We describe the identification of a candidate positron emission tomography (PET) imaging agent for the NLRP3 protein. NLRP3 plays a critical role in the immune system and has proven a difficult target for the development of imaging agents due to its low and cell-specific expression profile. A recently described series of pyridazine-based inhibitors, with improved permeability and brain-penetration properties, was used as a starting point for the development of a suitable PET imaging agent.
View Article and Find Full Text PDFWe describe here our efforts to develop a PET tracer for imaging GluN2A-containing NMDA receptors, based on a 5H-thiazolo[3,2-α]pyrimidin-5-one scaffold. The metabolic stability and overall properties could be optimized satisfactorily, although binding affinities remained a limiting factor for in vivo imaging. We nevertheless identified 7-(((2-fluoroethyl)(3-fluorophenyl)amino)-methyl)-3-(2-(hydroxymethyl)cyclopropyl)-2-methyl-5H-thiazolo-[3,2-α]pyrimidin-5-one ([ F]7b) as a radioligand providing good-quality images in autoradiographic studies, as well as a tritiated derivative, 2-(7-(((2-fluoroethyl)(4-fluorophenyl)amino)methyl)-2-methyl-5-oxo-5H-thiazolo[3,2-α]pyrimidin-3-yl)cyclopropane-1-carbonitrile ([ H ]15b), which was used for the successful development of a radioligand binding assay.
View Article and Find Full Text PDFThe restoration of a youthful appearance to the midface can enhance its femininity. In this article, we discuss several strategies and techniques, both surgical and nonsurgical, for augmentation of the lateral and centro-lateral midface.
View Article and Find Full Text PDFAnn Plast Surg
September 2018
Background: Chest wall recontouring is a common surgical treatment of gender dysphoria in transmen and nonbinary individuals assigned female at birth. This study reviews more than 20 years of cases to identify risk factors for postoperative complications and likelihood of preservation of nipple sensation.
Methods: One hundred thirty-seven cases of female-to-male chest wall recontouring by a single surgeon from 1994 to 2016 were reviewed, 99 of which were included for final analysis.
[carboxyl-(14) C]Celivarone was synthesised from barium [(14) C]carbonate with overall radiochemical yields in the range 49-53%. The synthetic route involves [(14) C]carbonylation methodology, which both decreased the number of synthetic steps and increased the yields obtained from previous synthetic routes.
View Article and Find Full Text PDF5-Substituted and 5,5-disubstituted hydantoins are synthesised from the corresponding aldehydes or ketones, using a one-pot, gallium(III) triflate-catalysed procedure that is compatible with a range of substrates and solvents.
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