Effects of some rigid analogues of imipramine and amitriptyline on the uptake of noradrenaline, serotonin and choline in rat brain synaptosomes

Summary The inhibitory activities of four new rigid analogues of imipramine and amitriptyline on noradrenaline, serotonin and choline uptake were investigated in rat brain synaptosomes. The potency of the original drugs as inhibitors of noradrenaline and serotonin uptake was drastically reduced in all the four analogues. In contrast one of them, the lupinyliden-dibenzocy-cloheptadiene, strongly inhibited choline uptake at a concentration at which the original drugs were ineffective.