Mulè A, Pirisino G, Moretti M D, Sparatore F, Dimich P M, Satta M, Peana A
Istituto di Tecnica Farmaceutica, Università di Sassari, Italia.
Farmaco. 1992 Sep;47(9):1161-72.
Two new cyclopentenylethylamines were prepared and were submitted to a pharmacological screening together with some others previously described and now reprepared. All compounds exhibited different degrees of depressive activity on CNS and good analgesic activity. Compound 5, bearing a phenyl group on the carbon atom to which the amino group is connected, appears rather interesting being the most active as analgesic and the least toxic. Compounds 2 and 3 are able to antagonize in a certain degree lethal doses of physostigmine and also, respectively, of pentylenetetrazole and strychnine.
制备了两种新的环戊烯基乙胺,并将它们与一些先前描述过且现在重新制备的其他化合物一起进行了药理筛选。所有化合物对中枢神经系统均表现出不同程度的抑制活性和良好的镇痛活性。在与氨基相连的碳原子上带有苯基的化合物5似乎相当有趣,它是镇痛活性最强且毒性最小的。化合物2和3能够在一定程度上拮抗毒扁豆碱的致死剂量,并且分别还能拮抗戊四氮和士的宁的致死剂量。