PHA 4107 Lecture Notes - Lecture 15: Prostaglandin D2, Prostaglandin E1, Prostacyclin
12 Jul 2018
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Document Summary
Pgs activate gpcrs distributed in many cells/tissues to control inflammatory signals and physiological functions. Pgs are involved in the late phase of acute inflammation (cyclic involvement in chronic inflammation) Increase vasopermeability and aid in diapedesis of phagocytic cells: dilate precapillary arterioles while constricting postcapillary venules to increase blood supply, promote clotting to prevent bleeding. Nsaids classification: carboxylic acids, salicylic acid (asa), acetic acid (indomethacin, propionic acid (naproxen & ibuprofen, enolic acid, oxicams (piroxicam, meloxicam, para-aminopheno (acetaminophen) Salicylate first recognized medicinal properties of willow bark (salicin) ~1750: purified in 1829, also found in other plants including spirea, wintergreen. Dr. hoffman, a chemist employed by bayer was the first to synthesize acetylsalicylic acid (asa/aspirin) 1897. Discovery of the cox-2 enzyme provided an (cid:498)inflammatory target(cid:499) for pharmaceutical companies. Inhibition of cox enzymes by non-selective and selective nsaids: aspirin acetylates a serine in the active site blocking access to aeachidonic acid, nsaids block the opening of both cox-1 and cox-2 by interacting with arg.
