At. Ilagouma et al., ARYLCYCLOHEXYLAMINES DERIVED FROM BTCP ARE POTENT INDIRECT CATECHOLAMINE AGONISTS, European journal of medicinal chemistry, 28(5), 1993, pp. 377-385
N-[1-(2-Benzo[b]thiophenyl)cyclohexyl]piperidine (BTCP)-related molecu
les were prepared by means of chemical modulation of the 3 rings which
constitute this dopamine (DA) and norepinephrine (NE) uptake inhibito
r. Tested in vitro (binding to the DA uptake complex and to the PCP re
ceptor sites, inhibition of the synaptosomal uptake of DA and NE) and
in vivo (locomotor activity in mice) these molecules showed good homog
eneity of action. The newly prepared structures, although formally rel
ated to the phencyclidine (PCP) structural model, no longer display si
gnificant affinity for the PCP receptor. These compounds behave like a
new series of indirect potent stimulants of the dopaminergic and nora
drenergic systems leading to potential antidepressive compounds.