𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Fluorine-18-labeled tropane analogs for PET imaging studies of the dopamine transporter

✍ Scribed by Robert H. Mach; Michael A. Nader; Richard L. Ehrenkaufer; H. Donald Gage; Steven R. Childers; L. Mark Hodges; Melinda M. Hodges; Huw M.L. Davies

Publisher
John Wiley and Sons
Year
2000
Tongue
English
Weight
295 KB
Volume
37
Category
Article
ISSN
0887-4476

No coin nor oath required. For personal study only.

✦ Synopsis

A series of PET imaging studies were conducted with two fluorine-18-labeled tropane analoges, (18)F-FTT and (18)F-FCT. Both compounds possessed a high affinity and selectivity for the dopamine transporter and had a higher accumulation in the basal ganglia, a brain region having a high density of the dopamine transporter (DAT) than the cerebellum, a reference region devoid of dopaminergic terminals. (18)F-FCT had a higher brain uptake and more suitable basal ganglia:cerebellum (BG:Cb) ratio than (18)F-FTT. (18)F-FCT also displayed reversible binding kinetics in vivo, indicating that the measurement of DAT density in vivo with PET will be relatively insensitive to changes in cerebral blood flow that can occur as a consequence of disease or prolonged cocaine abuse. The uptake of (18)F-FCT was also displaced by an intravenous injection of cocaine (1.0 mg/kg), which is consistent with the labeling of the DAT in vivo by this radiotracer. These data suggest that (18)F-FCT may be a suitable radiotracer for studying DAT function in vivo with PET.

📜 SIMILAR VOLUMES

Fluorine-18 labelling of small interferi
Fluorine-18 labelling of small interfering RNAs (siRNAs) for PET imaging
✍ Thomas Viel; Bertrand Kuhnast; Françoise Hinnen; Raphaël Boisgard; Bertrand Tavi 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 French ⚖ 181 KB

## Abstract Small interfering RNAs (siRNAs), a class of macromolecules constituted by the association of two single‐stranded ribonucleic acids of short sequences, have been labelled with the positron‐emitter fluorine‐18 (__T__~1/2~: 109.8 min). The strategy involves (1) prosthetic conjugation of a

Fluorine-18 labelling of PNAs functional
Fluorine-18 labelling of PNAs functionalized at their pseudo-peptidic backbone for imaging studies with PET
✍ B. Kuhnast; F. Hinnen; R. Hamzavi; R. Boisgard; B. Tavitian; P. E. Nielsen; F. D 📂 Article 📅 2004 🏛 John Wiley and Sons 🌐 French ⚖ 150 KB

## Abstract Peptide nucleic acids (PNAs) form a unique class of synthetic macromolecules, originally designed as ligands for the recognition of double‐stranded DNA, where the deoxyribose phosphate backbone of original DNA is replaced by a pseudo‐peptide __N__‐(2‐aminoethyl)glycyl backbone, while re

Radiosynthesis of [18F]LBT-999, a select
Radiosynthesis of [18F]LBT-999, a selective radioligand for the visualization of the dopamine transporter with PET
✍ Frédéric Dollé; Françoise Hinnen; Patrick Emond; Sylvie Mavel; Zoïa Mincheva; Wa 📂 Article 📅 2006 🏛 John Wiley and Sons 🌐 French ⚖ 161 KB

LBT-999 (8-((E)-4-fluoro-but-2-enyl)-3b-p-tolyl-8-aza-bicyclo[3.2.1]octane-2b-carboxylic acid methyl ester) is a cocaine derivative belonging to a new generation of highly selective dopamine transporter ligands (K D :9 nM). LBT-999 was labelled with fluorine-18 at its fluoromethylvinyl moiety using

One-step radiosynthesis of [18F]LBT-999:
One-step radiosynthesis of [18F]LBT-999: a selective radioligand for the visualization of the dopamine transporter with PET
✍ Frédéric Dollé; Julie Helfenbein; Françoise Hinnen; Sylvie Mavel; Zoïa Mincheva; 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 French ⚖ 153 KB

## Abstract LBT‐999 (8‐((__E__)‐4‐fluoro‐but‐2‐enyl)‐3‐beta‐__p__‐tolyl‐8‐aza‐bicyclo[3.2.1]octane‐2‐beta‐carboxylicacid methyl ester) is a recently developed cocaine derivative belonging to a new generation of highly selective dopamine transporter (DAT) ligands (__K__~D~: 9 nM for the DAT and IC~5

N-substituted phenyltropanes as in vivo
N-substituted phenyltropanes as in vivo binding ligands for rapid imaging studies of the dopamine transporter
✍ Ursula Scheffel; John R. Lever; Philip Abraham; Karol R. Parham; William B. Math 📂 Article 📅 1997 🏛 John Wiley and Sons 🌐 English ⚖ 80 KB 👁 1 views

Variously substituted phenyltropanes are proven as superb binding ligands for the dopamine transporter (DAT). In this study, we examine four N-substituted phenyltropanes which are derivatives of RTI-55 as in vivo binding ligands in mice. In this series, the methyl group on the nitrogen was replaced