VU0477573

Names

[ CAS No. ]:
1946021-40-4

[ Name ]:
VU0477573

[Synonym ]:
MFCD30146434
2-Pyridinecarboxamide, N,N-diethyl-5-[2-(3-fluorophenyl)ethynyl]-
N,N-Diethyl-5-[(3-fluorophenyl)ethynyl]-2-pyridinecarboxamide

Biological Activity

[Description]:

A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM; shows no activity against the other mGlu receptor subtypes (>10 uM); exhibits full occupancy of the MPEP site, does not completely inhibit maximal effects of mGlu5 agonists on intracellular calcium mobilization, inositol phosphate (IP) accumulation, or inhibition of synaptic transmission at the hippocampal Schaffer collateral-CA1 synapse; acts as a full NAM when measuring effects on mGlu5-mediated ERK1/2 phosphorylation; shows robust efficacy, comparable to the mGlu5 NAM MTEP, in models of anxiolytic activity.

[References]

References 1. Nickols HH, et al. J Pharmacol Exp Ther. 2016 Jan;356(1):123-36. View Related Products by Target mGluR

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
472.3±40.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₈H₁₇FN₂O

[ Molecular Weight ]:
296.339

[ Flash Point ]:
239.4±27.3 °C

[ Exact Mass ]:
296.132477

[ LogP ]:
3.23

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.589