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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
Structure of THK-5351 F-18

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

HIDE SMILES / InChI

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

TargetsConditions

Conditions

Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer


Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
likely
unlikely
PubMed

PubMed

TitleDatePubMed
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
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
by admin
on Sat Dec 16 11:19:16 GMT 2023
Edited
by admin
on Sat Dec 16 11:19:16 GMT 2023
Record UNII
X7F1935FL1
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
THK-5351 F-18
Common Name English
(18F)(S)-THK-5351
Common Name English
(18F)THK-5351
Common Name English
2-PROPANOL, 1-(FLUORO-18F)-3-((2-(6-(METHYLAMINO)-3-PYRIDINYL)-6-QUINOLINYL)OXY)-, (2S)-
Systematic Name English
THK5351 F-18
Common Name English
J3.349.112C
Code English
Code System Code Type Description
CAS
1707148-68-2
Created by admin on Sat Dec 16 11:19:16 GMT 2023 , Edited by admin on Sat Dec 16 11:19:16 GMT 2023
PRIMARY
FDA UNII
X7F1935FL1
Created by admin on Sat Dec 16 11:19:16 GMT 2023 , Edited by admin on Sat Dec 16 11:19:16 GMT 2023
PRIMARY
PUBCHEM
91810702
Created by admin on Sat Dec 16 11:19:16 GMT 2023 , Edited by admin on Sat Dec 16 11:19:16 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY