199738-99-3Relevant academic research and scientific papers
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D2/3 receptors in their high-affinity state
Van Wieringen, Jan-Peter,Shalgunov, Vladimir,Janssen, Henk M.,Fransen, P. Michel,Janssen, Anton G. M.,Michel, Martin C.,Booij, Jan,Elsinga, Philip H.
, p. 391 - 410 (2014/02/14)
Imaging of dopamine D2/3 receptors (D2/3R) can shed light on the nature of several neuropsychiatric disorders in which dysregulation of D2/3R signaling is involved. Agonist D2/3 tracers for PET/SPECT imaging are considered to be superior to antagonists because they are more sensitive to dopamine concentrations and may selectively label the high-affinity receptor state. Carbon-11-labeled D2/3R agonists have been developed, but these short-lived tracers can be used only in centers with a cyclotron. Here, we report the development of a series of novel D2R agonist compounds based on the 2-aminomethylchromane (AMC) scaffold that provides ample opportunities for the introduction of longer-lived [ 18F] or [123I]. Binding experiments showed that several AMC compounds have a high affinity and selectivity for D2/3R and act as agonists. Two fluorine-containing compounds were [18F]-labeled, and both displayed specific binding to striatal D2/3R in rat brain slices in vitro. These findings encourage further in vivo evaluations.
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans
Mewshaw, Richard E.,Kavanagh, Joseph,Stack, Gary,Marquis, Karen L.,Shi, Xiaojie,Kagan, Michael Z.,Webb, Michael B.,Katz, Alan H.,Park, Anna,Kang, Young H.,Abou-Gharbia, Magid,Scerni, Rosemary,Wasik, Theodore,Cortes-Burgos, Luz,Spangler, Taylor,Brennan, Julie A.,Piesla, Michael,Mazandargmi, Hossein,Cockett, Mark I.,Ochalski, Rafal,Coupet, Joseph,Andree, Terrance H.
, p. 4235 - 4256 (2007/10/03)
A series of 2-(aminomethyl)chromans (2-AMCs) was synthesized and evaluated for their affinity and selectivity for both the high- and low- affinity agonist states (D2(High) and D2(Low), respectively) of the dopamine (DA) D2
