SML2783
VU0409551
≥98% (HPLC)
Synonym(s):
JNJ 46778212, JNJ-46778212, VU 0409551, [6,7-Dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](4-fluorophenyl)methanone
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About This Item
Empirical Formula (Hill Notation):
C20H17FN2O3
CAS Number:
Molecular Weight:
352.36
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI key
QUZLMKNNIUSREV-UHFFFAOYSA-N
SMILES string
O=C(N1CCC2=C(C1)OC(COC3=CC=CC=C3)=N2)C4=CC=C(C=C4)F
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
VU0409551 (JNJ-46778212) is an orally available, potent and selective biased metabotropic glutamate receptor subtype 5 positive allosteric modulator (mGlu5 PAM). VU0409551 (JNJ-46778212) selectively potentiates mGlu5 coupling to Gaq-mediated signaling without modulation of NMDAR currents in hippocampal neurons. VU0409551 exhibits potent antipsychotic-like and cognition enhancing activity in animal models.
orally available, potent and selective biased mGlu5 PAM
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Darrick T Balu et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 41(8), 2052-2061 (2016-01-08)
There is substantial evidence that NMDA receptor (NMDAR) hypofunction contributes to the pathophysiology of schizophrenia (SCZ). A recent large-scale genome-wide association study identified serine racemase (SR), the enzyme that produces the NMDAR co-agonist D-serine, as a risk gene for SCZ.
Shane D Hellyer et al.
Journal of neurochemistry, 151(3), 301-315 (2019-08-04)
Allosteric modulators of metabotropic glutamate receptor 5 (mGlu5 ) are a promising therapeutic strategy for a number of neurological disorders. Multiple mGlu5 -positive allosteric modulator (PAM) chemotypes have been discovered that act as either pure PAMs or as PAM-agonists in
Jerri M Rook et al.
Neuron, 86(4), 1029-1040 (2015-05-06)
Schizophrenia is associated with disruptions in N-methyl-D-aspartate glutamate receptor subtype (NMDAR)-mediated excitatory synaptic signaling. The metabotropic glutamate receptor subtype 5 (mGlu5) is a closely associated signaling partner with NMDARs and regulates NMDAR function in forebrain regions implicated in the pathology
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