Pegoli, Andrea published the artcileRadiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor, Application In Synthesis of 140-28-3, the publication is Journal of Medicinal Chemistry (2017), 60(8), 3314-3334, database is CAplus and MEDLINE.
The dualsteric ligand approach, aiming at ligands with improved subtype selectivity, has been increasingly applied to muscarinic receptors (MRs). In this article we present the synthesis and characterization of a M2R subtype-preferring radiolabeled dibenzodiazepinone-type antagonist [3H]UNSW-MK259, (I) and its homodimeric analog [3H]UR-AP060, (II). Saturation binding studies at the M2R, using the orthosteric antagonist atropine to determine unspecific binding, proved that the monomeric and the dimeric compound bind to the orthosteric binding site (apparent Kd: 0.87 and 0.24 nM, resp.). Various binding studies with I and II at the M2R, for instance, saturation binding experiments in the presence of the allosteric MR modulators W84 or LY2119620 (Schild-like anal.) suggested a competitive mechanism between the allosteric modulator and the dibenzodiazepinone derivatives, and thus a dualsteric binding mode of both I and II. This was consistent with the results of M2R MD simulations (¡Ý2 ¦Ìs) performed with I and II.
Journal of Medicinal Chemistry published new progress about 140-28-3. 140-28-3 belongs to catalysis-chemistry, auxiliary class Benzenes, name is N1,N2-Dibenzylethane-1,2-diamine, and the molecular formula is C16H20N2, Application In Synthesis of 140-28-3.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia