Researchers at Merck & Co. Inc. have presented the discovery of novel selective metabotropic glutamate receptor 2 (mGluR2) negative allosteric modulators (NAMs) as potential PET imaging agents. Synthesis and optimization of a series of analogues of a potent and selective mGluR2 NAM resulted in the identification of compound MK-8056 as a high-affinity mGluR2 NAM (Ki=0.19 nM) with desirable lipophilicity (logD7.0=2.46) and low P-gp susceptibility.
Helmholtz Zentrum Dresden Rossendorf has patented 3-((3-([1,1’-biphenyl]-3-ylmethoxy)phenoxy)methyl)benzonitrile derivatives that are radiolabeled compounds targeting programmed cell death 1 ligand 1 (PD-L1; CD274). They are reported to be potentially useful for the diagnosis and/or radionuclide therapy treatment of cancer and SARS-CoV-2.
Monoacylglycerol lipase (MAGL) is a key regulator of the endocannabinoid system (ECS), which has a critical neuromodulatory involvement in numerous functional mechanisms in the CNS. Based on this, MAGL is considered a promising therapeutic target in neuroinflammation and neurodegeneration. Researchers from ETH Zürich and affiliated organizations have recently presented their work on (R)-[18F]YH-134, a novel reversible radiotracer for imaging MAGL in the brain.
Dopamine D3 receptors play a relevant role in the CNS modulating neurological activity, and its dysfunction is linked to disorders such as schizophrenia, drug abuse or Parkinson’s disease. There is a need for blood-brain barrier (BBB)-penetrant D3 receptor radiotracers with high brain uptake to be used for neurological and neuropsychiatric disease diagnosis.
Despite the success of CAR T-cell therapies for cancer immunotherapy, only a small percent of patients have a significant clinical response, and it is difficult to distinguish responders from nonresponders at an early stage with current imaging techniques.
Researchers from University North Carolina, Chapel Hill have discovered prostate-specific member antigen (PSMA)-targeted agents with reduced salivary gland uptake while maintaining high tumor uptake. Synthesis and subsequent screening of PSMA agents bearing different chelators and targeting ligands led to the identification of two lead agents, NOTA-UNC-PSMA-2 and DOTA-UNC-PSMA-2.