Catalog Number: 2333
Chemical Name: (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Biological Activity
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
  • M.Wt:
    325.41
  • Formula:
    C20H23NO3
  • Solubility:
    Soluble to 100 mM in ethanol and to 25 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    409345-29-5
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.
Background References
  1. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist.
    Lavreysen et al.
    Neuropharmacology, 2004;47:961
  2. 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
  3. Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task.
    Steckler et al.
    Behav.Brain Res., 2005;164:52
  4. 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:

The citations listed below are publications that use Tocris products. Selected citations for JNJ 16259685 include:

5 Citations: Showing 1 - 5
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  1. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci 2015;35:11252
  2. Activation of a temporal memory in purkinje cells by the mGluR7 receptor.
    Authors: Johansson Et al.
    Cell Rep. 2015;13:1741
  3. 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
  4. Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
    Authors: Shin Et al.
    Aquat Toxicol 2008;105:746
  5. 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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