Synthesis and pharmacological properties of some new 3-(2-N,N-dialkylaminoethyl)-pyrido [2,3-d]-pyrymidin-4-ones.

The following new derivatives of pyrido [2,3-d]-pyrimidin-4(3H)-one were synthesized: 3-(2-N,N-dimethylaminoethyl), 3-(2-N-pyrolidynylethyl), 3-(2-piperidinylethyl) and 3-(2-N-morpholidinylethyl). Their chemical structures were confirmed by MS, IR and 1H NMR spectroscopic data. Newly synthesized compounds were investigated pharmacologically for their central properties in mice and rats.

Synthesis and some central pharmacological properties of new 5(1H)oxo-2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic esters.

Six new 5(1H)oxo-2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic ethyl esters bearing an aromatic substituent in position 1 or 2 were obtained. Pharmacological studies on the central action of these derivatives were carried out on mice and rats. The highest activity showed compounds 1 and 2 which produced analgesic effects in mice.

Involvement of alpha 2-adrenoceptors in the activation of kininogenesis by clonidine.

The effects of clonidine and alpha 2-adrenoceptor blocking agents, yohimbine and tolazoline on kininogen and prekallikrein levels in plasma and on blood pressure were investigated in male Wistar rats. Clonidine (0.5 mg/kg) decreased concentration of kininogen.

Hypertensive drugs and plasma kinins in rats.

The influence of phenylephrine (PHE), methoxamine (MET) and ephedrine (EPH) on kininogen and prekallikrein level in plasma was investigated in male Wistar rats. Simultaneously the effect of these drugs on blood pressure was monitored. No changes in kininogenesis were observed during the hypertension period (2 h after ip injection).