Anti-histaminic, anti-inflammatory and bronchorelaxant activities of 2, 7-dimethyl-3-nitro-4H pyrido [1,2-a] pyrimidine-4-one

An immunopharmacological profile of 2, 7-dimethyl-3-nitro-4H pyrido [1,2-a] pyrimidine-4-one (P-I) has been investigated using in vitro and in vivo models representing various features of Type I allergy. P-I prevented compound 48/80-mediated histamine release from rat peritoneal mast cells. A promis...

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Bibliographic Details
Published in:International immunopharmacology 2008-07, Vol.8 (7), p.1049-1055
Main Authors: Youssouf, M.S., Kaiser, P., Singh, G.D., Singh, S., Bani, S., Gupta, V.K., Satti, N.K., Suri, K.A., Johri, R.K.
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents - pharmacology
Biological and medical sciences
Bronchodilation
Bronchodilator Agents - pharmacology
Cetirizine
Compound 48/80
Cytokines
Cytokines - biosynthesis
Edema - drug therapy
Eosinophil
Eosinophil peroxidase
Eosinophils - drug effects
Histamine
Histamine H1 Antagonists - pharmacology
Ketotifen
Male
Mast cells
Medical sciences
Mice
Mice, Inbred BALB C
Paw edema
Pharmacology. Drug treatments
Promethazine
Pyridines - pharmacology
Pyridopyrimidine
Pyrimidinones - pharmacology
Rats
Rats, Wistar
Trachea - drug effects
Trachea - physiology
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Summary:An immunopharmacological profile of 2, 7-dimethyl-3-nitro-4H pyrido [1,2-a] pyrimidine-4-one (P-I) has been investigated using in vitro and in vivo models representing various features of Type I allergy. P-I prevented compound 48/80-mediated histamine release from rat peritoneal mast cells. A promising anti-inflammatory activity of P-I was evident in active paw anaphylaxis (mice) and carragenan-induced paw edema (rat). P-I inhibited eosonophil accumulation and eosinophil peroxidase activity in bronchoalveolar lavage fluid from ovalbumin challenged balb/c mice: in these animals blood levels of IL-5, and CD4 + T cells also remained attenuated. A promising bronchorelaxant effect of P-I was observed in histamine-contracted guinea pig tracheal chain via its antagonism to H1 receptor. These findings were compared with some known compounds (ketotifen, cetirizine and promethazine). The anti-histaminic, anti-inflammatory and bronchorelaxant activities of P-I has been discussed in context with its potential profile as an anti-allergic and anti-asthmatic agent.
ISSN:1567-5769
1878-1705
DOI:10.1016/j.intimp.2008.03.015