List of works - Charles S. Elmore

2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity

scientific article

Absence of direct effects on the dopamine D2 receptor by mGluR2/3-selective receptor agonists LY 354,740 and LY 379,268.

scientific article published in January 2011

Abstracts of the 24th international isotope society (UK group) symposium: synthesis and applications of labelled compounds 2015.

scientific article published on 18 March 2016

An integrated strategy for in vivo metabolite profiling using high-resolution mass spectrometry based data processing techniques ⬇️

scientific article published on April 16, 2013

Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity

scientific article published on 12 November 2012

Bioactivation of 2,3-diaminopyridine-containing bradykinin B1 receptor antagonists: irreversible binding to liver microsomal proteins and formation of glutathione conjugates

scientific article published in June 2005

Contribution of artifacts to N-methylated piperazine cyanide adduct formation in vitro from N-alkyl piperazine analogs

scientific article published on 19 February 2013

D2 receptor occupancy in conscious rat brain is not significantly distinguished with [3H]-MNPA, [3H]-(+)-PHNO, and [3H]-raclopride

scientific article published in August 2010

Design, synthesis, in vitro characterization and preliminary imaging studies on fluorinated bile acid derivatives as PET tracers to study hepatic transporters

scientific article published on 9 December 2016

Determining the isotopic abundance of a labeled compound by mass spectrometry and how correcting for natural abundance distribution using analogous data from the unlabeled compound leads to a systematic error.

scientific article

Deuterated active pharmaceutical ingredients: A science-based proposal for synthesis, analysis, and control. Part 1: Framing the problem

scientific article published on 18 June 2019

Development of a 18F-labeled PET radioligand for imaging 5-HT1B receptors: [18F]AZ10419096

scientific article published on 22 October 2019

Development of a PET radioligand for the central 5-HT1B receptor: radiosynthesis and characterization in cynomolgus monkeys of eight radiolabeled compounds

scientific article published on 3 December 2010

Development of new carbon-11 labelled radiotracers for imaging GABAA- and GABAB-benzodiazepine receptors.

scientific article published on 24 May 2012

Differential In Vitro Effects of SGLT2 Inhibitors on Mitochondrial Oxidative Phosphorylation, Glucose Uptake and Cell Metabolism

scientific article published in 2022

Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs

scientific article published on 12 January 2007

Editorial

Evaluation of UV-HPLC and mass spectrometry methods for specific activity determination

scientific article published on 16 September 2014

In vitro and in vivo metabolism of a selective δ-opioid receptor

scientific article published on 13 July 2011

In vitro binding of a radio-labeled positive allosteric modulator for metabotropic glutamate receptor subtype 5.

scientific article published on 6 December 2012

Increased Brain Exposure of an Alpha-Synuclein Fibrillization Modulator by Utilization of an Activated Ester Prodrug Strategy

scientific article published on 19 June 2018

Isotope chemistry; a useful tool in the drug discovery arsenal

scientific article

Isotope labelling by reduction of nitriles: Application to the synthesis of isotopologues of tolmetin and celecoxib

scientific article

Late-occurring and long-circulating metabolites of GABAAα2,3 receptor modulator AZD7325 involving metabolic cyclization and aromatization: relevance to MIST analysis and application for patient compliance.

scientific article published on 8 January 2018

Metabolism of a G protein-coupled receptor modulator, including two major 1,2,4-oxadiazole ring-opened metabolites and a rearranged cysteine-piperazine adduct

scientific article published on 7 March 2012

Multiple compound-related adverse properties contribute to liver injury caused by endothelin receptor antagonists

scientific article

New trends and applications in carboxylation for isotope chemistry.

scientific article

PET Tracers To Study Clinically Relevant Hepatic Transporters

scientific article published on 16 June 2015

Pre-clinical validation of a novel alpha-7 nicotinic receptor radiotracer, [(3)H]AZ11637326: target localization, biodistribution and ligand occupancy in the rat brain

scientific article published on 07 April 2011

Preclinical Evaluation of [F]LCATD as a PET Tracer to Study Drug-Drug Interactions Caused by Inhibition of Hepatic Transporters

scientific article published on 30 July 2018

Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission.

scientific article

Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors.

scientific article

Synthesis of 1β-hydroxydeoxycholic acid in H-2 and unlabeled forms.

scientific article published on 9 February 2017

Synthesis of 2 C-14 labeled cathepsin C inhibitors: The use of a cyanide to displace a Benzotriazole

scientific article published on 21 March 2017

Synthesis of C-14 Labeled GABAA α2/α3 Selective Partial Agonists and the Investigation of Late-Occurring and Long-Circulating Metabolites of GABAA Receptor Modulator AZD7325.

