Pharmacological activity of FPP028 (2-phenylpyrazolo-4-ethyl-4,7-dihydro [1,5a]pyrimidin-7-one) a new non-steroid anti-inflammatory agent.
The activity of 2-phenylpyrazolo-4-ethyl-4,7-dihydro [1,5a]pyrimidin-7-one (FPP028), a non-acidic, analgesic, antipyretic, and anti-inflammatory compound, was investigated in a number of pharmacological tests performed in rats. The anti-inflammatory properties of FPP028 were evaluated through the carrageenan induced paw edema and the cotton pellet induced granuloma and compared with the activity of indomethacin, phenylbutazone, and isoxicam; as a result, the activity of FPP028 was shown to be similar to that of the latter compounds. To assess the analgesic properties of FPP028 in comparison with indomethacin and phenylbutazone, the Randall and Sellitto and the mouse-writhing tests were used; in both tests, FPP028 demonstrated a significant analgesic activity. FPP028 was shown to possess antipyretic properties in the test of yeast-induced pyrexia. The gastro-erosive activity of phenylbutazone and FPP028 was studied in restraint-stressed rats; in such test the ulcerogenic activity of phenylbutazone appeared to be dose-related; conversely, FPP028 demonstrated a gastro-protective effect since the number of gastric lesions induced either by stress or phenylbutazone treatment was decreased bu FPP028. Our data show that FPP028 is endowed with most of the pharmacological properties of the classic antiinflammatory drugs. Further studies are however needed to more fully elucidate its mechanism of action because our in-vivo data indicate that FPP028 is not an inhibitor of prostaglandin biosynthesis.
D000315:Adrenalectomy; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000633:toxicity; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001241:Aspirin / Q000494:pharmacology; D004487:Edema / Q000188:drug therapy; D005744:Gastric Acid / Q000378:metabolism; D006099:Granuloma / Q000188:drug therapy; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D051379:Mice; D010653:Phenylbutazone / Q000494:pharmacology; D010894:Piroxicam / Q000031:analogs & derivatives*; D011453:Prostaglandins / Q000096:biosynthesis; D011720:Pyrazoles / Q000494:pharmacology* / Q000633:toxicity; D011743:Pyrimidines / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000139:chemically induced; D013843:Thiazines / Q000494:pharmacology
D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011453:Prostaglandins; D011720:Pyrazoles; D011743:Pyrimidines; D013843:Thiazines; D010894:Piroxicam; C039837:4-ethyl-4,7-dihydro-2-phenylpyrazolo(1,5-a)pyrimidin-7-one; C013580:isoxicam; D010653:Phenylbutazone; D001241:Aspirin; D007213:Indomethacin