The protective effect of a new antiallergic agent, KP-136 on mast cell activation: a comparison with disodium cromoglycate.
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.
Kuriyama
K
K
Kyoto Research Laboratories, Kaken Pharmaceutical Co. Ltd., Japan.
Hiyama
Y
Y
Ito
K
K
Yoshinaka
I
I
Bito
Y
Y
D000818:Animals; D000001:Calcimycin / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism; D002867:Chromones / Q000494:pharmacology*; D004205:Cromolyn Sodium / Q000494:pharmacology*; D005260:Female; D006461:Hemolysis; D006358:Hot Temperature; D007166:Immunosuppressive Agents / Q000494:pharmacology*; D008407:Mast Cells / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism; D010741:Phospholipases A / Q000494:pharmacology; D054467:Phospholipases A2; D051381:Rats; D011919:Rats, Inbred Strains; D013777:Tetrazoles
D002867:Chromones; D007166:Immunosuppressive Agents; D013777:Tetrazoles; D000001:Calcimycin; C053066:KP 136; D010741:Phospholipases A; D054467:Phospholipases A2; D004205:Cromolyn Sodium; D002118:Calcium