Novelli F, Sparatore F
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Farmaco. 1996 Aug-Sep;51(8-9):551-8.
A set of 3-[2-(1-aryl-piperazin-4-yl)ethyl]-3,4-dihydro-3-methyl-1,2, 4-benzotriazines, bearing different substituents on the aromatic nuclei, was prepared and found to be endowed with good antihypertensive activity. The simplest compound 1, subjected to a broad pharmacological screening, exhibited also analgesic and antiallergic activities and hints of hypocholesterolemic action. Moreover this compound inhibited (in vitro tests) the guinea pig ileum contractions induced by several agents, the rat vas deferens contractions induced by phenylphrine (alpha 1 antagonism), the platelet aggregation induced by arachidonate and the tracheal tone.
制备了一组在芳环上带有不同取代基的3-[2-(1-芳基-哌嗪-4-基)乙基]-3,4-二氢-3-甲基-1,2,4-苯并三嗪,发现它们具有良好的抗高血压活性。最简单的化合物1经过广泛的药理筛选,还表现出镇痛和抗过敏活性以及降胆固醇作用的迹象。此外,该化合物(体外试验)抑制了几种药物诱导的豚鼠回肠收缩、去氧肾上腺素诱导的大鼠输精管收缩(α1拮抗作用)、花生四烯酸诱导的血小板聚集以及气管张力。