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Antiallergic profile of the novel H1-antihistaminic compound levocabastine.
Arzneimittelforschung. 1993 Dec; 43(12):1331-7.A

Abstract

Levocabastine hydrochloride (R50 547, CAS79516-68-0) caused no inhibitory effect on the histamine release from rat peritoneal mast cells induced by compound 48/80, A23187 and concanavalin A. However, the drug inhibited histamine release from passively sensitized mast cells and passive peritoneal anaphylaxis in rats, though higher concentrations or doses were required. Moreover, levocabastine provided a relatively potent inhibitory effect on histamine release from lung pieces of actively sensitized guinea pigs exposed to antigen, and simultaneously the drug prevented a decrease in the cyclic AMP (cAMP) content. Levocabastine potently inhibited histamine-induced cutaneous reactions in rats and the drug also prevented histamine-induced contraction of isolated guinea pig ileum. Levocabastine did not induce any significant changes in platelet aggregation or in the contraction of guinea pig ileum induced by platelet activating factor (PAF). However, the drug inhibited eosinophil migration induced by PAF. The chemotaxis of neutrophils induced by N-formyl-methionyl-leucylphenylalanine (fMLP) was also inhibited by levocabastine in a dose-dependent fashion. Levocabastine has no influence on the order parameter tested with liposomes, suggesting that the drug provides no significant effect on the membrane fluidity of lipid bilayer. These results seem to indicate that the antiallergic effect of levocabastine is mainly dependent on its potent antihistaminic activity.

Authors+Show Affiliations

Tasaka K
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okyama University, Japan.
Kamei C
No affiliation info available
Akagi M
No affiliation info available
Mio M
No affiliation info available
Shirasaka T
No affiliation info available
Chokki M
No affiliation info available

MeSH

AnaphylaxisAnimalsChemotaxis, LeukocyteComplement Inactivator ProteinsCyclic AMPGuinea PigsHistamineHistamine H1 AntagonistsHistamine ReleaseHypersensitivityImmunoglobulin EIn Vitro TechniquesLungMaleMast CellsMiceMice, Inbred BALB CMuscle, SmoothPiperidinesPlatelet AggregationProstaglandins ERabbitsRatsRats, WistarSkin Tests

Pub Type(s)

Journal Article

Language

eng

PubMed ID

7511378

Citation

Tasaka, K, et al. "Antiallergic Profile of the Novel H1-antihistaminic Compound Levocabastine." Arzneimittel-Forschung, vol. 43, no. 12, 1993, pp. 1331-7.
Tasaka K, Kamei C, Akagi M, et al. Antiallergic profile of the novel H1-antihistaminic compound levocabastine. Arzneimittelforschung. 1993;43(12):1331-7.
Tasaka, K., Kamei, C., Akagi, M., Mio, M., Shirasaka, T., & Chokki, M. (1993). Antiallergic profile of the novel H1-antihistaminic compound levocabastine. Arzneimittel-Forschung, 43(12), 1331-7.
Tasaka K, et al. Antiallergic Profile of the Novel H1-antihistaminic Compound Levocabastine. Arzneimittelforschung. 1993;43(12):1331-7. PubMed PMID: 7511378.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antiallergic profile of the novel H1-antihistaminic compound levocabastine. AU - Tasaka,K, AU - Kamei,C, AU - Akagi,M, AU - Mio,M, AU - Shirasaka,T, AU - Chokki,M, PY - 1993/12/1/pubmed PY - 1993/12/1/medline PY - 1993/12/1/entrez SP - 1331 EP - 7 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 43 IS - 12 N2 - Levocabastine hydrochloride (R50 547, CAS79516-68-0) caused no inhibitory effect on the histamine release from rat peritoneal mast cells induced by compound 48/80, A23187 and concanavalin A. However, the drug inhibited histamine release from passively sensitized mast cells and passive peritoneal anaphylaxis in rats, though higher concentrations or doses were required. Moreover, levocabastine provided a relatively potent inhibitory effect on histamine release from lung pieces of actively sensitized guinea pigs exposed to antigen, and simultaneously the drug prevented a decrease in the cyclic AMP (cAMP) content. Levocabastine potently inhibited histamine-induced cutaneous reactions in rats and the drug also prevented histamine-induced contraction of isolated guinea pig ileum. Levocabastine did not induce any significant changes in platelet aggregation or in the contraction of guinea pig ileum induced by platelet activating factor (PAF). However, the drug inhibited eosinophil migration induced by PAF. The chemotaxis of neutrophils induced by N-formyl-methionyl-leucylphenylalanine (fMLP) was also inhibited by levocabastine in a dose-dependent fashion. Levocabastine has no influence on the order parameter tested with liposomes, suggesting that the drug provides no significant effect on the membrane fluidity of lipid bilayer. These results seem to indicate that the antiallergic effect of levocabastine is mainly dependent on its potent antihistaminic activity. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/7511378/Antiallergic_profile_of_the_novel_H1_antihistaminic_compound_levocabastine_ L2 - https://medlineplus.gov/allergy.html DB - PRIME DP - Unbound Medicine ER -