Antiedema activity

By far the greatest number of reports have referred to the anti-inflammatory activity found for a variety of 1,2-benzothiazines.15 An initial report by Lombardino et al.9 indicated that potent anti-inflammatory activity was present in a series of 4-hydroxy-2H-l,2-benzothiazine-3-carboxanilide 1,1-dioxides. Antiedema activity in a rat model indicated that carboxanilide 132 (CP-14, 304) was twice as potent as the standard anti-inflammatory agent phenylbutazone. This observation on compound 132 was later confirmed and extended by others.17,85 Studies of the metabolism of compound 132 in animals indicated that a major metabolite resulted from hydroxylation of the carboxanilide moiety.86 The plasma half-life of compound 132 was found to be 21 hours in man.86... 

Much literature exists on the potent anti-inflammatory agent piroxicam (29). Lombardino, Wiseman, and co-workers have described the synthesis and potent antiedema activity of piroxicam in animals.19-21 The biotransformation products of piroxicam in animals108 and man109 have been reported. Piroxicam is an inhibitor of platelet aggregation110 and a potent inhibitor of prostaglandin biosynthesis in cultures of either MC5-5 cells or synovial cells.111 In man, piroxicam has a long half-life (45 h)112 and is effective in the treatment of rheumatoid arthritis,113,114 osteoarthritis,115 and other painful musculoskeletal conditions116-119 when administered as... 

Affinine (27) shows a little CNS depression and no analgesic, antipyretic, antiedema and diuretic activity (21). Affinisine (16) is a CNS depressant at 50 mg/kg po in the mouse and possesses a moderate analgesic activity and no... 

The TET-induced inhibitory influence on cyclic 3 ,5 -AMP phosphodiesterase (PDE) activities precedes edema formation in the rat brain [74]. lb clarify the mechanism of the protective action of EGb against TET-toxidty in rats, in vitro and ex vivo effects of EGb on PDE activities of cerebral tissue were investigated [75]. Higher concentrations of EGb (5-250 mg/L) inhibited the PDE activity in the brain in normal rats, whereas lower concentrations (0.25-4.0 mg/L) of EGb enhanced the activity of the enzyme. The inhbitory effect of TET on the high affinity PDE activity (measured with 0.25 ftM cyclic AMP) of the brain was diminished in the presence of low EGb concentrations. Furthermore, preventive and curative treatment of 1 El-poisoned rats with EGb (100 mg/kg, p.o., for 7 days) prevented both the formation of edema and the fall of PDE activity induced by TET alone. These results suggested the antiedema action of EGb might be partly associated with its modulating influences on cellular cyclic AMP levels via activation of membrane-bound PDE. 

Furthermore, pretreatment with the flavonic extract of Oxyris quadripartita significantly diminished the increase in the mucosal permeability induced by bradykinin in rats, evidencing a marked antiedema and vasoprotective action of this compound. These results confirmed that Oxyris quadripartita exerted protective mucosal activity through vascular mechanisms [224],... 

Antiedema, anti-inflammatory, diuretic, gonadotropic activity, estrogenic activity, and antihypertensive activity were also reported in vivo The antihypertensive activity may be explained in view of a recent report by Kwan et al. in which Siberian ginseng aqueous extract resulted in a concentration-dependent relaxation in different contracted vascular preparations (dog carotid arterial rings, rat aorta, and rat artery) at 0.04—2.0 mg/mL. The observed relaxation was attributed to NO and/ or EDHF, in addition to other possible mechanisms. ... 

---