Chemical Name: (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Biological ActivityJNJ 16259685 is a sub-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist.
Lavreysen et al.
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
Mabire et al.
Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task.
Steckler et al.
Behav.Brain Res., 2005;164:52
Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats.
Xie et al.
Psychopharmacology (Berl)., 2010;208:1
Citations for JNJ 16259685
The citations listed below are publications that use Tocris products. Selected citations for JNJ 16259685 include:
10 Citations: Showing 1 - 10
Long-Term Potentiation at the Mossy Fiber-Granule Cell Relay Invokes Postsynaptic Second-Messenger Regulation of Kv4 Channels.
Authors: Rizwan Et al.
J Neurosci 2016;36:11196
Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
Authors: Tabatadze Et al.
J Neurosci 2015;35:11252
Activation of a temporal memory in purkinje cells by the mGluR7 receptor.
Authors: Johansson Et al.
Cell Rep. 2015;13:1741
mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions.
Authors: Lum Et al.
Synaptic depression via mGluR1 positive allosteric modulation suppresses cue-induced cocaine craving.
Authors: Loweth Et al.
Nat Neurosci 2014;17:73
Effects of a metabotropic glutamate 1 receptor antagonist on light responses of retinal ganglion cells in a rat model of retinitis pigmentosa.
PLoS One 2013;8:e79126
Prolonged postinhibitory rebound firing in the cerebellar nuclei mediated by group I metabotropic glutamate receptor potentiation of L-type calcium currents.
Authors: Zheng and Raman
J Neurosci 2011;31:10283
Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines.
Authors: Hildebrand Et al.
J Neurosci 2009;29:9668
Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
Authors: Shin Et al.
Aquat Toxicol 2008;105:746
Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices.
Authors: Fukunaga Et al.
Br J Pharmacol 2007;151:870
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