Cascio G, Manghisi E, Erba R, Magistretti M J
Farmaco Sci. 1976 Jun;31(6):442-56. doi: 10.1002/chin.197639189.
A series of new butyrophenones was synthesized, the aim being to reduce neuroleptic activity and enhance the hypotensive effects of this class of drugs. The compounds were screened for toxicity according to the Irwin scheme and tested in anaesthetized cats for their effects on systemic arterial pressure. The most interesting compound, i.e. 1-(4'-fluorobenzoyl)-3-pyrrolidinyl-propane, was tested also in anaesthetized rabbits, cats, and dogs and in concious dogs. Moreover its central nervous system effects were tested in rats and mice. The compound proved practically devoid of neurological effects and showed interesting hypotensive activity.
合成了一系列新的丁酰苯类化合物，目的是降低这类药物的抗精神病活性并增强其降压作用。根据欧文方案对这些化合物进行了毒性筛选，并在麻醉猫身上测试了它们对体动脉压的影响。最有趣的化合物，即1-(4'-氟苯甲酰基)-3-吡咯烷基丙烷，还在麻醉的兔子、猫和狗以及清醒的狗身上进行了测试。此外，还在大鼠和小鼠身上测试了其对中枢神经系统的作用。该化合物几乎没有神经学作用，并显示出有趣的降压活性。
