Abstract
1. 1. The influence of the two antischistosomal drugs (±) praziquantel and (±) oxamniquine on PGI 2 synthesis by the male rat thoracic aorta and day-20 pregnant rat myometrium in vitro was investigated using a rat platelet antiaggregatory bioassay method. 2. 2. Pretreatment of the tissues with praziquantel (64–512 μM) or oxamniquine (36–288 μM) for 30 min at 37°C significantly inhibited basal PGI 2 synthesis in a concentration-dependent manner ( P <0.005, n = 5–6). 3. 3. Both drugs failed to inhibit PGI 2 synthesis in presence of exogenous arachidonic acid (AA) (16.6 μM). 4. 4. Furthermore, they did not antagonize AA (4 nmol kg −1)-induced hypotension in urethane-anaesthetized rats. Thus, the drugs seemed to act via inhibition of phospholipase A 2 enzyme (PLA 2). 5. 5. The highly lipophilic drugs may interact with membrane phospholipids resulting in prevention of interaction between the substrates and the enzyme's active site.
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