Harfenist M, Soroko F E, McKenzie G M
J Med Chem. 1978 Apr;21(4):405-9. doi: 10.1021/jm00202a021.
Unlike the related noncyclic amidines which are broad-spectrum cestocides, a number of 2-imidazolines substituted in the 2 position by alkoxyaryl groups were not highly active in screening tests against the mouse tapeworms Hymenolepsis nana and Oochoristica symmetrica. Certain of the 2-(4-alkoxynaphthyl)-2-imidazolines and 2-(6-alkoxy-2-naphthyl)-2-imidzolines, however, had activity interpreted as antidepressant in the mouse. This activity paralleled in vitro irreversible inhibitory activity against mouse brain MAO for those where no substitution is present on the imidazoline ring. This irreversibility probably has a different origin from that postulated to explain the irreversible MAO inhibition of proparglic, cyclopropyl, and other "chemically reactive" MAO inhibitors.
与具有广谱杀绦虫作用的相关非环状脒不同，许多在2位被烷氧基芳基取代的2-咪唑啉在针对小鼠绦虫微小膜壳绦虫和对称奥氏绦虫的筛选试验中活性不高。然而，某些2-(4-烷氧基萘基)-2-咪唑啉和2-(6-烷氧基-2-萘基)-2-咪唑啉在小鼠中具有被解释为抗抑郁的活性。对于咪唑啉环上无取代的那些化合物，这种活性与对小鼠脑MAO的体外不可逆抑制活性平行。这种不可逆性可能与假定用于解释炔丙基、环丙基和其他“化学反应性”MAO抑制剂对MAO的不可逆抑制的起源不同。
