445874
mGluR5 Antagonist, MTEP
The mGluR5 Antagonist, MTEP, also referenced under CAS 329205-68-7, controls the biological activity of mGluR5. This small molecule/inhibitor is primarily used for Neuroscience applications.
Sinônimo(s):
mGluR5 Antagonist, MTEP, 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine
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About This Item
Fórmula empírica (Notação de Hill):
C11H8N2S
Número CAS:
Peso molecular:
200.26
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77
Preço e disponibilidade não estão disponíveis no momento.
Produtos recomendados
Nível de qualidade
Ensaio
≥98% (HPLC)
Formulário
solid
fabricante/nome comercial
Calbiochem®
condição de armazenamento
OK to freeze
protect from light
cor
white to yellow
solubilidade
methanol: 1 mg/mL
DMSO: 5 mg/mL
Condições de expedição
ambient
temperatura de armazenamento
2-8°C
cadeia de caracteres SMILES
[s]1c(nc(c1)C#Cc2cnccc2)C
InChI
1S/C11H8N2S/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10/h2-3,6-8H,1H3
chave InChI
NRBNGHCYDWUVLC-UHFFFAOYSA-N
Descrição geral
A brain-permeable (thiazole-pyridine)alkyne compound that acts as a potent, selective and non-competitive mGluR5 (metabotropic glutamate receptor subtype-5) antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM) with in vivo anxiolytic activity in a rodent model (ED50 = 1 mg/kg, ip and 7 mg/kg, po). Devoid of any side effects seen with MPEP and benzodiazepines. Reported to weakly affect the activities of other enzymes and receptors tested (IC50 = 30 µM for MAO-A, >100 µM for mGlu1R, 2R & 7R, and >300 µM for NR2BR).
Ações bioquímicas/fisiológicas
Cell permeable: yes
Primary Target
mGluR5
mGluR5
Product does not compete with ATP.
Reversible: no
Target IC50: 5 nM in Ca2+-flux assay
Target Ki: 16 nM for mGluR5 (metabotropic glutamate receptor subtype-5)
Embalagem
Packaged under inert gas
Advertência
Toxicity: Standard Handling (A)
Reconstituição
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Outras notas
Bradbury, M.J., et al. 2005. J. Pharmacol. Exp. Ther.313, 395.
Busse, C.S., et al. 2004. Neuropsychopharmacology29, 1971.
Roppe, J.R., et al. 2004. Bioorg. Med. Chem. Lett.14, 3993.
Klodzinska, A., et al. 2004. Neuropharmacology47, 342.
Cosford, N.D.P., et al. 2003. J. Med. Chem.46, 204.
Brodkin, J., et al. 2002. Eur. J. Neurosci.16, 2241.
Busse, C.S., et al. 2004. Neuropsychopharmacology29, 1971.
Roppe, J.R., et al. 2004. Bioorg. Med. Chem. Lett.14, 3993.
Klodzinska, A., et al. 2004. Neuropharmacology47, 342.
Cosford, N.D.P., et al. 2003. J. Med. Chem.46, 204.
Brodkin, J., et al. 2002. Eur. J. Neurosci.16, 2241.
Informações legais
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 1
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
Certificados de análise (COA)
Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.
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Jeffrey R Roppe et al.
Bioorganic & medicinal chemistry letters, 14(15), 3993-3996 (2004-07-01)
Structure-activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo receptor occupancy, and is efficacious in the rat fear-potentiated startle
Chris S Busse et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 29(11), 1971-1979 (2004-08-12)
Previous reports have demonstrated the anxiolytic effect of the potent and systemically active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP) in rodents. Here, we present evidence for the anxiolytic activity of a novel mGlu5 receptor antagonist, 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP)
Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice.
Margaret J Bradbury et al.
The Journal of pharmacology and experimental therapeutics, 313(1), 395-402 (2004-12-14)
The metabotropic glutamate receptor subtype mGlu5 modulates central reward pathways. Many transmitter systems within reward pathways affect feeding. We examined the potential role of mGlu5 in body weight regulation using genetic and pharmacological approaches. Adult mice lacking mGlu5, mGluR5-/-, weighed
Nicholas D P Cosford et al.
Journal of medicinal chemistry, 46(2), 204-206 (2003-01-10)
2-Methyl-6-(phenylethynyl)pyridine (3), a potent noncompetitive mGlu5 receptor antagonist widely used to characterize the pharmacology of mGlu5 receptors, suffers from a number of shortcomings as a therapeutic agent, including off-target activity and poor aqueous solubility. Seeking to improve the properties of
J Brodkin et al.
The European journal of neuroscience, 16(11), 2241-2244 (2002-12-11)
It hs been suggested that metabotropic glutamate receptor subtype 5 (mGluR5) play a role in the expression of anxiety, based on anxiolytic-like effects of the selective mGluR5 antagonist MPEP (2-methyl-6-(phenylethynyl)pyridine) in rodent models of anxiety, including stress-induced hyperthermia (SIH). To
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