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Details

Stereochemistry ACHIRAL
Molecular Formula C13H16FN3O2.H2O
Molecular Weight 283.2987
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FK-960 MONOHYDRATE

SMILES

O.CC(=O)N1CCN(CC1)NC(=O)C2=CC=C(F)C=C2

InChI

InChIKey=YCRCWHFFTTVANS-UHFFFAOYSA-N
InChI=1S/C13H16FN3O2.H2O/c1-10(18)16-6-8-17(9-7-16)15-13(19)11-2-4-12(14)5-3-11;/h2-5H,6-9H2,1H3,(H,15,19);1H2

HIDE SMILES / InChI

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C13H16FN3O2
Molecular Weight 265.2834
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/11172755 http://adisinsight.springer.com/drugs/800008887

FK-960 [N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate], a novel putative anti-dementia drug of piperazine derivative, ameliorates memory deficits in a variety of animal models of dementia in rats and monkeys, and also augments long-term potentiation (LTP) in the mossy fiber-CA3 pathway in guinea-pig hippocampal slices. FK-960 acts as Serotonin modulator. FK-960 had been in phase II clinical trials by Fujisawa Pharmaceutical (now Astellas) for the treatment of Alzheimer's disease (AD). However this study was suspended. In 2003 Phase-II for Alzheimer's disease in USA was discontinued and in Jul 2004 - Phase-II for Cognition disorders in Europe.

CNS Activity

Curator's Comment: After oral administration to rhesus monkeys, FK960 is distributed to the entire brain.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Increase by FK960, a novel cognitive enhancer, in glial cell line-derived neurotrophic factor production in cultured rat astrocytes.
2004 Jul 15
Patents

Sample Use Guides

Rhesus macaques: FK960 was intramuscularly administered at doses of 0, 0.01, 0.1, or 1 mg/kg for seven consecutive days. No statistically significant change in any region was observed at doses of 0.01 or 0.1 mg/kg.
Route of Administration: Intramuscular
FK960 (100nM) increased mRNA and protein levels of glial cell line-derived neurotrophic factor (GDNF) in cultured rat astrocytes.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:22:32 UTC 2023
Edited
by admin
on Fri Dec 15 16:22:32 UTC 2023
Record UNII
2GB92V6H2O
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FK-960 MONOHYDRATE
Common Name English
BENZAMIDE, N-(4-ACETYL-1-PIPERAZINYL)-4-FLUORO-, HYDRATE (1:1)
Systematic Name English
FK-960 HYDRATE
Common Name English
Code System Code Type Description
CAS
208186-69-0
Created by admin on Fri Dec 15 16:22:33 UTC 2023 , Edited by admin on Fri Dec 15 16:22:33 UTC 2023
PRIMARY
FDA UNII
2GB92V6H2O
Created by admin on Fri Dec 15 16:22:33 UTC 2023 , Edited by admin on Fri Dec 15 16:22:33 UTC 2023
PRIMARY
PUBCHEM
6918345
Created by admin on Fri Dec 15 16:22:33 UTC 2023 , Edited by admin on Fri Dec 15 16:22:33 UTC 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
ANHYDROUS->SOLVATE
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ACTIVE MOIETY