SML3230
VU0360172 hydrochloride
≥98% (HPLC)
Synonym(s):
N-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide hydrochloride
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About This Item
Empirical Formula (Hill Notation):
C18H15FN2O · HCl
CAS Number:
Molecular Weight:
330.78
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C18H15FN2O.ClH/c19-15-4-1-3-13(11-15)7-9-16-10-8-14(12-20-16)18(22)21-17-5-2-6-17;/h1,3-4,8,10-12,17H,2,5-6H2,(H,21,22);1H
SMILES string
FC1=CC=CC(C#CC2=NC=C(C=C2)C(NC3CCC3)=O)=C1.Cl
InChI key
NBGAPTWZQXSEAA-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
−20°C
Quality Level
Related Categories
General description
VU0360172 is a potent (EC50 = 16.6 nM), systemically active positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5). It is the first orally active mGlu5 PAM to be efficacious in an in vivo preclinical antipsychotic model, producing a dose-dependent reversal of amphetamine-induced hyperlocomotion. It was also found to reduce spontaneous absence seizures in WAG/Rij rats and to inhibit pain. Reduced spontaneous spike and wave discharges without impacting motor behavior in a rat model of absence epilepsy have been observed.
Biochem/physiol Actions
Potent, systemically active mGluR5 PAM
VU0360172 is a potent (EC50 = 16.6 nM), systemically active positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5). It is the first orally active mGlu5 PAM to be efficacious in an in vivo preclinical antipsychotic model, producing a dose-dependent reversal of amphetamine-induced hyperlocomotion. It was also found to reduce absence seizures in WAG/Rij rats and to inhibit pain.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Alice L Rodriguez et al.
Molecular pharmacology, 78(6), 1105-1123 (2010-10-07)
Modulators of metabotropic glutamate receptor subtype 5 (mGluR5) may provide novel treatments for multiple central nervous system (CNS) disorders, including anxiety and schizophrenia. Although compounds have been developed to better understand the physiological roles of mGluR5 and potential usefulness for
Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats
V. D'Amore, et al.
Neuropharmacology, 330-338 (2013)
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