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PMID: 2571246 Published · ppublish English Comparative Study Journal Article

The effect of azelastine and some other antiasthmatic and antiallergic drugs on calmodulin and protein kinase C.

Agents and actions ·Vol. 28 ·No. 1-2 ·1989-08-00 ·Pages 9-15

Middleton E, Ferriola P, Drzewiecki G, Sofia RD

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.

MeSH Terms
3',5'-Cyclic-AMP Phosphodiesterases/antagonists & inhibitors Animals Brain/enzymology Calcium/pharmacology Calmodulin/antagonists & inhibitors,pharmacology Fluorescent Dyes Histamine H1 Antagonists/pharmacology Ketotifen/pharmacology Phosphodiesterase Inhibitors Phthalazines/pharmacology Protein Kinase C/antagonists & inhibitors Pyridazines/pharmacology Rats Serum Albumin, Bovine/metabolism Spectrometry, Fluorescence Sulfonamides/pharmacology
Chemicals
Calmodulin Fluorescent Dyes Histamine H1 Antagonists Phosphodiesterase Inhibitors Phthalazines Pyridazines Sulfonamides Serum Albumin, Bovine W 7 Protein Kinase C 3',5'-Cyclic-AMP Phosphodiesterases Calcium Ketotifen azelastine
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Middleton E
Department of Medicine State University of New York, Buffalo 14214.
Ferriola P
Drzewiecki G
Sofia R D
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23 references, click to expand
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Article Info
Journal
Agents and actions
Abbr.
Agents Actions
ISSN
0065-4299
DOI
10.1007/BF02022974
Published
1989-08-00
Pages
9-15
Language
English
Region
Switzerland
NLM ID
0213341
Subset
IM
External Links
PubMed source DOI: 10.1007/BF02022974
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