Inhibition, of PGE2-release

Table 11. Inhibition of PGE2-Release from Mouse Peritoneal Macrophages Stimulated with Calcium lonophore A23187 (10 M) by Budlejasaponin IV and Sandrosaponin I...

PGE can stimulate or inhibit its own hormone-induced synthesis via an ability to stimulate cAMP production. In the canine renal collecting tubule there appear to be two PGE receptors ". One of these receptors is an inhibitory receptor which modulates vasopressin-induced H2O flow . The other receptor is coupled to stimulation of adenylate cyclase activity. This latter receptor may be involved in inhibition of arachidonate release and feedback inhibition of hormone-induced PGE production. Similarly, neutrophil activation (and PGE2 synthesis) induced by f-met-leu-phe is under feedback inhibitory control by a PGE receptor apparently coupled to The opposite situation occurs in the thyroid. In the thyroid, there are two phases to PGE synthesis. The second phase is cAMP dependent and PGE serves to augment its own synthesis by its ability to stimulate adenylate cyclase activity ... 

Merck s L-651,896 (54) was the lead compound from a series of dihydro-benzofuranols [158]. L-651,896 inhibited cRBL (1 //M) as well as platelet 12-LO (5.9 /zM). In zymosan-stimulated mouse macrophages, both LTC4 and PGE2 release were inhibited (0.1 //M and 1.1 //M, respectively) similar potency was seen in rat and human ISN. Potent topical activity in AAE was seen, with LT production and oedema both inhibited at 20-30 nM/ear. LT levels were also reduced in mouse oxazolone contact sensitivity, but in this... 

---