Bioactivity | 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]. |
Invitro | 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: |
Name | 3,3'-Difluorobenzaldazine |
CAS | 15332-10-2 |
Formula | C14H10F2N2 |
Molar Mass | 244.24 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |