title: The effect of azelastine and some other antiasthmatic and antiallergic drugs on calmodulin and protein kinase C.
abstract: The antiallergic and antiasthmatic drug, azelastine, interacts strongly with calmodulin (but not bovine serum albumin) as determined by an indirect assay; it also moderately inhibited the Ca2+-calmodulin-dependent enzyme bovine brain phosphodiesterase. Ketotifen was less active than azelastine in both assays of calmodulin reactivity and both drugs were less active than the recognized calmodulin inhibitor, W-7. Neither azelastine nor ketotifen had any inhibitory effect on the Ca2+- and phospholipid-dependent protein kinase C. A number of other commonly employed antiallergic and antiasthmatic drugs were essentially inactive in the calmodulin assays and had no or marginal inhibitory effect on protein kinase C.
authors.affiliation: Department of Medicine State University of New York, Buffalo 14214.
authors.forename: E
authors.initials: E
authors.lastname: Middleton
authors.forename: P
authors.initials: P
authors.lastname: Ferriola
authors.forename: G
authors.initials: G
authors.lastname: Drzewiecki
authors.forename: R D
authors.initials: RD
authors.lastname: Sofia
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors; D000818:Animals; D001921:Brain / Q000201:enzymology; D002118:Calcium / Q000494:pharmacology; D002147:Calmodulin / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D005456:Fluorescent Dyes; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D007665:Ketotifen / Q000494:pharmacology; D010726:Phosphodiesterase Inhibitors; D010793:Phthalazines / Q000494:pharmacology*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D011724:Pyridazines / Q000494:pharmacology*; D051381:Rats; D012710:Serum Albumin, Bovine / Q000378:metabolism; D013050:Spectrometry, Fluorescence; D013449:Sulfonamides / Q000494:pharmacology
chemical_list: D002147:Calmodulin; D005456:Fluorescent Dyes; D006634:Histamine H1 Antagonists; D010726:Phosphodiesterase Inhibitors; D010793:Phthalazines; D011724:Pyridazines; D013449:Sulfonamides; D012710:Serum Albumin, Bovine; C017967:W 7; D011493:Protein Kinase C; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D002118:Calcium; D007665:Ketotifen; C020976:azelastine