One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 2403-88-5, Name is 2,2,6,6-Tetramethyl-4-piperidinol, formurla is C9H19NO. In a document, author is Ogawa, Kazuma, introducing its new discovery. Safety of 2,2,6,6-Tetramethyl-4-piperidinol.
Development of a novel radiobromine-labeled sigma-1 receptor imaging probe
Introduction: Sigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 receptor, and synthesized radiobrominated (+)-pBrV. This radiobrominated (+)-pBrV showed high tumor uptake in tumor-bearing mice; however, radioactivity accumulation in normal tissues, such as the liver, was high. We assumed that the accumulation of (+)-pBrV in the non-target tissues was partially derived from its high lipophilicity; therefore, we synthesized and evaluated (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-bromophenol [(+)-BrV-OH], which is a more hydrophilic compound. Although we aimed to develop a PET tracer using( 76)Br, in these initial studies, we used(77)Br because of its longer half-life. Methods: (+)-[Br-77]BrV-OH was synthesized using the chloramine-T method with a radiochemical purity of 95%. Lipophilicity and affinity for sigma-1 receptor of (+)-[Br-77]BrV-OH were determined, and biodistribution experiments were performed. We also performed an in vivo blocking study by co-injecting excess amounts of the sigma-1 receptor ligand, SA4503, into mice. Results: The lipophilicity and affinity for sigma-1 receptor of (+)-[Br-77]BrV-OH were lower than those of (+)-[Br-77]pBrV. (+)-[Br-77]BrV-OH also showed high tumor uptake in biodistribution experiments in DU-145 tumor-bearing mice,. Although (+)-[Br-77]pBrV was retained in most tissues, (+)-[Br-77]BrV-OH was cleared from these tissues. In blocking studies, the co-injection of SA4503 significantly decreased the tumor uptake of (+)-[Br-77]BrV-OH. Conclusion: These results indicate that (+)-[Br-76]BrV-OH has potential as a PET probe for sigma-1 receptor imaging. (C) 2018 Elsevier Inc. All rights reserved.
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Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem