In vitro vasorelaxing activity of suloctidil.

The vasorelaxing effect of suloctidil was evaluated in isolated rat and rabbit aorta and in isolated rabbit mesenteric and saphenous artery. Suloctidil inhibited contractions induced by increasing extracellular calcium in depolarized arteries, mainly in a competitive way. In the rat aorta, the pA2 value was 7.

Antihypertensive activity of tibalosine (CP 804 S) in the rat. Possible involvement of a central alpha 1-adrenergic receptor blockade.

The effect of tibalosine (CP 804 S) on systolic blood pressure and heart rate of unanaesthetized normotensive, spontaneously hypertensive (SHR) and DOCA-salt and Goldblatt hypertensive rats has been examined. After a single oral dose, tibalosine (1.9 to 15 mg/kg) elicited dose-dependent reductions in blood pressure in the four models tested.

Anticonvulsant activity of milacemide.

The anticonvulsant activity of a new drug, milacemide (2-(pentylamino)-acetamide), has been studied in animal models of convulsions like those induced by bicuculline, pentylenetetrazol, picrotoxin, strychnine, inhibitors of GABA synthesis as 3-mercaptopropionic acid, allylglycine, isoniazid and thiosemicarbazide and electroshock. Milacemide is particularly effective in inhibiting the convulsions induced by bicuculline. The ED50 is 5.