JNJ 16259685
Chemical Name: (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Purity: ≥98%
Biological Activity
JNJ 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Astrocyte inositol triphosphate receptor type 2 and cytosolic phospholipase A2 alpha regulate arteriole responses in mouse neocortical brain slices.
He L, Linden D, Sapirstein A
PLoS ONE, 2102;7(8):e42194. -
Physiological activation of mGlu5 receptors supports the ion channel function of NMDA receptors in hippocampal LTD induction in vivo
KJ O'Riordan, NW Hu, MJ Rowan
Sci Rep, 2018;8(1):4391. -
JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist.
Lavreysen et al.
Neuropharmacology, 2004;47:961 -
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
Mabire et al.
J.Med.Chem., 2005;48:2134 -
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
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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
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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
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Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
Authors: Tabatadze Et al.
J Neurosci 2015;35:11252
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Activation of a temporal memory in purkinje cells by the mGluR7 receptor.
Authors: Johansson Et al.
Cell Rep. 2015;13:1741
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mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions.
Authors: Lum Et al.
Neuropharmacology 2014;79:679
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Synaptic depression via mGluR1 positive allosteric modulation suppresses cue-induced cocaine craving.
Authors: Loweth Et al.
Nat Neurosci 2014;17:73
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Effects of a metabotropic glutamate 1 receptor antagonist on light responses of retinal ganglion cells in a rat model of retinitis pigmentosa.
Authors: Jensen
PLoS One 2013;8:e79126
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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
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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
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Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
Authors: Shin Et al.
Aquat Toxicol 2008;105:746
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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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