Chemical Name: (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
Compound Libraries
JNJ 16259685 is also offered as part of the
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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.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
8.14
25
ethanol
32.54
100
Preparing Stock Solutions
The following data is based on the product molecular weight 325.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Lavreysenet al (2004) JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 47 961 PMID: 15555631
Mabireet al (2005) Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 48 2134 PMID: 15771457
Steckleret al (2005) Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 164 52 PMID: 16043241
Xieet al (2010) Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats. Psychopharmacology (Berl). 208 1 PMID: 19847405
Keywords: JNJ 16259685, supplier, potent, mGlu1, mGluR1-selective, non-competitive, antagonists, Group, I, Receptors, Glutamate, Metabotropic, JNJ16259685, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience