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| Hauptseite > Publikationsdatenbank > [18F]ALX5406: A Brain-Penetrating Prodrug for GlyT1-Specific PET Imaging > print |
| Hauptseite > Publikationsdatenbank > [18F]ALX5406: A Brain-Penetrating Prodrug for GlyT1-Specific PET Imaging > print |
| 001 | 894996 | ||
| 005 | 20210930133543.0 | ||
| 024 | 7 | _ | |a 10.1021/acschemneuro.1c00284 |2 doi |
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| 100 | 1 | _ | |a Hoffmann, Chris |0 P:(DE-Juel1)180770 |b 0 |u fzj |
| 245 | _ | _ | |a [18F]ALX5406: A Brain-Penetrating Prodrug for GlyT1-Specific PET Imaging |
| 260 | _ | _ | |a Washington, DC |c 2021 |b ACS Publ. |
| 336 | 7 | _ | |a article |2 DRIVER |
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| 520 | _ | _ | |a Selective inhibition of glycine transporter 1 (GlyT1) has emerged as a potential approach to alleviate N-methyl-D-aspartate receptor (NMDAR) hypofunction in patients with schizophrenia and cognitive decline. ALX5407 is a potent and selective inhibitor of GlyT1 derived from the metabolic intermediate sarcosine (N-methylglycine) that showed antipsychotic potential in a number of animal models. Whereas clinical application of ALX5407 is limited by adverse effects on motor performance and respiratoryfunction, a suitably radiolabeled drug could represent a promising PET tracer for the visualization of GlyT1 in the brain. Herein, [18F]ALX5407 and the corresponding methyl ester, [18F]ALX5406, were prepared by alcoholenhanced copper mediated radiofluorination and studied in vitro in rat brain slices and in vivo in normal rats. [18F]ALX5407 demonstrated accumulation consistent with the distribution of GlyT1 in in vitro autoradiographic studies but no brain uptake in μPET experiments in naıv̈ e rats. In contrast, the methyl ester [18F]ALX5406 rapidly entered the brain and was enzymatically transformed into [18F]ALX5407, resulting in a regional accumulation pattern consistent with GlyT1 specific binding. We conclude that [18F]ALX5406 is a promising and easily accessible PET probe for preclinical in vivo imaging of GlyT1 in the brain. |
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| 700 | 1 | _ | |a Neumaier, Felix |0 P:(DE-Juel1)175142 |b 2 |u fzj |
| 700 | 1 | _ | |a Zlatopolskiy, Boris D. |0 P:(DE-Juel1)176188 |b 3 |
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| 700 | 1 | _ | |a Neumaier, Bernd |0 P:(DE-Juel1)166419 |b 9 |e Corresponding author |
| 773 | _ | _ | |a 10.1021/acschemneuro.1c00284 |g Vol. 12, no. 18, p. 3335 - 3346 |0 PERI:(DE-600)2528493-9 |n 18 |p 3335 - 3346 |t ACS chemical neuroscience |v 12 |y 2021 |x 1948-7193 |
| 856 | 4 | _ | |y Published on 2021-08-27. Available in OpenAccess from 2022-08-27. |u https://juser.fz-juelich.de/record/894996/files/Autorenversion.pdf |
| 856 | 4 | _ | |y Published on 2021-08-27. Available in OpenAccess from 2022-08-27. |u https://juser.fz-juelich.de/record/894996/files/Supporting%20Information.pdf |
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