1946021-40-4

1946021-40-4 structure

Name: VU0477573
Chemical Name: N,N-Diethyl-5-[(3-fluorophenyl)ethynyl]-2-pyridinecarboxamide
CAS Number: 1946021-40-4
Molecular Formula: C₁₈H₁₇FN₂O
Molecular Weight: 296.339
Create Date: 2020-01-12 09:27:06
Modify Date: 2024-08-17 08:36:35
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.

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

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