N-[1-(2-Benzo[b]thiophenyl)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 vivo (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 display 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.
FOTADAR, UPINDER, INDIAN J. CHEM., 1981, 20, N 11, 1006-1007
作者:FOTADAR, UPINDER
DOI:——
日期:——
US5248686A
申请人:——
公开号:US5248686A
公开(公告)日:1993-09-28
Fotadar, Upinder, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1981, vol. 20, # 11, p. 1006 - 1007