FK-960

Details

Stereochemistry	ACHIRAL
Molecular Formula	C13H16FN3O2
Molecular Weight	265.2834
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=XTOKQKWTUYYVAO-UHFFFAOYSA-N

InChI=1S/C13H16FN3O2/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)

HIDE SMILES / InChI

Description
Sources: http://en.pharmacodia.com/web/drug/1_6000.html
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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
synaptic transmission, glutamatergic 2 Target ID: GO:0035249 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12531516	Modulator 828
serotonin metabolic process 3 Target ID: GO:0042428 Sources: http://adisinsight.springer.com/drugs/800008887 \| https://www.axonmedchem.com/product/1607	Modulator 828
somatostatin secretion 3 Target ID: GO:0070253 Sources: https://www.axonmedchem.com/product/1607	Modulator 828
Glial cell line-derived neurotrophic factor 3 Target ID: Q07731\|\|\|Q9QXJ8 Gene ID: 25453.0 Gene Symbol: Gdnf Target Organism: Rattus norvegicus (Rat) Sources: https://www.ncbi.nlm.nih.gov/pubmed/15193999	Activator 1430

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alzheimer’s disease 272 Sources: http://adisinsight.springer.com/drugs/800008887	Primary		Phase II 1132	Unknown Approved Use Unknown
Cognition disorders 21 Sources: http://adisinsight.springer.com/drugs/800008887	Primary		Phase II 1132	Unknown Approved Use Unknown

Sourcing

Vendor/Aggregator	ID	URL
Axon MedChem	1607	https://www.axonmedchem.com/product/1607
MolPort	MolPort-022-863-699	https://www.molport.com/shop/molecule-link/MolPort-022-863-699
MuseChem	I005972	https://www.musechem.com/product/I005972.html
eMolecules	275137585	https://orderbb.emolecules.com/search/#?query=275137585
eMolecules	36367180	https://orderbb.emolecules.com/search/#?query=36367180

PubMed

Title	Date	PubMed
Increase by FK960, a novel cognitive enhancer, in glial cell line-derived neurotrophic factor production in cultured rat astrocytes.	2004 Jul 15	15193999

Patents

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.

Name

Type

Language

FK-960

Code

English

BENZAMIDE, N-(4-ACETYL-1-PIPERAZINYL)-4-FLUORO-

Systematic Name

English

FK960

Code

English

Code System Code Type Description

EPA CompTox

DTXSID50158424