacological_properties_of_optical_isomers_and_a_racemic_mixture_of_epinastine_ DB - PRIME DP - Unbound Medicine ER -