The author of 《PET imaging of microglia by targeting macrophage colony-stimulating factor 1 receptor (CSF1R)》 were Horti, Andrew G.; Naik, Ravi; Foss, Catherine A.; Minn, Il; Misheneva, Varia; Du, Yong; Wang, Yuchuan; Mathews, William B.; Wu, Yunkou; Hall, Andrew; La Course, Catherine; Ahn, Hye-Hyun; Nam, Hwanhee; Lesniak, Wojciech G.; Valentine, Heather; Pletnikova, Olga; Troncoso, Juan C.; Smith, Matthew D.; Calabresi, Peter A.; Savonenko, Alena V.; Dannals, Robert F.; Pletnikov, Mikhail V.; Pomper, Martin G.. And the article was published in Proceedings of the National Academy of Sciences of the United States of America in 2019. Category: piperazines The author mentioned the following in the article:
While neuroinflammation is an evolving concept and the cells involved and their functions are being defined, microglia are understood to be a key cellular mediator of brain injury and repair. The ability to measure microglial activity specifically and noninvasively would be a boon to the study of neuroinflammation, which is involved in a wide variety of neuropsychiatric disorders including traumatic brain injury, demyelinating disease, Alzheimer disease (AD), and Parkinson disease, among others. We have developed [11C]CPPC [5-cyano-N-(4-(4-[11C]methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide], a positron-emitting, high-affinity ligand that is specific for the macrophage colony-stimulating factor 1 receptor (CSF1R), the expression of which is essentially restricted to microglia within brain. [11C]CPPC demonstrates high and specific brain uptake in a murine and nonhuman primate lipopolysaccharide model of neuroinflammation. It also shows specific and elevated uptake in a murine model of AD, exptl. allergic encephalomyelitis murine model of demyelination and in postmortem brain tissue of patients with AD. Radiation dosimetry in mice indicated [11C]CPPC to be safe for future human studies. [11C]CPPC can be synthesized in sufficient radiochem. yield, purity, and specific radioactivity and possesses binding specificity in relevant models that indicate potential for human PET imaging of CSF1R and the microglial component of neuroinflammation. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Category: piperazines)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics