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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
MOL RATIO 1 MOL RATIO (average)
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
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
FK960 (100nM) increased mRNA and protein levels of glial cell line-derived neurotrophic factor (GDNF) in cultured rat astrocytes.
Substance Class Chemical
Record UNII
2GB92V6H2O
Record Status Validated (UNII)
Record Version