Kinetic isotope effects and synthetic strategies for deuterated carbon-11 and fluorine-18 labelled PET radiopharmaceuticals
MA Klenner, G Pascali, BH Fraser… - Nuclear Medicine and …, 2021 - Elsevier
The deuterium labelling of pharmaceuticals is a useful strategy for altering pharmacokinetic
properties, particularly for improving metabolic resistance. The pharmacological effects of …
properties, particularly for improving metabolic resistance. The pharmacological effects of …
A rapid MS/MS method to assess the deuterium kinetic isotope effect and associated improvement in the metabolic stability of deuterated biological and …
The deuterium kinetic isotope effect has been known for a period of 40 years, but it is only
relatively recently that new drug entities (NDEs) incorporating deuterium demonstrating …
relatively recently that new drug entities (NDEs) incorporating deuterium demonstrating …
PET radiopharmaceuticals: state-of-the-art and future prospects
TJ Tewson, KA Krohn - Seminars in nuclear medicine, 1998 - Elsevier
In this review we provide a conceptual overview of radiopharmaceuticals containing positron-
emitting isotopes, not a catalog of radiopharmaceuticals or details of syntheses. We hope to …
emitting isotopes, not a catalog of radiopharmaceuticals or details of syntheses. We hope to …
Probing the biochemical basis of the PET image. Mechanistic PET studies of (sup 11 C) L-deprenyl binding using the deuterium isotope effect
JS Fowler, AP Wolf, RR MacGregor, SL Dewey… - Journal of Labelled …, 1989 - osti.gov
Subject: 63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON
LIVING ORGS. AND BIOL. MAT.; ENZYME INHIBITORS; CARBON 11; DOUBLE …
LIVING ORGS. AND BIOL. MAT.; ENZYME INHIBITORS; CARBON 11; DOUBLE …
Fluorine-for-hydrogen: a strategy for radiolabeling, not a replacement
MR Kilbourn - Nuclear medicine and biology, 2013 - Elsevier
As the development of new radiopharmaceuticals for in vivo imaging in Nuclear Medicine
has moved towards the targeting of high affinity/low density sites on proteins, chemists have …
has moved towards the targeting of high affinity/low density sites on proteins, chemists have …
The status of PET radiochemistry for drug development and evaluation
VW Pike - Drug information journal: DIJ/Drug Information …, 1997 - Springer
Positron emission tomography (PET), when coupled to appropriate organic radiotracers, is a
powerful quantitative imaging technique for probing biochemical pathways, molecular …
powerful quantitative imaging technique for probing biochemical pathways, molecular …
Chemistry considerations for the clinical translation of oncology PET radiopharmaceuticals
L Allott, EO Aboagye - Molecular Pharmaceutics, 2020 - ACS Publications
Positron emission tomography (PET) has proven to be an invaluable tool in the staging and
management of disease in oncology; however,[18F] fluorodeoxyglucose ([18F] FDG) …
management of disease in oncology; however,[18F] fluorodeoxyglucose ([18F] FDG) …
A decade of deuteration in medicinal chemistry
JF Liu, SL Harbeson, CL Brummel, R Tung… - Annual Reports in …, 2017 - Elsevier
The use of deuterium substitution in an effort to produce kinetic isotope effects (KIEs) that
favorably alter pharmacokinetics and metabolism in drug discovery has accelerated in the …
favorably alter pharmacokinetics and metabolism in drug discovery has accelerated in the …
[HTML][HTML] Improving metabolic stability of fluorine-18 labeled verapamil analogs
RM Raaphorst, G Luurtsema, CJ Schokker… - Nuclear medicine and …, 2018 - Elsevier
Introduction Fluorine-18 labeled positron emission tomography (PET) tracers were
developed to obtain more insight into the function of P-glycoprotein (P-gp) in relation to …
developed to obtain more insight into the function of P-glycoprotein (P-gp) in relation to …
Studies into radiolytic decomposition of fluorine-18 labeled radiopharmaceuticals for positron emission tomography
Radiolytic decomposition of high specific concentration radiopharmaceuticals is an
undesired side-effect that can hamper development of novel PET tracers. This was …
undesired side-effect that can hamper development of novel PET tracers. This was …