Inhibitory Effects of Emedastine Difumarate on Histamine Release.
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- Saito Tadayuki
- New Drug Research Laboratories, Kanebo, Ltd.
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- Hagihara Asako
- New Drug Research Laboratories, Kanebo, Ltd.
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- Igarashi Naoko
- New Drug Research Laboratories, Kanebo, Ltd.
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- Matsuda Naomi
- New Drug Research Laboratories, Kanebo, Ltd.
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- Yamashita Akira
- New Drug Research Laboratories, Kanebo, Ltd.
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- Ito Keizo
- New Drug Research Laboratories, Kanebo, Ltd.
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- Mio Mitsunobu
- Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University
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- Tasaka Kenji
- Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University
Bibliographic Information
- Other Title
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- Effects of Heparin on the Inhibitory Activities of Human Urinary Trypsin Inhibitor (Ulinastatin) on Trypsin, Chymotrypsin and Leukocyte Elastase
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Abstract
The inhibitory effects of emedastine difumarate on histamine release were studied in rat peritoneal mast cells. Emedastine significantly inhibited substance P (SP)-induced histamine release at concentrations above 10-9 M in the presence of extracellular Ca2+ and at concentrations above 10-11 M in its absence. At concentrations of 10-8 M or higher, emedastine significantly inhibited SP-induced Ca2- release from intracellular Ca stores and SP-induced 45Ca uptake into mast cells. Emedastine also inhibited passive peritoneal anaphylaxis in rats and guinea pigs. We conclude that the clinical antiallergic effects of emedastine involve the inhibition of histamine release and that this inhibition is mediated by the inhibition of Ca2+ release from intracellular Ca stores and the inhibition of Ca2+ influx into mast cells.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 62 (2), 137-143, 1993
The Japanese Pharmacological Society
