ARYLCYCLOHEXYLAMINES DERIVED FROM BTCP ARE POTENT INDIRECT CATECHOLAMINE AGONISTS

Citation
At. Ilagouma et al., ARYLCYCLOHEXYLAMINES DERIVED FROM BTCP ARE POTENT INDIRECT CATECHOLAMINE AGONISTS, European journal of medicinal chemistry, 28(5), 1993, pp. 377-385
Citations number
37
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
28
Issue
5
Year of publication
1993
Pages
377 - 385
Database
ISI
SICI code
0223-5234(1993)28:5<377:ADFBAP>2.0.ZU;2-#
Abstract
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.