363140-16-3Relevant academic research and scientific papers
Preparation of a technetium-99m SPECT agent for imaging the sigma-2 receptor status of solid tumors
Mach, Robert H.,Wheeler, Kenneth T.,Blair, Suwanna,Yang, Biao,Day, Cynthia S.,Blair, Joseph B.,Choi, Seok-Rye,Kung, Hank F.
, p. 899 - 908 (2001)
The synthesis and in vitro binding of a novel 99mTc-labeled radiotracer for imaging the sigma-2 (σ2) receptor status of breast tumors is described. Structural characterization and in vitro binding studies were conducted using the cor
Synthesis and sigma receptor binding affinities of 8-azabicyclo[3.2.1]octan-3α-yl and 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamates
Mach,Yang,Wu,Kuhner,Whirrett,West
, p. 339 - 355 (2007/10/03)
A series of N-(8-benzyl-8-azabicyclo[3.2.1]octan-3α-yl)carbamates and N-(9-benzyl-9-azabicyclo[3.3.1]nonan-3α-yl)carbamates was prepared and their affinities for sigma (σ1 and σ2) and serotonin 5-HT3 and 5-HT4 receptors was measured in vitro. The results of this structure-activity relationship study identified a novel compound, N-(9-benzyl-9-aza-bicyclo[3.3.1]nonan-3α-yl)N′- (2-methoxy-5-methylphenyl)carbamate (4i), having a high affinity and moderate selectivity for σ2 versus σ1 receptors and a low affinity for 5-HT3 and 5-HT4 receptors. The results of this structure-activity relationship study should provide valuable information for the preparation of σ2-selective ligands that can be used to further characterize the functional role of this receptor in vivo.
