Effect of picumast on histamine release from rat cardiac and peritoneal mast cells.
Compound 48/80-induced histamine release (HR) from the isolated perfused rat heart was markedly and significantly inhibited by picumast (PIC), possibly by acting as a calmodulin antagonist (CMA) or membrane stabilizer. Trifluoperazine (TFP, another CMA in clinical use) had a similar effect. However, an action as CMA being the basis of inhibition of HR could not be confirmed in another 'allergy' model, namely HR from rat peritoneal mast cells (RPMC). PIC, TFP and two other CMA, W7 and N-(4-aminobutyl)-5-chloro-1-naphthalenesulfonamide) failed consistently to inhibit 48/80-induced HR from RPMC, and when used on their own at high concentration these compounds caused HR. PIC and TFP also potentiated the heat-induced haemolysis of rat erythrocytes, i.e. lacked membrane stabilizing effect in this model.
Wan
B Y
BY
Department of Pharmacology, University College London, UK.
Peh
K H
KH
Assem
E S
ES
D000818:Animals; D002147:Calmodulin / Q000037:antagonists & inhibitors; D003374:Coumarins / Q000494:pharmacology*; D006461:Hemolysis / Q000187:drug effects; D006633:Histamine Antagonists / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D006358:Hot Temperature; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000502:physiology*; D009206:Myocardium / Q000166:cytology*; D010529:Peritoneal Cavity / Q000166:cytology*; D051381:Rats; D011919:Rats, Inbred Strains; D014268:Trifluoperazine / Q000494:pharmacology; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology
D002147:Calmodulin; D003374:Coumarins; D006633:Histamine Antagonists; C013373:picumast; D014268:Trifluoperazine; D003189:p-Methoxy-N-methylphenethylamine