Antidepressant agents. 9. 3,3-Diphenylcyclobutylamines, a new class of central stimulants

Abstract

3,3-Diphenylcyclobutylamine (4), N-methyl-3,3-diphenylcyclobutylamine (6) and N,N-dimethyl-3,3-diphenylcyclobutylamine (7) were prepared and tested as potential antidepressant agents. The secondary (6) and tertiary (7) amines strongly decrease the accumulation of NA [norepinephrine] and 5-HT [serotonin] in rat brain slices in vitro and in vivo. The cyclobutylamines also cause motor stimulation. The most potent compound in this respect is the tertiary amine 7. The increase in locomotion is not blocked by pretreatment with phenoxybenzamine, methergoline or .alpha.-methyltyrosine. Pre-treatment with pimozide or reserpine reduces the hyperactivity induced by 7. This hyperstimulation seems to be caused by a mechanism of action which differs from that of amphetamine. The tertiary 7 amine may cause increase in locomotion by release of dopamine from granular stores.