JNJ 16259685

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Cat.No. 2333 - JNJ 16259685 | C20H23NO3 | CAS No. 409345-29-5
Description: Extremely 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% (HPLC)
Datasheet
Citations (5)
Literature

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.

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Technical Data

M. Wt 325.41
Formula C20H23NO3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 409345-29-5
PubChem ID 11313361
InChI Key QOTAQTRFJWLFCR-UHFFFAOYSA-N
Smiles O=[C@@]([C@@H]4CC[C@H](OC)CC4)C(C=C3)=CC1=C3N=C(OCCC2)C2=C1

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.

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

References

References are publications that support the products' biological activity.

Lavreysen et al (2004) JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 47 961 PMID: 15555631

Mabire et 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

Steckler et al (2005) Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 164 52 PMID: 16043241

Xie et 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


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Keywords: JNJ 16259685, supplier, potent, mGlu1, mGluR1-selective, non-competitive, antagonists, Group, I, Receptors, Glutamate, Metabotropic, JNJ16259685, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience

5 Citations for JNJ 16259685

Citations are publications that use Tocris products. Selected citations for JNJ 16259685 include:

Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252 PMID: 26269634

Johansson et al (2015) Activation of a temporal memory in purkinje cells by the mGluR7 receptor. Cell Rep. 13 1741 PMID: 26655894

Hildebrand et al (2009) Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines. J Neurosci 29 9668 PMID: 19657020

Shin et al (2008) Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. Aquat Toxicol 105 746 PMID: 18174329

Fukunaga et al (2007) Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices. Br J Pharmacol 151 870 PMID: 17502847


Do you know of a great paper that uses JNJ 16259685 from Tocris? If so please let us know.

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