Cat. No. 2333
Chemical Name: (3,4-Dihydro-2H-pyrano[2,3-b]quinol
Biological ActivitySub-nanomolar potent, non-competitive mGlu1 antagonist (Ki = 0.34 nM). Inhibits glutamate-induced Ca2+ response at the human mGlu1 receptor with an IC50 value of 0.55 nM. Selective over mGlu5 (> 400-fold) and displays no activity at mGlu2, mGlu3, mGlu4, mGlu6, AMPA or NMDA receptors (IC50 > 10 μM). Centrally active following systemic administration.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Xie et al (2010) Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats. Psychopharmacology (Berl). 208 1. PMID: 19847405.
Mabire et al (2005) Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 48 2134. PMID: 15771457.
Steckler et al (2005) Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 164 52. PMID: 16043241.
Lavreysen et al (2004) JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 47 961. PMID: 15555631.
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Citations are publications that use Tocris products. Selected citations for JNJ 16259685 include:
Johansson et al (2015) Activation of a temporal memory in purkinje cells by the mGluR7 receptor. Cell Rep. 13 1741. PMID: 26655894.
Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252. PMID: 26269634.
Hildebrand et al (2009) Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines. J Neurosci 29 9668. PMID: 19657020.
Shin et al (2008) Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. Aquat Toxicol 105 746. PMID: 18174329.
Fukunaga et al (2007) Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices. Br J Pharmacol 151 870. PMID: 17502847.
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Keywords: JNJ 16259685, supplier, potent, mGlu1, mGluR1-selective, non-competitive, antagonists, Group, I, Receptors, Glutamate, Metabotropic, JNJ16259685, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Antagonist products
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