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[Inhibition of 3', 5'-cyclic AMP phosphodiesterase in the guinea pig lung by a new anti-allergic: 10-(3-quinuclidinylmethyl) phenothiazine (LM 209)].
Arch Int Pharmacodyn Ther. 1976 Jan; 219(1):160-8.AI

Abstract

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.

Authors

No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

fre

PubMed ID

178283

Citation

Uzan, A, and G Le Fur. "[Inhibition of 3', 5'-cyclic AMP Phosphodiesterase in the Guinea Pig Lung By a New Anti-allergic: 10-(3-quinuclidinylmethyl) Phenothiazine (LM 209)]." Archives Internationales De Pharmacodynamie Et De Therapie, vol. 219, no. 1, 1976, pp. 160-8.
Uzan A, Le Fur G. [Inhibition of 3', 5'-cyclic AMP phosphodiesterase in the guinea pig lung by a new anti-allergic: 10-(3-quinuclidinylmethyl) phenothiazine (LM 209)]. Arch Int Pharmacodyn Ther. 1976;219(1):160-8.
Uzan, A., & Le Fur, G. (1976). [Inhibition of 3', 5'-cyclic AMP phosphodiesterase in the guinea pig lung by a new anti-allergic: 10-(3-quinuclidinylmethyl) phenothiazine (LM 209)]. Archives Internationales De Pharmacodynamie Et De Therapie, 219(1), 160-8.
Uzan A, Le Fur G. [Inhibition of 3', 5'-cyclic AMP Phosphodiesterase in the Guinea Pig Lung By a New Anti-allergic: 10-(3-quinuclidinylmethyl) Phenothiazine (LM 209)]. Arch Int Pharmacodyn Ther. 1976;219(1):160-8. PubMed PMID: 178283.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Inhibition of 3', 5'-cyclic AMP phosphodiesterase in the guinea pig lung by a new anti-allergic: 10-(3-quinuclidinylmethyl) phenothiazine (LM 209)]. AU - Uzan,A, AU - Le Fur,G, PY - 1976/1/1/pubmed PY - 1976/1/1/medline PY - 1976/1/1/entrez SP - 160 EP - 8 JF - Archives internationales de pharmacodynamie et de therapie JO - Arch Int Pharmacodyn Ther VL - 219 IS - 1 N2 - 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. SN - 0003-9780 UR - https://www.unboundmedicine.com/medline/citation/178283/[Inhibition_of_3'_5'_cyclic_AMP_phosphodiesterase_in_the_guinea_pig_lung_by_a_new_anti_allergic:_10__3_quinuclidinylmethyl__phenothiazine__LM_209_]_ DB - PRIME DP - Unbound Medicine ER -