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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in ethanol and to 25 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Additional Information
Licensing Caveats:
Sold under license from Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV
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
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