Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C18H18FN3O2 |
| Molecular Weight | 326.3554 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC1=CC=C(C=N1)C2=NC3=C(C=C2)C=C(OC[C@H](O)C[18F])C=C3
InChI
InChIKey=DLVXFZWSPCOWSN-DHZJDKHOSA-N
InChI=1S/C18H18FN3O2/c1-20-18-7-3-13(10-21-18)17-5-2-12-8-15(4-6-16(12)22-17)24-11-14(23)9-19/h2-8,10,14,23H,9,11H2,1H3,(H,20,21)/t14-/m1/s1/i19-1
| Molecular Formula | C18H18FN3O2 |
| Molecular Weight | 326.3554 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
18F-THK-5351 is a novel radiotracer that demonstrates high binding selectivity and affinity for tau pathology and exhibits better pharmacokinetics in the living brain than previous THK tau probes. FluoroTau is in phase II clinical trials as a positron emission tomography (PET) imaging agent for the diagnosis and monitoring of the progression of Alzheimer's disease(AD) in South Korea.
This compound was originally discovered by Tohoku University, and now is being developed by GE Healthcare, Samung Medical Centre and Asan Medical Center.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Dynamic PET Measures of Tau Accumulation in Cognitively Normal Older Adults and Alzheimer's Disease Patients Measured Using [18F] THK-5351. | 2016 |
|
| Structure-Activity Relationship of 2-Arylquinolines as PET Imaging Tracers for Tau Pathology in Alzheimer Disease. | 2016 Apr |
|
| 18F-Labeled 2-Arylquinoline Derivatives for Tau Imaging: Chemical, Radiochemical, Biological and Clinical Features. | 2017 |
|
| Tau imaging with [(18) F]THK-5351 in progressive supranuclear palsy. | 2017 Jan |
Patents
Sample Use Guides
18F-THK-5351 radiotracer was injected through a venous line into the arm of 12
subjects with a mean administered activity of 377.8 +/-14.0 MBq. The scanning
protocol included 1–2 min emission scans for four cycles at 10, 60, 120, and 240
min post-injection. Each cycle consisted of seven bed positions, thus the
whole-body scanning time was 10 min per cycle.
Route of Administration:
Intravenous
In Vitro Use Guide
Curator's Comment: In vitro saturation binding assays were conducted to measure
the binding affinity of 18F-THK5351 for postmortem tissues from
AD patients.
18F-THK5351 bound to AD hippocampal
homogenates with high affinity (Kd 5 2.9 nmol/L; maximum
number of binding sites =368.3 pmol/g tissue).
| Substance Class |
Chemical
Created
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admin
on
Edited
Sat Dec 16 11:19:16 GMT 2023
by
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| Record UNII |
X7F1935FL1
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| Record Status |
Validated (UNII)
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X7F1935FL1
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91810702
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ACTIVE MOIETY |
