Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H26FNO3 |
Molecular Weight | 358.4378 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CNc1ccc(/C(/[H])=C(\[H])/c2ccc(cc2)OCCOCCOCCF)cc1
InChI
InChIKey=NCWZOASIUQVOFA-FWZJPQCDSA-N
InChI=1S/C21H26FNO3/c1-23-20-8-4-18(5-9-20)2-3-19-6-10-21(11-7-19)26-17-16-25-15-14-24-13-12-22/h2-11,23H,12-17H2,1H3/b3-2+/i22-1
Molecular Formula | C21H26FNO3 |
Molecular Weight | 358.4378 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
DescriptionCurator's Comment:: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/?term=21971456; https://www.ncbi.nlm.nih.gov/pubmed/?term=22354138
Curator's Comment:: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/?term=21971456; https://www.ncbi.nlm.nih.gov/pubmed/?term=22354138
Florbetaben F18 is a18F-labeled stilbene derivative used as a tracer for PET imaging of beta-amyloid deposits in the human brain. The F 18 isotope produces a positron signal that is detected by a PET scanner. 3H-florbetaben in vitro binding experiments reveal two binding sites (Kd of 16 nM and 135 nM) in frontal cortex homogenates from patients with AD. Binding of florbetaben F18 to beta-amyloid plaques in post-mortem brain sections from patients with AD using autoradiography correlates with both immunohistochemical and Bielschowsky silver stains. Florbetaben F 18 does not bind to tau or alpha-synuclein in tissue from patients with AD. Neither Neuraceq nor non-radioactive florbetaben F 19 bind to AT8 positive tau deposits in brain tissue from patients with frontotemporal dementia (FTD), using autoradiography and immunohistochemistry, respectively.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P05067|||Q13764|||Q8WZ99 Gene ID: 351.0 Gene Symbol: APP Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19837759 |
3.72 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Diagnostic | NEURACEQ Approved UseNeuraceq is indicated for Positron Emission Tomography (PET) imaging of the brain to estimate β-amyloid neuritic plaque density in adult patients with cognitive impairment who are being evaluated for Alzheimer’s Disease (AD) and other causes of cognitive decline. Launch Date1.39518725E12 |
Sample Use Guides
The recommended dose is 300 MBq (8.1 mCi), maximum 30 mcg mass dose, administered as a single slow intravenous bolus (6 sec/mL) in a total volume of up to 10 mL.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19837759
Fresh-frozen and paraffin-embedded tissue from AD, FTLD-tau and DLB patients and age-matched non-demented controls were used for autoradiographic analysis. Frozen sections, sliced at a 18-μm thickness on a cryostate, and paraffin sections, sliced on a sliding microtome at a thickness of 6μm, were mounted onto glass slides. Paraffin sections were deparaffinized using routine histological methods before performing binding studies and immunohistochemistry, respectively. For autoradiography, sections were incubated with 10 Bq/μl [18F]-florbetaben (specific activity, 351 Ci/mmol) diluted in 25 mM HEPES buffer, pH 7.4, and 0.1% bovine serum albumin (BSA) (200μl/slide) for 1 h at room temperature (RT) in a humidified chamber. Autoradiographic signals were detected by a phosphoimager device (Fuji BAS5000).
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 07:34:39 UTC 2021
by
admin
on
Sat Jun 26 07:34:39 UTC 2021
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Record UNII |
TLA7312TOI
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Record Status |
Validated (UNII)
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Record Version |
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EMA ASSESSMENT REPORTS |
NEURACEQ (AUTHORIZED: RADIONUCLIDE IMAGING)
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NCI_THESAURUS |
C2124
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EMA ASSESSMENT REPORTS |
NEURACEQ (AUTHORIZED: ALZHEIMER DISEASE)
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NDF-RT |
N0000177914
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WHO-ATC |
V09AX06
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FDA ORPHAN DRUG |
732420
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902143-01-5
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7769
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1492940
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TLA7312TOI
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M11720
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C132687
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SUB119774
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9184
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4818
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902143-01-5
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11501341
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DB09148
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CHEMBL1908906
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Florbetaben F 18
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N0000175869
Created by
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PRIMARY | Positron Emitting Activity [MoA] |
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BINDER->LIGAND |
BINDING
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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