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 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.
Youssouf
M S
MS
Division of Pharmacology and Natural Products Chemistry, Indian Institute of Integrative Medicine (CSIR), Jammu-Tawi 180001, India.
Kaiser
P
P
Singh
G D
GD
Singh
S
S
Bani
S
S
Gupta
V K
VK
Satti
N K
NK
Suri
K A
KA
Johri
R K
RK
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001993:Bronchodilator Agents / Q000494:pharmacology*; D016207:Cytokines / Q000096:biosynthesis; D004487:Edema / Q000188:drug therapy; D004804:Eosinophils / Q000187:drug effects; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D011725:Pyridines / Q000494:pharmacology*; D011744:Pyrimidinones / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D014132:Trachea / Q000187:drug effects / Q000502:physiology
C530538:2,7-dimethyl-3-nitro-4H-pyrido(1,2-a)pyrimidine-4-one; D000893:Anti-Inflammatory Agents; D001993:Bronchodilator Agents; D016207:Cytokines; D006634:Histamine H1 Antagonists; D011725:Pyridines; D011744:Pyrimidinones