JNJ 16259685

Pricing Availability   Qty
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)
Datasheet
Citations (10)
Reviews
Literature (5)

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.

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 for JNJ 16259685

Certificate of Analysis / Product Datasheet
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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


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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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Metabotropic Glutamate Receptors Scientific Review

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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