6-hydroxyindole and ifenprodil

6-hydroxyindole has been researched along with ifenprodil* in 1 studies

Other Studies

1 other study(ies) available for 6-hydroxyindole and ifenprodil

Article	Year
Synthesis, modelling and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-d-aspartate receptors. Bioorganic & medicinal chemistry, 2014, Feb-01, Volume: 22, Issue:3 A three-step synthetic pathway has been employed to synthesize a small library of 2-(4-arylpiperidin-1-yl)-1-(1H-indol-3-yl)ethanone and 2-(4-arylpiperidin-1-yl)-1-(1H-indol-3-yl)ethane-1,2-dione derivatives that have been screened in [(3)H]ifenprodil competition binding assay. Some compounds exhibited significant binding affinity at nanomolar concentration, the most active being ligand 35 (IC50=5.5nM). Docking experiments suggested the main interactions between 35 and GluN2B-containing NMDA receptors. Notably, the compound 35 reduced NMDA-mediated excitatory post-synaptic currents recorded in mouse hippocampal slices indicating antagonistic effects (50nM). Moreover, the compound 35 has shown antioxidant effects in a preliminary screening, thus suggesting that it might be considered prototype for future drug development of novel 'dual target' neuroprotective agents. Topics: Animals; Anticonvulsants; Antioxidants; Binding, Competitive; Chemistry Techniques, Synthetic; Hippocampus; In Vitro Techniques; Indoles; Ligands; Mice; Mice, Inbred DBA; Mice, Inbred Strains; Molecular Docking Simulation; Molecular Structure; Piperidines; Receptors, N-Methyl-D-Aspartate; Small Molecule Libraries	2014

Article

Year

Synthesis, modelling and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-d-aspartate receptors.

Bioorganic & medicinal chemistry, 2014, Feb-01, Volume: 22, Issue:3

A three-step synthetic pathway has been employed to synthesize a small library of 2-(4-arylpiperidin-1-yl)-1-(1H-indol-3-yl)ethanone and 2-(4-arylpiperidin-1-yl)-1-(1H-indol-3-yl)ethane-1,2-dione derivatives that have been screened in [(3)H]ifenprodil competition binding assay. Some compounds exhibited significant binding affinity at nanomolar concentration, the most active being ligand 35 (IC50=5.5nM). Docking experiments suggested the main interactions between 35 and GluN2B-containing NMDA receptors. Notably, the compound 35 reduced NMDA-mediated excitatory post-synaptic currents recorded in mouse hippocampal slices indicating antagonistic effects (50nM). Moreover, the compound 35 has shown antioxidant effects in a preliminary screening, thus suggesting that it might be considered prototype for future drug development of novel 'dual target' neuroprotective agents.

Topics: Animals; Anticonvulsants; Antioxidants; Binding, Competitive; Chemistry Techniques, Synthetic; Hippocampus; In Vitro Techniques; Indoles; Ligands; Mice; Mice, Inbred DBA; Mice, Inbred Strains; Molecular Docking Simulation; Molecular Structure; Piperidines; Receptors, N-Methyl-D-Aspartate; Small Molecule Libraries

2014