Pharmacodynamic study of a pyrophtalone: [methyl-2 (piperidino-2 ethyl-1)-1 dihydro 1-4 pyridylidene-4 yl]-2 indanedione 1-3. II. Mechanism of action.
The anti-inflammatory activity of the pyrophtalone derivative, [methyl-2 (piperidino-2 ethyl-1)-1 dihydro 1-4 pyridylidene-4 yl]-2 indanedione 1-3 or PpEtgammaL is not dependent upon adrenal gland stimulation. PpEtgammaL has an inhibitory effect neither on prostaglandin release after biosynthesis nor on prostaglandin synthetase. The reduced prostaglandin production, as result of drug action can be explained by impairment of substrate availability for this enzyme. There are several hypotheses, but according to the present results of our work, the most plausible one is an inhibition of unsaturated fatty acids release from cell membrane lipids.
D000273:Adipose Tissue / Q000187:drug effects / Q000378:metabolism; D000315:Adrenalectomy; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D003366:Cosyntropin / Q000494:pharmacology; D004487:Edema / Q000503:physiopathology; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007189:Indans / Q000494:pharmacology*; D007192:Indenes / Q000494:pharmacology*; D008168:Lung / Q000201:enzymology; D008247:Lysosomes / Q000187:drug effects; D008297:Male; D008566:Membranes / Q000187:drug effects; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011247:Pregnancy; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D011458:Prostaglandins E / Q000096:biosynthesis; D011817:Rabbits; D051381:Rats; D014590:Uterine Contraction / Q000187:drug effects; D014664:Vasodilation / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D007189:Indans; D007192:Indenes; D011458:Prostaglandins E; D003366:Cosyntropin; D011451:Prostaglandin-Endoperoxide Synthases