82625-25-0Relevant articles and documents
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3Receptor
Rosier, Niklas,Gr?tz, Lukas,Schihada, Hannes,M?ller, Jan,I?bilir, Ali,Humphrys, Laura J.,Nagl, Martin,Seibel, Ulla,Lohse, Martin J.,Pockes, Steffen
, p. 11695 - 11708 (2021/08/20)
The histamine H3 receptor (H3R) is considered an attractive drug target for various neurological diseases. We here report the synthesis of UR-NR266, a novel fluorescent H3R ligand. Broad pharmacological characterization revealed UR-NR266 as a sub-nanomolar compound at the H3R with an exceptional selectivity profile within the histamine receptor family. The presented neutral antagonist showed fast association to its target and complete dissociation in kinetic binding studies. Detailed characterization of standard H3R ligands in NanoBRET competition binding using UR-NR266 highlights its value as a versatile pharmacological tool to analyze future H3R ligands. The low nonspecific binding observed in all experiments could also be verified in TIRF and confocal microscopy. This fluorescent probe allows the highly specific analysis of native H3R in various assays ranging from optical high throughput technologies to biophysical analyses and single-molecule studies in its natural environment. An off-target screening at 14 receptors revealed UR-NR266 as a selective compound.
Design, synthesis, and evaluation of some novel biphenyl imidazole derivatives for the treatment of Alzheimer's disease
Ramrao, Salunke Prashant,Shrivastava, Sushant Kumar,Tripathi, Prabhash Nath,Verma, Akash,Waiker, Digambar Kumar
, (2021/08/06)
The multi-targeted organized strategy provides effectual and significant results to cure progressive neurodegenerative diseases like AD. Treatment for this awful disease is in infancy till now. A series of novel 4, 5-diphenyl-1H-imidazole linked piperazin
Controlled Reduction of Nitriles by Sodium Hydride and Zinc Chloride
Chiba, Shunsuke,Ong, Derek Yiren
, p. 1369 - 1378 (2020/04/27)
A new protocol for the controlled reduction of nitriles to aldehydes was developed using a combination of sodium hydride and zinc chloride. The iminyl zinc intermediates derived from aromatic nitriles could be further functionalized with allylmetal nucleophiles to afford homoallylamines. As the method allows the reduction of various aliphatic and aromatic nitriles with a concise procedure under milder reaction conditions and exhibits wide functional group compatibility, it is well suited for use in various opportunities in chemical synthesis.