JNJ 16259685

Name: JNJ 16259685
Brand: Tocris Bioscience
SKU: 2333

Catalog # 2333 | Tocris Bioscience a Bio-Techne Brand

Citations (10)

COA / SDS

Highly potent, mGlu1-selective non-competitive antagonist

Key Product Details

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)
Molecular Weight:	325.41

View Full Technical Details for JNJ 16259685

Technical Data
Citations (10) / Reviews

Biological Activity for JNJ 16259685

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.

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 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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References for JNJ 16259685

References are publications that support the biological activity of the 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

Citations for JNJ 16259685 (10)

Showing 1 - 10 of 10 citations Showing All

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Citations are publications that use Bio-Techne 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
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
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
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
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
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

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