
The action of a new antiallergic agent, 10-(3-quinuclidinylmethyl) phenothiazine or LM 209, on cAMP phosphodiesterase (PDE) was studied on a guinea-pig lung preparation and compared with that of other compounds such as cromoglycate (I), dexamethasone (II), dexchlorpheniramine (III), promethazine (IV) and theophylline (V). Compounds I, IV and V are competitive inhibitors whereas LM 209 and compound III are non competitive inhibitors of PDE. Compound II is practically inactive on the enzyme. Compounds III and V produce an inhibition of equal intensity, independently of the substrate concentration. Compounds I and IV are more active on PDE with low affinity than on PDE with strong affinity, whereas it is the contrary with LM 209. The mechanism of action of LM 209 at the pulmonary level is discussed in the light of these findings.
Chlorpheniramine, Quinuclidines, Phosphodiesterase Inhibitors, Guinea Pigs, In Vitro Techniques, Promethazine, Dexamethasone, Kinetics, Theophylline, 3',5'-Cyclic-AMP Phosphodiesterases, Phenothiazines, Cromolyn Sodium, Animals, Female, Lung
Chlorpheniramine, Quinuclidines, Phosphodiesterase Inhibitors, Guinea Pigs, In Vitro Techniques, Promethazine, Dexamethasone, Kinetics, Theophylline, 3',5'-Cyclic-AMP Phosphodiesterases, Phenothiazines, Cromolyn Sodium, Animals, Female, Lung
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