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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=NC=C(C=C1)C2=NC3=CC=C(OC[C@H](O)C[18F])C=C3C=C2

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

Description

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.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Diagnostic
Unknown
Diagnostic
Unknown
Diagnostic
Unknown

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer


Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
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
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).