1428630-85-6
1428630-85-6
Chemical Structure
VU0424465
- CAS 番号: 1428630-85-6
- Formula:C19H19FN2O2
- Molecular Weight:326.36
IUPAC Name: (R)-5-((3-fluorophenyl)ethynyl)-N-(3-hydroxy-3-methylbutan-2-yl)picolinamide
InChIKey: ZPKZAFDYFVJULO-CYBMUJFWSA-N
SMILES: O=C(N[C@H](C)C(O)(C)C)C1=NC=C(C=C1)C#CC2=CC=CC(F)=C2
Biological Activity: VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons[1][2].
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VU0424465 | 99.84% | VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons. | ||||||||||||||||||||
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References
- [1]. Sengmany K, et al. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017;115:60-72. [Content Brief]
- [2]. Rook JM, Noetzel MJ, Pouliot WA, et al. Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol Psychiatry. 2013;73(6):501-509. [Content Brief]
