JNJ 16259685

Key Product Details

Product Description

JNJ 16259685 is a sub-nanomolar potent, non-competitive mGlu₁ antagonist (K_i = 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.

Product Specifications for JNJ 16259685

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for JNJ 16259685

The following data is based on the product molecular weight 325.41.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.07 mL	15.37 mL	30.73 mL
5 mM	0.61 mL	3.07 mL	6.15 mL
10 mM	0.31 mL	1.54 mL	3.07 mL
50 mM	0.06 mL	0.31 mL	0.61 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 100 publications citing the usage of this product.

• Xie Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats. Psychopharmacology (Berl). 2010 PMID: 19847405
• Mabire Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 2005 PMID: 15771457
• Steckler Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 2005 PMID: 16043241
• Lavreysen JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 2004 PMID: 15555631

Product Documents for JNJ 16259685