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| | NPS 2390 Basic information |
| Product Name: | NPS 2390 | | Synonyms: | N-tricyclo[3.3.1.13,7]dec-1-yl-2-quinoxalinecarboxamide;N-(1-adamantyl)quinoxaline-2-carboxamide;N-(Adamantan-1-yl)quinoxaline-2-carboxamide;Inhibitor,NPS2390,Calcium-sensing receptor,NPS-2390,mGluR,inhibit,Metabotropic glutamate receptors,CaSR,NPS 2390;2-Quinoxalinecarboxamide, N-tricyclo[3.3.1.13,7]dec-1-yl- | | CAS: | 226878-01-9 | | MF: | C19H21N3O | | MW: | 307.39 | | EINECS: | | | Product Categories: | | | Mol File: | 226878-01-9.mol |  |
| | NPS 2390 Chemical Properties |
| Boiling point | 542.4±30.0 °C(Predicted) | | density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Soluble to 50 mM in DMSO and to 50 mM in ethanol | | form | Powder | | pka | 11.53±0.20(Predicted) | | color | White to light yellow |
| | NPS 2390 Usage And Synthesis |
| Description | Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively). At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes. At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum. | | Uses | NPS 2390 is an inhibitor of CaSR (Calcium-sensing recpetor). NPS 2390 up-regulated anti-apoptotic protein Bcl-2 expression and down-regulated pro-apoptotic protein Bax. | | Uses | Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively). At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes. At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum. | | storage | Store at RT |
| | NPS 2390 Preparation Products And Raw materials |
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