NPS 2390 Inhibitor CAS No. 226878-01-9

Cat. No.	Name	Size	Price	Add Cart
KI1105	NPS 2390	10 mg	$310

Chemical Characteristic

Product Name	NPS 2390
CAS No.	226878-01-9
Molecular Weight	307.39
Formula	C₁₉H₂₁N₃O
Chemical Name	N-((1r,3R,5r,7S)-adamantan-1-yl)quinoxaline-2-carboxamide
Smiles	n1c(cnc2ccccc12)C(=O)NC12CC3CC(CC(C1)C3)C2
Chemical Structure

Biological activities

NPS2390 is a group I mGlu antagonist. NPS2390 displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors.^[1] In vitro, pre-incubation with NPS2390 (10 µM) significantly reduces the stimulatory effect of NPS R-467 on Exp oocytes.^[2] NPS2390 inhibits [³H]R214127 binding to rat mGlu1a receptor CHO-dhfr-membranes with a Ki value of 1.36 nM.^[3] In addition, NPS2390 has a higher potency in inhibiting [³H]R214127 binding with an IC50 of 15 nM than BAY 36-7620. In vivo, NPS2390 exhibits a relatively high potency in occupying mGlu1 receptors in rat cerebellum and thalamus with ED50 of 0.75 and 0.63 mg/kg, respectively.^[4]

Protocols

In vitro: NPS2390 is dissolved in DMSO.^[4]

References

[1] Mabire D, et al. Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J Med Chem. 2005, 48(6): 2134-2153. [2] De Santis T, et al. The extracellular calcium-sensing receptor is expressed in the cumulus-oocyte complex in mammals and modulates oocyte meiotic maturation. Reproduction. 2009, 138(3): 439-452. [3] Lavreysen H, et al. [³H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. Mol Pharmacol. 2003, 63(5): 1082-1093. [4] Lavreysen H, et al. Metabotropic glutamate 1 receptor distribution and occupancy in the rat brain: a quantitative autoradiographic study using [³H]R214127. Neuropharmacology. 2004, 46(5): 609-619.

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