Compounds > vu0092273
Page last updated: 2024-11-12

vu0092273

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Description

VU0092273: mGlu(5) positive allosteric modulator [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16000100
CHEMBL ID1684241
SCHEMBL ID3637291
MeSH IDM0577326

Synonyms (22)

Synonym
AKOS005420976
OPREA1_591781
EU-0040376
SCHEMBL3637291
CHEMBL1684241 ,
vu0092273
VU0092273-7
bdbm50337957
(4-hydroxypiperidin-1-yl)(4-(phenylethynyl)phenyl)methanone
VU0092273-6
MLS003871697
smr002528235
gtpl6421
(4-hydroxypiperidin-1-yl)-[4-(2-phenylethynyl)phenyl]methanone
vu 0092273
393110-43-5
1-[4-(2-phenylethynyl)benzoyl]piperidin-4-ol
1-[4-(phenylethynyl)benzoyl]-4-piperidinol
4-hydroxypiperidin-1-yl-((4-phenylethynyl)phenyl)methanone
Q27089171
Z245197204
(4-hydroxypiperidino)[4-(2-phenyl-1-ethynyl)phenyl]methanone
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.01420.01680.0210AID716175
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
metabotropic glutamate receptor 5 precursorRattus norvegicus (Norway rat)EC50 (µMol)0.52300.52300.52300.5230AID588715
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)EC50 (µMol)0.27000.00151.653710.0000AID716174
Metabotropic glutamate receptor 5Homo sapiens (human)EC50 (µMol)0.01000.00190.61454.1000AID578606
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
desensitization of G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of DNA-templated transcriptionMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
learning or memoryMetabotropic glutamate receptor 5Homo sapiens (human)
learningMetabotropic glutamate receptor 5Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticityMetabotropic glutamate receptor 5Homo sapiens (human)
synapse organizationMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of calcium-mediated signalingMetabotropic glutamate receptor 5Homo sapiens (human)
cognitionMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
cellular response to amyloid-betaMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 5Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase activator activityMetabotropic glutamate receptor 5Homo sapiens (human)
A2A adenosine receptor bindingMetabotropic glutamate receptor 5Homo sapiens (human)
identical protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase bindingMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
dendriteMetabotropic glutamate receptor 5Homo sapiens (human)
cytoplasmMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic spineMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic shaftMetabotropic glutamate receptor 5Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 5Homo sapiens (human)
Schaffer collateral - CA1 synapseMetabotropic glutamate receptor 5Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 5Homo sapiens (human)
postsynaptic density membraneMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID716176Negative allosteric modulation of rat mGlu3 assessed as inhibition of glutamate-induced thallium flux through GIRK channels by cell-based assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
AID578606Positive allosteric modulation of mGlu5 receptor assessed as calcium mobilization2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.
AID716174Positive allosteric modulation of rat mGlu5 expressed in HEK293 cells in presence of glutamate EC20 concentration by Fluo-2AM dye based fluorescence analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
AID716175Negative allosteric modulation of rat mGlu3 assessed as assessed as thallium flux through GIRK channels by cell-based assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
AID578607Positive allosteric modulation of mGlu5 receptor assessed as calcium mobilization at 30 uM relative to glutamate2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.
AID1346254Rat mGlu5 receptor (Metabotropic glutamate receptors)2012Molecular pharmacology, Feb, Volume: 81, Issue:2
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (80.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		2.1110pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		2.1110primary amine
thiazoles
[no description available]		2.11101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
methoxyhydroxyphenylglycol
Methoxyhydroxyphenylglycol: Synthesized from endogenous epinephrine and norepinephrine in vivo. It is found in brain, blood, CSF, and urine, where its concentrations are used to measure catecholamine turnover.		2.2510methoxybenzenes;
phenols
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.0710glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
3,4-dihydroxyphenylglycol
3,4-dihydroxyphenylglycol: noradrenaline metabolite in mouse brain; RN given refers to cpd without isomeric designation. 3,4-dihydroxyphenylethyleneglycol : A tetrol composed of ethyleneglycol having a 3,4-dihydroxyphenyl group at the 1-position.		2.2510catechols;
tetrol		metabolite;
mouse metabolite
piperidines
Piperidines: A family of hexahydropyridines.		2.8130
vu0409106
VU0409106: a metabotropic glutamate receptor 5 antagonist; structure in first source		2.1110
n-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide
N-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide: an mGlu5 agonist; structure in first source		2.4920
ml289
ML289: metabotropic glutamate receptor 3 probe		2.0710
ConditionIndicatedRelationship StrengthStudiesTrials
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0710
Cerebral Ischemia
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Astrocytosis
[description not available]		02.2510
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		02.2510