AustralieFrV1, Main, Exploration, bibRecord, 008A97

Radiosynthesis of [18F]PBR111, a selective radioligand for imaging the translocator protein (18kDa) with PET

Identifieur interne : 008A97 ( Main/Exploration ); précédent : 008A96; suivant : 008A98

Radiosynthesis of [18F]PBR111, a selective radioligand for imaging the translocator protein (18kDa) with PET

Auteurs : Frédéric Dollk [France] ; Francoise Hinnen [France] ; Annelaure Damont [France] ; Bertrand Kuhnast [France] ; Christopher Fookes [Australie] ; Tien Pham [Australie] ; Bertrand Tavitian [France] ; Andrew Katsifis [Australie]

Source :

Journal of labelled compounds & radiopharmaceuticals [ 0362-4803 ] ; 2008.

RBID : Pascal:09-0126325

Descripteurs français

Pascal (Inist)
- Fluor 18, Sélectivité, Lipophilie, Récepteur benzodiazépinique périphérique, Potassium Fluorure, Produit radioisotopique, Synthèse chimique, Marquage radioisotopique, Fluor Isotope, Ligand, Cryptand, Dérivé de l'imidazopyridine, Propriété physicochimique, Radiosynthèse, Radioligand, Diaza-18-crown-6(éthylènedioxydiéthylène), Imidazo[1,2-a]pyridine dérivé, Imidazo[1,2-a]pyridine-3-acétamide(6-chloro-N,N-diéthyl-2-[4-(3-fluoropropoxy)phényl]).

English descriptors

KwdEn :
- Chemical synthesis, Cryptand, Fluorine 18, Fluorine Isotopes, Imidazopyridine derivatives, Ligand, Lipophilicity, Peripheral benzodiazepine receptor, Physicochemical properties, Potassium Fluorides, Radioisotopic product, Radiolabelling, Selectivity.

Abstract

PBR111 (2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-diethylacetamide) is a novel, reported, high-affinity and selective ligand for the translocator protein (18 kDa). PBR111 has been labelled with fluorine-18 (half-life: 109.8min) using our Zymate-XP robotic system. The process involves (A) a simple one-step tosyloxy-for-fluorine nucleophilic aliphatic substitution (performed at 165°C for 5min in DMSO using K[¹⁸F]F-Kryptofix 222 and 6.8-7.6 μmol of the corresponding tosylate as precursor for labelling) followed by (B) C-18 PrepSep cartridge pre-purification and (C) semi-preparative HPLC purification on a Waters Symmetry C-18. Up to 4.8 GBq (130 mCi) of [¹⁸F]PBR111 could be obtained with specific radioactivities ranging from 74 to 148GBq/μmol (2-4Ci/μmol) in 75-80min (HPLC purification and SepPak" -based formulation included), starting from a 37.0 GBq (1.0 Ci) [¹⁸F]fluoride batch. Overall non-decay-corrected isolated yields were 8-13% (13-21% decay-corrected).

Affiliations:

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Le document en format XML

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<term>Fluorine Isotopes</term>
<term>Imidazopyridine derivatives</term>
<term>Ligand</term>
<term>Lipophilicity</term>
<term>Peripheral benzodiazepine receptor</term>
<term>Physicochemical properties</term>
<term>Potassium Fluorides</term>
<term>Radioisotopic product</term>
<term>Radiolabelling</term>
<term>Selectivity</term>
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<keywords scheme="Pascal" xml:lang="fr"><term>Fluor 18</term>
<term>Sélectivité</term>
<term>Lipophilie</term>
<term>Récepteur benzodiazépinique périphérique</term>
<term>Potassium Fluorure</term>
<term>Produit radioisotopique</term>
<term>Synthèse chimique</term>
<term>Marquage radioisotopique</term>
<term>Fluor Isotope</term>
<term>Ligand</term>
<term>Cryptand</term>
<term>Dérivé de l'imidazopyridine</term>
<term>Propriété physicochimique</term>
<term>Radiosynthèse</term>
<term>Radioligand</term>
<term>Diaza-18-crown-6(éthylènedioxydiéthylène)</term>
<term>Imidazo[1,2-a]pyridine dérivé</term>
<term>Imidazo[1,2-a]pyridine-3-acétamide(6-chloro-N,N-diéthyl-2-[4-(3-fluoropropoxy)phényl])</term>
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<front><div type="abstract" xml:lang="en">PBR111 (2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-diethylacetamide) is a novel, reported, high-affinity and selective ligand for the translocator protein (18 kDa). PBR111 has been labelled with fluorine-18 (half-life: 109.8min) using our Zymate-XP robotic system. The process involves (A) a simple one-step tosyloxy-for-fluorine nucleophilic aliphatic substitution (performed at 165°C for 5min in DMSO using K[<sup>18</sup>
F]F-Kryptofix 222 and 6.8-7.6 μmol of the corresponding tosylate as precursor for labelling) followed by (B) C-18 PrepSep cartridge pre-purification and (C) semi-preparative HPLC purification on a Waters Symmetry C-18. Up to 4.8 GBq (130 mCi) of [<sup>18</sup>
F]PBR111 could be obtained with specific radioactivities ranging from 74 to 148GBq/μmol (2-4Ci/μmol) in 75-80min (HPLC purification and SepPak" -based formulation included), starting from a 37.0 GBq (1.0 Ci) [<sup>18</sup>
F]fluoride batch. Overall non-decay-corrected isolated yields were 8-13% (13-21% decay-corrected).</div>
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<name sortKey="Tavitian, Bertrand" sort="Tavitian, Bertrand" uniqKey="Tavitian B" first="Bertrand" last="Tavitian">Bertrand Tavitian</name>
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Radiosynthesis of [18F]PBR111, a selective radioligand for imaging the translocator protein (18kDa) with PET

Radiosynthesis of [18F]PBR111, a selective radioligand for imaging the translocator protein (18kDa) with PET

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri