Extinction of mineralocorticoid effects in 19-norprogesterone derivatives: structure-activity relationships.

19-Norprogesterone (19-NOR-P) is a potent progestagen in mammals by s.c. injection, but is almost inactive when given p.

Pharmacological profile of the new pituitary-gonadic suppressant 17 beta-acetoxy-5 alpha, 17 alpha-pregn-2-ene-20-yne.

17 beta-Acetoxy-5 alpha, 17 alpha-pregn-2-ene-20-yne (TX 380) strongly suppresses the hypophyso-gonadic axis at central and peripheral levels. Depending on the dosage and on the hormonal status at the time of treatment, this combined inhibition results in major disturbances of the estrus cycle and in impaired ovulation. TX 380 shows minimal androgenic activity.

Prostacyclin bioassays using inhibition of platelet aggregation and relaxation of rabbit coeliac artery.

Bioassays of prostacyclin by inhibition of velocity and maximum of both irreversible and biphasic platelet aggregation, and by relaxation of the potassium-contracted isolated superfused rabbit coeliac artery have been undertaken. The use of each parameter is possible within a range of PGI2 concentrations, which have been determined for each of the five parameters studied. The optimal concentrations of PGI2 for a bioassay have also been determined, corresponding to each range.

Anti-thrombotic effect of very low doses of acetyl salicylic acid in rats.

The anti-thrombotic effect of acetyl salicylic acid (ASA) was studied using the following experimental model: a silk thread was inserted in an extracorporeal shunt between the right carotid artery and the opposite jugular vein. A thrombus developed around the thread which was weighed at 10 minutes intervals. ASA inhibits the development of the thrombus at a dose of 3.

[Changes of the course of experimental epileptic attacks by curarization].

In our studies on the Rabbit, the time of seizure in increase after curarization. The curare do not pass through the blood brain barrier ; the action of drug can not be a direct action on the central nervous system.