scientific article

Synthesis of C-14 labeled Rac-(3R,2S)-Glycopyrronium Bromide

scientific article published on 31 May 2020

Synthesis of [(3) H] and [(2) H6 ]AZD6642, an inhibitor of 5-lipoxygenase activating protein (FLAP).

scientific article published on 14 June 2016

Synthesis of di-docosahexaenoyl (C22:6)-bis(monoacylglycerol) phosphate in unlabelled and C-13 labelled forms for use as a biomarker of drug induced phospholipidosis

scientific article published on 07 May 2019

Synthesis of three alpha 7 agonists in labeled form

scientific article published on 04 April 2014

Synthesis of ximelagatran, melagatran, hydroxymelagatran, and ethylmelagatran in H-3 labeled form.

scientific article

Synthesis, 3 H-labelling and in vitro evaluation of a substituted dipiperidine alcohol as a potential ligand for chemokine receptor 2

scientific article published on 01 May 2019

The Search for a Subtype-Selective PET Imaging Agent for the GABAA Receptor Complex: Evaluation of the Radiotracer [11C]ADO in Nonhuman Primates

scientific article

The impact of radiochemistry in drug projects: The use of C-14 labeled in the AZD8529, AZD7325 and AZD6280 projects

scientific article published on 16 December 2020

The pro-psychotic metabotropic glutamate receptor compounds fenobam and AZD9272 share binding sites with monoamine oxidase-B inhibitors in humans

scientific article published on 04 October 2019

The synthesis of a tritium, carbon-14, and stable isotope-labeled cathepsin C inhibitors

scientific article published on 21 November 2016

The synthesis of isotopologues of AZD7307: A selective β2 -adrenoreceptor agonist

scientific article published on 19 July 2019

The synthesis of one H-2 labeled and two H-3 labeled leukotriene C4 synthase inhibitors

scientific article published on 22 May 2020

The synthesis of tritium, carbon-14 and stable isotope labelled selective estrogen receptor degraders

scientific article published on 24 August 2016

Use of radiolabeled compounds in drug metabolism and pharmacokinetic studies

scientific article published on 28 February 2012

Visible-Light-Enabled Aminocarbonylation of Unactivated Alkyl Iodides with Stoichiometric Carbon Monoxide for Application on Late-Stage Carbon Isotope Labeling

scientific article published on 11 December 2019

[11C]AZ10419096 - a full antagonist PET radioligand for imaging brain 5-HT1B receptors

scientific article

[N-methyl-3H3]AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy.

scientific article published on 28 April 2009

[³H]Chiba-1001(methyl-SSR180711) has low in vitro binding affinity and poor in vivo selectivity to nicotinic alpha-7 receptor in rodent brain

scientific article published on 29 December 2011

[¹²⁵I]YP20: a novel radioligand specific for the extracellular domain of the CRF₁ receptor

scientific article published on 18 September 2010

List of works by Charles S. Elmore

2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity

Absence of direct effects on the dopamine D2 receptor by mGluR2/3-selective receptor agonists LY 354,740 and LY 379,268.

Abstracts of the 24th international isotope society (UK group) symposium: synthesis and applications of labelled compounds 2015.

An integrated strategy for in vivo metabolite profiling using high-resolution mass spectrometry based data processing techniques ⬇️

Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity

Bioactivation of 2,3-diaminopyridine-containing bradykinin B1 receptor antagonists: irreversible binding to liver microsomal proteins and formation of glutathione conjugates

Contribution of artifacts to N-methylated piperazine cyanide adduct formation in vitro from N-alkyl piperazine analogs

D2 receptor occupancy in conscious rat brain is not significantly distinguished with [3H]-MNPA, [3H]-(+)-PHNO, and [3H]-raclopride

Design, synthesis, in vitro characterization and preliminary imaging studies on fluorinated bile acid derivatives as PET tracers to study hepatic transporters

Determining the isotopic abundance of a labeled compound by mass spectrometry and how correcting for natural abundance distribution using analogous data from the unlabeled compound leads to a systematic error.

Deuterated active pharmaceutical ingredients: A science-based proposal for synthesis, analysis, and control. Part 1: Framing the problem

Development of a 18F-labeled PET radioligand for imaging 5-HT1B receptors: [18F]AZ10419096

Development of a PET radioligand for the central 5-HT1B receptor: radiosynthesis and characterization in cynomolgus monkeys of eight radiolabeled compounds

Development of new carbon-11 labelled radiotracers for imaging GABAA- and GABAB-benzodiazepine receptors.

