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Synthesis and preliminary evaluation of novel PET probes for GSK-3 imaging
Non-invasive imaging of GSK-3 expression in the brain will help to understand the role of GSK-3 in disease pathology and progression. Herein, we report the radiosynthesis and evaluation of two novel isonicotinamide based 18 F labeled PET probes, [ 18 F] 2 and [ 18 F] 6 for noninvasive imaging of GSK...
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Published in: | Scientific reports 2024-07, Vol.14 (1), p.15960-14, Article 15960 |
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Main Authors: | , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites |
Online Access: | Get full text |
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Summary: | Non-invasive imaging of GSK-3 expression in the brain will help to understand the role of GSK-3 in disease pathology and progression. Herein, we report the radiosynthesis and evaluation of two novel isonicotinamide based
18
F labeled PET probes, [
18
F]
2
and [
18
F]
6
for noninvasive imaging of GSK3. Among the developed PET probes, the in vitro blood–brain permeability coefficient of
2
(38 ± 20 × 10
–6
cm/s,
n
= 3) was found to be better than
6 (
8.75 ± 3.90 × 10
–6
cm/s,
n
= 5). The reference compounds
2
and
6
showed nanomolar affinity towards GSK-3α and GSK-3β. PET probe [
18
F]
2
showed higher stability (100%) in mouse and human serums compared to [
18
F]
6
(67.01 ± 4.93%,
n
= 3) in mouse serum and 66.20 ± 6.38%,
n
= 3) in human serum at 120 min post incubation. The in vivo imaging and blocking studies were performed in wild-type mice only with [
18
F]
2
due to its observed stability. [
18
F]
2
showed a SUV of 0.92 ± 0.28 (
n
= 6) in mice brain as early as 5 min post-injection followed by gradual clearance over time. |
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ISSN: | 2045-2322 2045-2322 |
DOI: | 10.1038/s41598-024-65943-z |