N-Arylalkylpiperidines as High-Affinity Sigma-1 and Sigma-2 Receptor Ligands: Phenylpropylamines as Potential Leads for Selective Sigma-2 Agents
摘要:
To delineate the differences between the structural requirements necessary for recognition at sigma-1 and sigma-2 receptors, a range of phenethyl- and phenylpropylpiperidines were evaluated in binding assays. Phenethylpiperidines were found to favor sigma-1 receptors, whereas phenylpropylpiperidines tend to favor sigma-2 receptors. It appears that phenylpropylamine is a potential pharmacophore for selective sigma-2 ligands. (C) 2002 Elsevier Science Ltd. All rights reserved.
A General Acid‐Mediated Hydroaminomethylation of Unactivated Alkenes and Alkynes
作者:Daniel Kaiser、Veronica Tona、Carlos R. Gonçalves、Saad Shaaban、Alberto Oppedisano、Nuno Maulide
DOI:10.1002/anie.201906910
日期:2019.10.7
its considerable potential to streamline amine synthesis. State-of-the-art protocols for hydroaminomethylation of alkenes rely largely on transition-metal catalysis, enabling this transformation only under highly designed and controlled conditions. Here we report a broadly applicable, acid-mediated approach to the hydroaminomethylation of unactivated alkenes and alkynes. This methodology employs cheap
[EN] HETEROCYCLIC ANALGESIC COMPOUNDS AND METHOD OF USE THEREOF<br/>[FR] COMPOSES ANALGESIQUES HETEROCYCLIQUES ET TECHNIQUE D'UTILISATION DE CEUX-CI
申请人:SEPRACOR INC
公开号:WO2001092226A1
公开(公告)日:2001-12-06
One aspect of the present invention relates to novel heterocyclic compounds, such as Formula (1). A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the invention relates to the use of the novel heterocyclic compounds as analgesics.