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PMID: 3146215 Published · ppublish English Comparative Study Journal Article

The protective effect of a new antiallergic agent, KP-136 on mast cell activation: a comparison with disodium cromoglycate.

Agents and actions ·Vol. 25 ·No. 3-4 ·1988-12-00 ·Pages 321-5

Kuriyama K, Hiyama Y, Ito K, Yoshinaka I, Bito Y

Abstract

The protective effects on mast cell activation were compared between a new antiallergic agent, KP-136 and disodium cromoglycate (DSCG), both of which inhibited the immunological degranulation of rat peritoneal mast cells. The IC50 was 0.03 micrograms/ml for KP-136 and 4.7 micrograms/ml for DSCG. KP-136 predominantly acted on the early stage of mast cell activation processes and inhibited the immunological increase in 45Ca uptake. KP-136 also inhibited A23187- and heat-induced degranulation and heat-induced hemolysis. In addition, KP-136 was effective on phospholipase A2-induced degranulation, although the compound did not directly affect the enzyme activity. In all tests for comparison, KP-136 and DSCG had similar profiles of action and the parallel experiments indicated that KP-136 was a more potent inhibitor of mast cell activation than DSCG, having a DSCG-like membrane stabilizing activity.

MeSH Terms
Animals Calcimycin/pharmacology Calcium/metabolism Chromones/pharmacology Cromolyn Sodium/pharmacology Female Hemolysis Hot Temperature Immunosuppressive Agents/pharmacology Mast Cells/drug effects,immunology,metabolism Phospholipases A/pharmacology Phospholipases A2 Rats Rats, Inbred Strains Tetrazoles
Chemicals
Chromones Immunosuppressive Agents Tetrazoles Calcimycin KP 136 Phospholipases A Phospholipases A2 Cromolyn Sodium Calcium
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Kuriyama K
Kyoto Research Laboratories, Kaken Pharmaceutical Co. Ltd., Japan.
Hiyama Y
Ito K
Yoshinaka I
Bito Y
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17 references, click to expand
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Article Info
Journal
Agents and actions
Abbr.
Agents Actions
ISSN
0065-4299
DOI
10.1007/BF01965038
Published
1988-12-00
Pages
321-5
Language
English
Region
Switzerland
NLM ID
0213341
Subset
IM
External Links
PubMed source DOI: 10.1007/BF01965038
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