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Submit ReviewJNJ 16259685
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% (HPLC)
Biological Activity for JNJ 16259685
JNJ 16259685 is a 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 for JNJ 16259685
JNJ 16259685 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JNJ 16259685
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JNJ 16259685
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 32.54 | 100 | |
| DMSO | 8.14 | 25 |
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 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 for JNJ 16259685
References for JNJ 16259685
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for JNJ 16259685, please let us know.
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Keywords: JNJ 16259685, JNJ 16259685 supplier, potent, mGlu1, mGluR1-selective, non-competitive, antagonists, Group, I, Receptors, Glutamate, Metabotropic, JNJ16259685, (Metabotropic), 2333, Tocris Bioscience
10 Citations for JNJ 16259685
Citations are publications that use Tocris products. Selected citations for JNJ 16259685 include:
Rizwan et al (2016) Long-Term Potentiation at the Mossy Fiber-Granule Cell Relay Invokes Postsynaptic Second-Messenger Regulation of Kv4 Channels. J Neurosci 36 11196 PMID: 27807163
Lum et al (2014) mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions. Neuropharmacology 79 679 PMID: 24467847
Loweth et al (2014) Synaptic depression via mGluR1 positive allosteric modulation suppresses cue-induced cocaine craving. Nat Neurosci 17 73 PMID: 24270186
Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252 PMID: 26269634
Shin et al (2008) Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. Aquat Toxicol 105 746 PMID: 18174329
Zheng and Raman (2011) Prolonged postinhibitory rebound firing in the cerebellar nuclei mediated by group I metabotropic glutamate receptor potentiation of L-type calcium currents. J Neurosci 31 10283 PMID: 21753005
Johansson et al (2015) Activation of a temporal memory in purkinje cells by the mGluR7 receptor. Cell Rep. 13 1741 PMID: 26655894
Jensen (2013) Effects of a metabotropic glutamate 1 receptor antagonist on light responses of retinal ganglion cells in a rat model of retinitis pigmentosa. PLoS One 8 e79126 PMID: 24205371
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
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? Please let us know.
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Literature in this Area
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Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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