Evaluation of drug penetration into the brain: a double study by in vivo imaging with positron emission tomography and using an in vitro model of the human blood …

V Josserand, H Pélerin, B De Bruin, B Jego… - … of Pharmacology and …, 2006 - ASPET
The blood-brain barrier (BBB) permeabilities of 11 compounds were measured both in vitro
with a newly developed coculture-based model of human BBB and in vivo with positron …

1-[3-(2-[18F]Fluoropyridin-3-yloxy)propyl]pyrrole-2,5-dione:  Design, Synthesis, and Radiosynthesis of a New [18F]Fluoropyridine-Based Maleimide Reagent for the …

B De Bruin, B Kuhnast, F Hinnen… - Bioconjugate …, 2005 - ACS Publications
FPyME (1-[3-(2-fluoropyridin-3-yloxy)propyl]pyrrole-2,5-dione) was designed as a [ 18 F]fluoropyridine-based
maleimide reagent for the prosthetic labeling of peptides and proteins via …

Design and Synthesis of a New [18F]Fluoropyridine-Based Haloacetamide Reagent for the Labeling of Oligonucleotides:  2-Bromo-N-[3-(2-[18F]fluoropyridin-3 …

B Kuhnast, B de Bruin, F Hinnen, B Tavitian… - Bioconjugate …, 2004 - ACS Publications
Based on the recently highlighted potential of nucleophilic heteroaromatic ortho-radiofluorinations
in the preparation of fluorine-18-labeled radiotracers and radiopharmaceuticals for …

Effect of deuteration on the metabolism and clearance of some pharmacologically active compounds—synthesis and in vitro metabolism of deuterated derivatives of …

J Schofield, D Brasseur, B de Bruin… - Journal of Labelled …, 2013 - Wiley Online Library
The synthesis and in vitro metabolism studies of a family of specifically deuterated derivatives
of dronedarone are described. Metabolic stability and clearance of the parent compound …

The use of biocatalysis in the synthesis of labelled compounds

J Allen, DM Brasseur, B De Bruin… - Journal of Labelled …, 2007 - Wiley Online Library
Since most biotransformations are highly chemo‐, regio‐ and stereoselective, they offer
many opportunities for the synthesis of compounds that are not easily attainable by classical …

Radiosynthesis of (E)-N-(2-[11C] methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor antagonist

C Thominiaux, B de Bruin, Y Bramoullé… - Applied radiation and …, 2006 - Elsevier
Recently, a novel series of amidines has been described, exhibiting high NR2B-subtype
selective N-methyl-D-aspartate (NMDA) antagonist activity with nanomolar or subnanomolar …

Two new convenient syntheses of 14C‐squalene from turbinaric acid

N Philippe, L Rivron, B De Bruin… - Journal of Labelled …, 2018 - Wiley Online Library
Carbon‐14 labeled (6E,10E,14E,18E)‐2,6,10,15,19,23‐hexamethyltetracosa‐2,6,10,14,18,22‐hexaene,
also known as squalene, was synthesized as a tool for pharmacokinetic studies…

Synthesis and in-vivo evaluation of [11C] p-PVP-MEMA as a PET radioligand for imaging nicotinic receptors

…, G Roger, RR Fulton, B Lagnel-de Bruin… - Australian journal of …, 2008 - CSIRO Publishing
Within the class of (4-pyridinyl)vinylpyridines developed by Abbott laboratories as potent
neuronal nicotinic acetylcholine receptor ligands, p-PVP-MEMA ({(R)-2-[6-chloro-5-((E)-2-…

[CITATION][C] Radiosynthesis of [C-11] SSR126374, a new selective CRF1 antagonist

…, F Hinnen, B de Bruin… - JOURNAL OF …, 2011 - … , 350 MAIN ST, MALDEN 02148, MA …

Synthesis of stable isotope labelled internal standards for drug–drug interaction (DDI) studies

J Atzrodt, J Blankenstein, D Brasseur… - Bioorganic & medicinal …, 2012 - Elsevier
The syntheses of stable isotope labelled internal standards of important CYP-isoform selective
probes, like testosterone 1, diclofenac 3, midazolam 5, and dextromethorphan 7, as well …