Differential In Vitro Effects of SGLT2 Inhibitors on Mitochondrial Oxidative Phosphorylation, Glucose Uptake and Cell Metabolism

Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs

Editorial

Evaluation of UV-HPLC and mass spectrometry methods for specific activity determination

In vitro and in vivo metabolism of a selective δ-opioid receptor

In vitro binding of a radio-labeled positive allosteric modulator for metabotropic glutamate receptor subtype 5.

Increased Brain Exposure of an Alpha-Synuclein Fibrillization Modulator by Utilization of an Activated Ester Prodrug Strategy

Isotope chemistry; a useful tool in the drug discovery arsenal

Isotope labelling by reduction of nitriles: Application to the synthesis of isotopologues of tolmetin and celecoxib

Late-occurring and long-circulating metabolites of GABAAα2,3 receptor modulator AZD7325 involving metabolic cyclization and aromatization: relevance to MIST analysis and application for patient compliance.

Metabolism of a G protein-coupled receptor modulator, including two major 1,2,4-oxadiazole ring-opened metabolites and a rearranged cysteine-piperazine adduct

Multiple compound-related adverse properties contribute to liver injury caused by endothelin receptor antagonists

New trends and applications in carboxylation for isotope chemistry.

PET Tracers To Study Clinically Relevant Hepatic Transporters

Pre-clinical validation of a novel alpha-7 nicotinic receptor radiotracer, [(3)H]AZ11637326: target localization, biodistribution and ligand occupancy in the rat brain

Preclinical Evaluation of [F]LCATD as a PET Tracer to Study Drug-Drug Interactions Caused by Inhibition of Hepatic Transporters

Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission.

Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors.

Synthesis of 1β-hydroxydeoxycholic acid in H-2 and unlabeled forms.

Synthesis of 2 C-14 labeled cathepsin C inhibitors: The use of a cyanide to displace a Benzotriazole

Synthesis of C-14 Labeled GABAA α2/α3 Selective Partial Agonists and the Investigation of Late-Occurring and Long-Circulating Metabolites of GABAA Receptor Modulator AZD7325.

Synthesis of C-14 labeled Rac-(3R,2S)-Glycopyrronium Bromide

Synthesis of [(3) H] and [(2) H6 ]AZD6642, an inhibitor of 5-lipoxygenase activating protein (FLAP).

Synthesis of di-docosahexaenoyl (C22:6)-bis(monoacylglycerol) phosphate in unlabelled and C-13 labelled forms for use as a biomarker of drug induced phospholipidosis

Synthesis of three alpha 7 agonists in labeled form

Synthesis of ximelagatran, melagatran, hydroxymelagatran, and ethylmelagatran in H-3 labeled form.

Synthesis, 3 H-labelling and in vitro evaluation of a substituted dipiperidine alcohol as a potential ligand for chemokine receptor 2

The Search for a Subtype-Selective PET Imaging Agent for the GABAA Receptor Complex: Evaluation of the Radiotracer [11C]ADO in Nonhuman Primates

The impact of radiochemistry in drug projects: The use of C-14 labeled in the AZD8529, AZD7325 and AZD6280 projects

The pro-psychotic metabotropic glutamate receptor compounds fenobam and AZD9272 share binding sites with monoamine oxidase-B inhibitors in humans

The synthesis of a tritium, carbon-14, and stable isotope-labeled cathepsin C inhibitors

The synthesis of isotopologues of AZD7307: A selective β2 -adrenoreceptor agonist

The synthesis of one H-2 labeled and two H-3 labeled leukotriene C4 synthase inhibitors

The synthesis of tritium, carbon-14 and stable isotope labelled selective estrogen receptor degraders

Use of radiolabeled compounds in drug metabolism and pharmacokinetic studies

Visible-Light-Enabled Aminocarbonylation of Unactivated Alkyl Iodides with Stoichiometric Carbon Monoxide for Application on Late-Stage Carbon Isotope Labeling

[11C]AZ10419096 - a full antagonist PET radioligand for imaging brain 5-HT1B receptors

[N-methyl-3H3]AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy.

[³H]Chiba-1001(methyl-SSR180711) has low in vitro binding affinity and poor in vivo selectivity to nicotinic alpha-7 receptor in rodent brain

[¹²⁵I]YP20: a novel radioligand specific for the extracellular domain of the CRF₁ receptor