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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
Structure of FLORBETABEN F-18

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

HIDE SMILES / InChI

Description
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.

CNS Activity

Curator's Comment:: Following intravenous administration, florbetaben F 18 crosses the blood brain barrier and shows differential retention in brain regions that contain beta-amyloid deposits

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P05067|||Q13764|||Q8WZ99
Gene ID: 351.0
Gene Symbol: APP
Target Organism: Homo sapiens (Human)
3.72 nM [Kd]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Diagnostic
NEURACEQ

Approved Use

Neuraceq 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 Date

1.39518725E12
PubMed

PubMed

TitleDatePubMed
Patents

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
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).
Name Type Language
FLORBETABEN F-18
DASH  
Common Name English
BAY-949172
Code English
AV-1
Code English
FLORBETABEN F 18 [MI]
Common Name English
NEURACEQ
Brand Name English
FLORBETABEN F-18 [ORANGE BOOK]
Common Name English
FLORBETABEN F 18
Common Name English
FLORBETABEN F18 [USAN]
Common Name English
FLORBETABEN (F-18)
Common Name English
FLORBETABEN
Common Name English
FLORBETABEN F18
USAN  
USAN  
Official Name English
FLORBETABEN (18F) [INN]
Common Name English
FLORBETABEN (18F)
INN   WHO-DD  
INN  
Official Name English
FLORBETABEN (18F) [WHO-DD]
Common Name English
BAY94-9172
Code English
BAY-94-9172
Code English
FLORBETABEN(18F) [JAN]
Common Name English
4-((1E)-2-(4-(2-(2-(2-((SUP 18(F))FLUOROETHOXY)ETHOXY)ETHOXY)PHENYL)ETH-1-EN-1-YL)-N-METHYLANILINE
Common Name English
ZK-6013443
Code English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS NEURACEQ (AUTHORIZED: RADIONUCLIDE IMAGING)
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
NCI_THESAURUS C2124
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
EMA ASSESSMENT REPORTS NEURACEQ (AUTHORIZED: ALZHEIMER DISEASE)
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
NDF-RT N0000177914
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
WHO-ATC V09AX06
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
FDA ORPHAN DRUG 732420
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
Code System Code Type Description
CAS
902143-01-5
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
IUPHAR
7769
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
RXCUI
1492940
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY RxNorm
FDA UNII
TLA7312TOI
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
MERCK INDEX
M11720
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
NCI_THESAURUS
C132687
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
EVMPD
SUB119774
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
INN
9184
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
DRUG CENTRAL
4818
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
EPA CompTox
902143-01-5
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
PUBCHEM
11501341
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
DRUG BANK
DB09148
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
ChEMBL
CHEMBL1908906
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
LACTMED
Florbetaben F 18
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY
NDF-RT
N0000175869
Created by admin on Sat Jun 26 07:34:39 UTC 2021 , Edited by admin on Sat Jun 26 07:34:39 UTC 2021
PRIMARY Positron Emitting Activity [MoA]