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JNJ 16259685

mGluR antagonist
ALX-550-412-M025 25 mg 505.00 USD
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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 Specification

Purity:≥98% (TLC)
Identity:Determined by 1H-NMR.
Appearance:White to off-white solid.
Solubility:Soluble in DMSO or 100% ethanol.
Long Term Storage:+4°C
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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;

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