5.04479
JNJ 16259685 - CAS 409345-29-5 - Calbiochem
Synonym(s):
JNJ 16259685 - CAS 409345-29-5 - Calbiochem, (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
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About This Item
Assay
≥98% (TLC)
Quality Level
form
solid
potency
0.55 nM IC50
0.34 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white to off-white
solubility
DMSO: 25 mM
storage temp.
2-8°C
General description
Biochem/physiol Actions
mGlu₁
Preparation Note
Other Notes
Steckler, T., et al. 2005. Psychopharmacology.179, 198.
Steckler, T., et al. 2005. Behav. Brain. Res.164, 52.
Mabire, D., et al. 2005. J. Med. Chem.48, 2134.
Fukunaga, I., et al. 2007. Br. J. Pharmacol.151, 870.
Knopfel, T., et al. 2007. Br. J. Pharmacol.151, 723.
Achat-Mendes, C., et al. 2012. J. Pharmacol. Exp. Ther.343, 214.
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Related Content
Glutamate is an excitatory neurotransmitter found in the synaptic vesicles of glutamatergic synapses. The post-synaptic neurons in these synapses contain ionotropic and metabotropic glutamate receptors. Glutamate binds to AMPA (α-amino-3-hydroxy-5- methylisoxazole-4-propionic acid) subtype glutamate receptors, leading to sodium influx into the post-synaptic cell and resulting in neuronal excitability and synaptic transmission. The NMDA (N-methyl-d-aspartate) subtype glutamate receptors, on the other hand, regulate synaptic plasticity, and can influence learning and memory. The metabotropic g-protein coupled mGluRs modulate downstream calcium signaling pathways and indirectly influence the synapse’s excitability. The synaptic architecture includes intracellular scaffolding proteins (PSD-95, GRIP), intercellular cell adhesion molecules (NCAMs, N-Cadherins), and a variety of signaling proteins (CaMKII/PKA, PP1/PP2B). Processes critical for synaptic transmission and plasticity are influenced by these molecules and their interactions. When the function of these molecules is disrupted, it leads to synaptic dysfunction and degeneration, and can contribute to dementia as seen in Alzheimer’s disease.
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