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

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.

• Authors: K Kuriyama, Y Hiyama, K Ito, I Yoshinaka, Y Bito
• Journal: Agents and actions (Agents Actions) Vol. 25 Issue 3-4 Pg. 321-5 (Dec 1988) ISSN: 0065-4299 [Print] Switzerland
• PMID: 3146215 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Chromones
• Immunosuppressive Agents
• Tetrazoles
• Calcimycin
• KP 136
• Phospholipases A
• Phospholipases A2
• Cromolyn Sodium
• Calcium

Topics

• 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