DFB

Names

[ Name ]:
DFB

[Synonym ]:
m-Fluor-benzaldazin
3,3'-Difluorobenzaldazine
3,3'-DIFLUOROBENZALDAZINE
DFB

Biological Activity

[Description]:

3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

[In Vitro]

3,3'-Difluorobenzaldazine (DFB) causes a concentration-dependent potentiation of the response of human mGluR5 CHO cells to 300 nM glutamate in this assay. The maximal potentiation at this concentration of glutamate is approximately 3.1-fold, with an EC50 for potentiation of 2.6 μM. 3,3'-Difluorobenzaldazine causes similar potentiation of the responses of both human mGluR5 and rat mGluR5 CHO cells to glutamate, quisqualate, and DHPG with comparable potencies[1].

[In Vivo]

3,3'-Difluorobenzaldazine (40-100 nmol; icv) attenuates the locomotor hyperactivity, motor incoordination, and cognitive impairment induced by Ketamine[2]. Animal Model: Male NMRI and ICR mice (8-9 weeks, 33-40 g)[2] Dosage: 40-100 nmol (~9.7-24.4 μg) Administration: ICV Result: Attenuated the locomotor hyperactivity, motor incoordination, and cognitive impairment induced by Ketamine.

[References]

[1]. O'Brien JA, et al, Chen TB, et al. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003;64(3):731-740.

[2]. O'Brien JA, et al. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003;64(3):731-740.

Chemical & Physical Properties

[ Density]:
1.12g/cm3

[ Boiling Point ]:
326.6ºC at 760mmHg

[ Molecular Formula ]:
C₁₄H₁₀F₂N₂

[ Molecular Weight ]:
244.23900

[ Flash Point ]:
151.3ºC

[ Exact Mass ]:
244.08100

[ PSA ]:
24.72000

[ LogP ]:
3.41780

[ Vapour Pressure ]:
0.000406mmHg at 25°C

[ Index of Refraction ]:
1.539

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H400

[ Precautionary Statements ]:
P273

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn: Harmful;N: Dangerous for the environment;

[ Risk Phrases ]:
R22

[ Safety Phrases ]:
S60

[ RIDADR ]:
UN 3077 9/PG 3

[ HS Code ]:
2928000090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2928000090

[ Summary ]:
2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

Articles

A novel safety assessment strategy applied to non-selective extracts.

Food Chem. Toxicol. 80 , 163-81, (2015)

A main challenge in food safety research is to demonstrate that processing of foodstuffs does not lead to the formation of substances for which the safety upon consumption might be questioned. This is...

Metabotropic glutamate receptor 5 positive allosteric modulators are neuroprotective in a mouse model of Huntington's disease.

Br. J. Pharmacol. 169 , 909-21, (2013)

Huntington's disease (HD) is an autosomal dominant neurodegenerative disorder caused by a polyglutamine expansion in the huntingtin protein. We have previously demonstrated that the cell signalling of...

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

Mol. Pharmacol. 64 , 731-740, (2003)

We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely related analogs exerts a spectrum of eff...

DFB