Structure− brain exposure relationships

SA Hitchcock, LD Pennington - Journal of medicinal chemistry, 2006 - ACS Publications
Healthy functioning of the human brain relies on effective shielding of the sensitive neural
microenvironment from potentially disruptive xenobiotic agents circulating in the periphery …

5-hydroxytryptamine (5-HT) receptor ligands

SL Kitson - Current pharmaceutical design, 2007 - ingentaconnect.com
Serotonin (5-HT) receptors are part of the G protein-coupled and ligand-gated ion channel
families. 5-HT exerts its diverse actions by binding to cell surface receptors which can be …

Facile One-Pot Direct Arylation and Alkylation of Nitropyridine N-Oxides with Grignard Reagents

F Zhang, XF Duan - Organic letters, 2011 - ACS Publications
Facile arylation and alkylation of nitropyridine N-oxides were developed through the
reactions of Grignard reagents with nitropyridine N-oxides. For the same 4-nitropyridine N …

New trends and current status of positron-emission tomography and single-photon-emission computerized tomography radioligands for neuronal serotonin receptors …

PP Hazari, A Pandey, S Chaturvedi… - Bioconjugate …, 2017 - ACS Publications
The critical role of serotonin (5-hydroxytryptamine; 5-HT) and its receptors (5-HTRs) in the
pathophysiology of diverse neuropsychiatric and neurodegenerative disorders render them …

A simple metal-free synthesis of 2-substituted pyridine-4, 5-dicarboxylates and their N-oxides

J Bezenšek, B Prek, U Grošelj, M Kasunič, J Svete… - Tetrahedron, 2012 - Elsevier
Herein a simple, metal-free synthesis of 2-alkyl-, 2-cycloalkyl-, 2-aryl-, and 2-heteroaryl-
substituted pyridine 3, 4-dicarboxylates and their N-oxides from the corresponding methyl …

Molecular structure and spectroscopic properties of new neodymium complex with 3-bromo-2-chloro-6-picolinic N-oxide showing the ligand-to-metal energy transfer

L Macalik, M Wandas, W Sąsiadek, J Lorenc… - Journal of Molecular …, 2021 - Elsevier
A new neodymium [Nd (BCPN) 3 (NO 3) 3 (H 2 O) 2] complex with 3-bromo-2-chloro-6-
picolinic N-oxide was synthesized and characterized by means of spectroscopic studies and …

Effective MicroPET imaging of brain 5‐HT1A receptors in rats with [18F]MeFWAY by suppression of radioligand defluorination

JY Choi, CH Kim, TJ Jeon, BS Kim, CH Yi, KS Woo… - Synapse, 2012 - Wiley Online Library
Abstract Introduction:[18F] MeFWAY has been developed for imaging the serotonin 1A
receptors in the brain. The purpose of this study were to verify the metabolic stability of [18F] …

Substitution of the Nitro Group with Grignard Reagents: Facile Arylation and Alkenylation of Pyridine N-Oxides

F Zhang, S Zhang, XF Duan - Organic letters, 2012 - ACS Publications
The unprecedented substitution of a nitro group with aryl or alkenyl groups of Grignard
reagents affords 2-aryl or alkenylpyridine N-oxides in modest to high yields with high …

Structural and vibrational study of 3-or 5-methyl substituted 2-N-ethylamino-4-nitropyridine N-oxides

J Lorenc, J Hanuza, J Janczak - Vibrational Spectroscopy, 2012 - Elsevier
X-ray crystal structures of two isomers C8H11N3O3, ie 2-N-ethylamino-5-methyl-4-
nitropyridine N-oxide (EN5MPO) and 2-N-ethylamino-3-methyl-4-nitropyridine N-oxide …

Optimization of the radiosynthesis of [18F]MEFWAY for imaging brain serotonin 1A receptors by using the GE TracerLab FXFN‐Pro module

JY Choi, CH Kim, YH Ryu, YB Seo… - Journal of Labelled …, 2013 - Wiley Online Library
The aim of this study was to develop a highly reliable radiofluorination method for the
preparation of N‐{2‐[4‐(2‐methoxyphenyl) piperazinyl] ethyl}‐N‐(2‐pyridyl)‐N‐(4‐18F …