95017-63-3Relevant articles and documents
Dual probes for the dopamine transporter and σ1 receptors: Novel piperazinyl alkyl-bis(4′-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents
Cao, Jianjing,Kulkarni, Santosh S.,Husbands, Stephen M.,Bowen, Wayne D.,Williams, Wanda,Kopajtic, Theresa,Katz, Jonathan L.,George, Clifford,Newman, Amy Hauck
, p. 2589 - 2598 (2007/10/03)
Both dopamine uptake inhibitors and σ1 receptor antagonists have been implicated as potential pharmacotherapeutics for the treatment of cocaine abuse. While the dopamine uptake inhibitors may share with cocaine neurochemical mechanisms underlyi
1-piperidines and Related Compounds, Potential Antipsychotic Agents with Low Cataleptogenic Profiles
Wise, Lawrence D.,Pattison, Ian C.,Butler, Donald E.,DeWald, Horace A.,Lewis, Edward P.,et al.
, p. 606 - 612 (2007/10/02)
On the basis of a structural model of the postsynaptic dopaminergic antagonist pharmacophore, a series of 1-piperidines and related compounds was synthesized and evaluated for potential antipsychotic activity.For a rapid measure of activity, the target compounds were initially screened in vitro for inhibition of haloperidol binding and in vivo in a test of locomotor activity.Behavioral efficacy of compounds identified from the initial screens was more accurately measured in rats by using a suppression of high base-line medial forebrain bundle self-stimulation test model.The propensity of these compounds for causing extrapyramidal side effects was evaluated by using a rat catalepsy method.On the basis of these test models, we have shown that the methine carbon of the 1-(4,4-diarylbutyl)piperidines can be advantageously replaced with a nitrogen atom.The 1-piperidines were less cataleptic than the corresponding 1-(4,4-diarylbutyl)piperidines.The compounds with the widest separation between efficacious dose and cataleptic dose are 8-propyl>-1-phenyl-1,3,8-triazaspirodecan-4-one (6), 1-propyl>-4-piperidinyl>-1,3-dihydro-2H-benzimidazol-2-one (11), 1-propyl>-1,2,3,6-tetrahydro-4-pyridinyl>-1,3-dihydro-2H-benzimidazol-2-one (22), and 1-propyl>-4-(2-methoxyphenyl)piperazine (26).