Sub-nanomolar potent, non-competitive mGlu1 antagonist (Ki=0.34nM). Inhibits glutamate-induced Ca2+ response at the human mGluR1 (IC50=0.55nM). Selective over mGluR5 (>400-fold). Displays no activity at mGluR2, mGluR3, mGluR4, mGluR6, AMPA or NMDA receptors (IC50>10µM). Centrally active following systemic administration.
Product Details
| Formula: | C20H23NO3 |
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| MW: | 325.4 |
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| CAS: | 409345-29-5 |
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| Purity: | ≥98% (TLC) |
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| Identity: | Determined by 1H-NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO or 100% ethanol. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | +4°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices: I. Fukunaga, et al.; Br. J. Pharmacol.
151, 870 (2007),
Abstract;
Two new non-competitive mGlu1 receptor antagonists are potent tools to unravel functions of this mGlu receptor subtype: T. Knöpfel; Br. J. Pharmacol.
151, 723 (2007),
Abstract;
Effects of mGlu1 receptor blockade on anxiety-related behaviour in the rat lick suppression test: T. Steckler, et al.; Psychopharmacology
179, 198 (2005),
Abstract;
Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial Water maze task: T. Steckler, et al.; Behav. Brain Res.
164, 52 (2005),
Abstract;
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists: D. Mabire, et al.; J. Med. Chem.
48, 2134 (2005),
Abstract;
JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist: H. Lavreysen, et al.; Neuropharmacology
47, 961 (2004),
Abstract;
