Compounds > (r)-(11c)1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide

(r)-(11c)1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide and Disease-Models--Animal

(r)-(11c)1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide has been researched along with Disease-Models--Animal* in 1 studies

Other Studies

1 other study(ies) available for (r)-(11c)1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide and Disease-Models--Animal

Article	Year
Synthesis of 6-[¹⁸F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET. Bioorganic & medicinal chemistry letters, 2011, Aug-15, Volume: 21, Issue:16 6-Fluoro-PBR28 (N-(6-fluoro-4-phenoxypyridin-3-yl)-N-(2-methoxybenzyl)acetamide), a fluorinated analogue of the recently developed TSPO 18 kDa ligand PBR28, was synthesized and labelled with fluorine-18. 6-Fluoro-PBR28 and its 6-chloro/6-bromo counterparts were synthesized in six chemical steps and obtained in 16%, 10% and 19% overall yields, respectively. Labelling with fluorine-18 was performed in one single step (chlorine/bromine-for-fluorine heteroaromatic substitution) using a Zymate-XP robotic system affording HPLC-purified, ready-to-inject, 6-[(18)F]fluoro-PBR28 (>95% radiochemically pure). Non-decay-corrected overall yields were 9-10% and specific radioactivities ranged from 74 to 148 GBq/μmol. In vitro binding experiments, dynamic μPET studies performed in a rat model of acute neuroinflammation (unilaterally, AMPA-induced, striatum-lesioned rats) and ex vivo autoradiography on the same model demonstrated the potential of 6-[(18)F]fluoro-PBR28 to image the TSPO 18 kDa using PET. Topics: Acetamides; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; Aminopyridines; Animals; Corpus Striatum; Disease Models, Animal; Fluorine Radioisotopes; Ligands; Molecular Imaging; Molecular Structure; Positron-Emission Tomography; Radiopharmaceuticals; Rats; Receptors, GABA; Stereoisomerism	2011

Article

Year

Synthesis of 6-[¹⁸F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET.

Bioorganic & medicinal chemistry letters, 2011, Aug-15, Volume: 21, Issue:16

6-Fluoro-PBR28 (N-(6-fluoro-4-phenoxypyridin-3-yl)-N-(2-methoxybenzyl)acetamide), a fluorinated analogue of the recently developed TSPO 18 kDa ligand PBR28, was synthesized and labelled with fluorine-18. 6-Fluoro-PBR28 and its 6-chloro/6-bromo counterparts were synthesized in six chemical steps and obtained in 16%, 10% and 19% overall yields, respectively. Labelling with fluorine-18 was performed in one single step (chlorine/bromine-for-fluorine heteroaromatic substitution) using a Zymate-XP robotic system affording HPLC-purified, ready-to-inject, 6-[(18)F]fluoro-PBR28 (>95% radiochemically pure). Non-decay-corrected overall yields were 9-10% and specific radioactivities ranged from 74 to 148 GBq/μmol. In vitro binding experiments, dynamic μPET studies performed in a rat model of acute neuroinflammation (unilaterally, AMPA-induced, striatum-lesioned rats) and ex vivo autoradiography on the same model demonstrated the potential of 6-[(18)F]fluoro-PBR28 to image the TSPO 18 kDa using PET.

Topics: Acetamides; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; Aminopyridines; Animals; Corpus Striatum; Disease Models, Animal; Fluorine Radioisotopes; Ligands; Molecular Imaging; Molecular Structure; Positron-Emission Tomography; Radiopharmaceuticals; Rats; Receptors, GABA; Stereoisomerism

2011