Arylcyclohexylamines derived from BTCP are potent indirect catecholamine agonists

Article abstract of DOI:10.1016/0223-5234(93)90124-W

N-<1-(2-Benzothiophenyl)cyclohexyl>piperidine (BTCP)-related molecules were prepared by means of chemical modulation of the 3 rings which constitute this dopamine (DA) and norepinephrine (NE) uptake inhibitor.Tested in vitro (binding to the DA uptake complex and to the PCP receptor sites, inhibition of the synaptosomal uptake of DA and NE) and in vitro (locomotor activity in mice) these molecules showed good homogeneity of action.The newly prepared structures, although formally related to the phencyclidine (PCP) structural model, no longer displey significant affinity for the PCP receptor.These compounds behave like a new series of indirect potent stimulants of the dopaminergic and noradrenergic systems leading to potential antidepressive compounds.BTCP / PCP receptor sites / dopamine uptake inhibitors / norepinephrine uptake inhibitors / locomotor activity