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A Novel Radiotracer for Imaging Monoacylglycerol Lipase in the Brain Using Positron Emission Tomography.
TLDR
The synthesis and pilot rodent imaging of a novel MAGL imaging agent is described, demonstrating the high specificity, good selectivity, and appropriate kinetics and distribution of [(11)C]SAR127303, validating its utility for imaging MAGL in the brain.
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Discrepancies in Kappa Opioid Agonist Binding Revealed through PET Imaging.
TLDR
Changes in BPND were measured using kappa antagonists (naloxone, naltrexone, LY2795050, JDTic, nor-BNI), and it was found BPND was affected similarly between [11C]GR103545 and [ 11C]LY2459989, and kappa agonists salvinorin A and U-50488 caused dramatic reductions inBPND but did not change [11 C]LY 2459989 binding.
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Site-selective 18F fluorination of unactivated C–H bonds mediated by a manganese porphyrin
A direct aliphatic C–H 18F labeling method using [18F]fluoride ion at inaccessible and unreactive sites is reported.
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Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
TLDR
A series of simplified indenoisoquinoline analogues possessing a linker spacing of 0-12 carbon atoms between the lactam nitrogen and the terminal amino group have been prepared, determining that 2-4-atom lengths are optimal for topoisomerase I inhibition and cytotoxicity.
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Development of a Fluorinated Class-I HDAC Radiotracer Reveals Key Chemical Determinants of Brain Penetrance.
TLDR
The study revealed the major structural contributors to brain uptake, as well as a more clinically relevant fluorinated HDAC radiotracer with comparable behavior to Martinostat, yet longer half-life.
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Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
TLDR
Analysis of the biological results suggests that the nitro group is important for Top1 inhibition and the methoxy group improves cytotoxicity, which has provided optimal Top1 inhibitors equipotent to camptothecin that demonstrate low nanomolar cytotoxicities toward cancer cells.
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(11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.
TLDR
Carbonyl radiopharmaceuticals based on labeled carboxylic acids, amides, carbamates and ureas now account for a substantial number of important imaging agents that have seen translation to higher species and clinical research of previously inaccessible targets, which is a testament to the creativity, utility and practicality of the underlying radiochemistry.
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Virtually instantaneous, room-temperature [(11)C]-cyanation using biaryl phosphine Pd(0) complexes.
TLDR
With this procedure, a variety of [(11)C]nitrile-containing pharmaceuticals were prepared with high radiochemical efficiency and demonstrates superior reactivity compared to previously reported systems.
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Novel radioligands for imaging sigma-1 receptor in brain using positron emission tomography (PET)
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Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
TLDR
The results of the two series indicate the existence of superior functional groups such as methoxy, fluorine, and cyano for the indenoisoquinoline 9-position, Interestingly, these functional groups coincide with established structure-activity relationships for the 11-position of camptothecin.
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