JNJ 16259685

Catalog # Availability Size / Price Qty
2333/10
2333/50
Cat.No. 2333 - JNJ 16259685 | C20H23NO3 | CAS No. 409345-29-5
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Description: Highly potent, mGlu1-selective non-competitive antagonist

Chemical Name: (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone

Purity: ≥98%

Product Details
Citations (10)
Supplemental Products
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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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

  1. 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
  2. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci  2015;35:11252
  3. Activation of a temporal memory in purkinje cells by the mGluR7 receptor.
    Authors: Johansson Et al.
    Cell Rep.  2015;13:1741
  4. mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions.
    Authors: Lum Et al.
    Neuropharmacology  2014;79:679
  5. Synaptic depression via mGluR1 positive allosteric modulation suppresses cue-induced cocaine craving.
    Authors: Loweth Et al.
    Nat Neurosci  2014;17:73
  6. 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
  7. 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
  8. 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
  9. Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
    Authors: Shin Et al.
    Aquat Toxicol  2008;105:746
  10. 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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