Development and Optimization of 11C-Labeled Radiotracers: A Review of the Modern Quality Control Design Process DOI
Paul Josef Myburgh, Kiran Kumar Solingapuram Sai

ACS Pharmacology & Translational Science, Journal Year: 2023, Volume and Issue: 6(11), P. 1616 - 1631

Published: Oct. 11, 2023

Introduction - Several 11C-tracers have demonstrated high potential in early diagnostic PET imaging applications of neurodegenerative diseases including Alzheimer's and Parkinson's disease. These radiotracers often track critical biomarkers disease pathogenesis such as tau fibrils ([11C]PBB3) or β-amyloid plaques ([11C]PiB) associated with diseases. Purpose The short review aims to serve a guideline the future development for students, postdocs and/or new radiochemists who will be synthesizing clinical grade novel research 11C-tracers, knowledge regulatory requirements. We aim bridge gap between established 11C-tracer quality control (QC) processes through exploring design process requirements 11C-pharmaceuticals. Methods A literature survey was undertaken identify articles detailed description QC methodology characterization each sections review. Overview First general summary production presented; this used establish possible places contamination assurances sterile final product. key mandated analyses use were then discussed. Further, we assessed methods reviewed routine tests preclinical translational validation studies. Therefore, both animal studies reviewed. Last, some examples optimization automation reviewed, implications practices procedures considered. Conclusion All common parameters under settings (along few exceptions) discussed detail. While it is important standard, peer-reviewed testing protocols entering umbrella, equal importance needed on address credibility repeatability study.

Language: Английский

In vitro characterization of [125I]HY-3-24, a selective ligand for the dopamine D3 receptor DOI Creative Commons
Ji Youn Lee, Ho Young Kim, Paul Martorano

et al.

Frontiers in Neuroscience, Journal Year: 2024, Volume and Issue: 18

Published: April 9, 2024

Introduction Dopamine D3 receptor (D3R) ligands have been studied for the possible treatment of neurological and neuropsychiatric disorders. However, selective D3R radioligands in vitro binding studies challenging to identify due high structural similarity between D2R D3R. In a prior study, we reported new conformationally-flexible benzamide scaffold having affinity excellent selectivity vs. D2R. current characterized properties radioiodinated ligand, [ 125 I]HY-3-24. Methods were conducted cell lines expressing receptors, rat striatal homogenates, non-human primate (NHP) brain tissues measure regional distribution this radioligand. Results HY-3-24 showed potency at ( K i = 0.67 ± 0.11 nM, IC 50 1.5 0.58 nM) compared other D2-like dopamine subtypes (D2R 86.7 11.9 nM D4R > 1,000). The d (0.34 0.22 B max (38.91 2.39 fmol/mg) values I]HY-3-24 determined. homogenates using antagonists confirmed Autoradiography results demonstrated that specifically binds D3Rs nucleus accumbens, islands Calleja, caudate putamen NHP sections. Conclusion These suggest appears be novel radioligand exhibits D3R, with low receptors. It is anticipated can used as specific

Language: Английский

Citations

0
Characterization of tritiated JNJ‐GluN2B‐5 (3‐[3H] 1‐(azetidin‐1‐yl)‐2‐(6‐(4‐fluoro‐3‐methyl‐phenyl)pyrrolo[3,2‐b]pyridin‐1‐yl)ethanone), a high affinity GluN2B radioligand with selectivity over sigma receptors DOI

Jeffrey Schoellerman,

Brian Lord,

Anindya Bhattacharya

et al.

Journal of Neurochemistry, Journal Year: 2024, Volume and Issue: unknown

Published: May 21, 2024

Here, we describe the characterization of a radioligand selective for GluN2B-containing NMDA receptors, 3-[

Language: Английский

Citations

0
Identification of novel tau positron emission tomography tracers for chronic traumatic encephalopathy by comprehensive in silico screening and molecular dynamics simulation DOI
Bote Qi,

Lulu Guan,

Jingwang Tan

et al.

Physical Chemistry Chemical Physics, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 10, 2024

This study identifies novel tau PET tracers for CTE via comprehensive in silico screening and molecular dynamics simulation.

Language: Английский

Citations

0
Development and Optimization of 11C-Labeled Radiotracers: A Review of the Modern Quality Control Design Process DOI
Paul Josef Myburgh, Kiran Kumar Solingapuram Sai

ACS Pharmacology & Translational Science, Journal Year: 2023, Volume and Issue: 6(11), P. 1616 - 1631

Published: Oct. 11, 2023

Introduction - Several 11C-tracers have demonstrated high potential in early diagnostic PET imaging applications of neurodegenerative diseases including Alzheimer's and Parkinson's disease. These radiotracers often track critical biomarkers disease pathogenesis such as tau fibrils ([11C]PBB3) or β-amyloid plaques ([11C]PiB) associated with diseases. Purpose The short review aims to serve a guideline the future development for students, postdocs and/or new radiochemists who will be synthesizing clinical grade novel research 11C-tracers, knowledge regulatory requirements. We aim bridge gap between established 11C-tracer quality control (QC) processes through exploring design process requirements 11C-pharmaceuticals. Methods A literature survey was undertaken identify articles detailed description QC methodology characterization each sections review. Overview First general summary production presented; this used establish possible places contamination assurances sterile final product. key mandated analyses use were then discussed. Further, we assessed methods reviewed routine tests preclinical translational validation studies. Therefore, both animal studies reviewed. Last, some examples optimization automation reviewed, implications practices procedures considered. Conclusion All common parameters under settings (along few exceptions) discussed detail. While it is important standard, peer-reviewed testing protocols entering umbrella, equal importance needed on address credibility repeatability study.

Language: Английский

Citations

1