25310-35-4Relevant academic research and scientific papers
Structure-Based Design of High-Affinity Fluorescent Probes for the Neuropeptide Y Y1Receptor
Müller, Christoph,Gleixner, Jakob,Tahk, Maris-Johanna,Kopanchuk, Sergei,Laasfeld, T?nis,Weinhart, Michael,Schollmeyer, Dieter,Betschart, Martin U.,Lüdeke, Steffen,Koch, Pierre,Rinken, Ago,Keller, Max
, p. 4832 - 4853 (2022/03/27)
The recent crystallization of the neuropeptide Y Y1 receptor (Y1R) in complex with the argininamide-type Y1R selective antagonist UR-MK299 (2) opened up a new approach toward structure-based design of nonpeptidic Y1R ligands. We designed novel fluorescent probes showing excellent Y1R selectivity and, in contrast to previously described fluorescent Y1R ligands, considerably higher (～100-fold) binding affinity. This was achieved through the attachment of different fluorescent dyes to the diphenylacetyl moiety in 2 via an amine-functionalized linker. The fluorescent ligands exhibited picomolar Y1R binding affinities (pKi values of 9.36-9.95) and proved to be Y1R antagonists, as validated in a Fura-2 calcium assay. The versatile applicability of the probes as tool compounds was demonstrated by flow cytometry- and fluorescence anisotropy-based Y1R binding studies (saturation and competition binding and association and dissociation kinetics) as well as by widefield and total internal reflection fluorescence (TIRF) microscopy of live tumor cells, revealing that fluorescence was mainly localized at the plasma membrane.
Scalable α-Arylation of Nitriles in Aqueous Micelles using Ultrasmall Pd Nanoparticles: Surprising Formation of Carbanions in Water
Ansari, Tharique N.,Bihani, Manisha,Bora, Pranjal P.,Finck, Lucie,Handa, Sachin,Jasinski, Jacek B.,Leahy, David K.,Pavuluri, Bhavana
, p. 6816 - 6821 (2020/07/16)
A scalable synthetic method is described for both the preparation of ultrasmall palladium nanoparticles and their subsequent use in catalyzing an α-arylation reaction of nitriles in aqueous micelles. This method involves the intermediacy of carbanions or keteniminates, which are presumably stabilized by the micellar environment rather than being quenched with water. These Pd nanoparticles are thoroughly characterized. Mechanistic studies using 31P NMR spectroscopy revealed the binding of phosphine ligand with the Pd surface and control experiment confirmed the zero-oxidation state of palladium. The scope of the transformation is demonstrated over 35 examples, including one at 50 g scale.
COMPOSITIONS AND METHODS FOR DETECTION OF METHADONE METABOLITE
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Page/Page column, (2013/08/15)
Methods and reagents are disclosed for conducting assays for EDDP. The reagents include a moiety selected from the group consisting of poly(amino acid) label moieties, non-poly(amino acid) label moieties, poly(amino acid) immunogenic carriers, non-poly(amino acid) immunogenic carriers, non-label poly(amino acid) moieties, and non-immunogenic carrier poly(amino acid) moieties linked to 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine at the 3-position of one of the phenyl rings. Antibodies produced from immunogenic EDDP conjugates and labeled EDDP conjugates are employed in assays for determining the presence and/or amount of EDDP in samples suspected of containing EDDP.
Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists
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Page/Page column 28, (2008/12/08)
The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The inv
