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JNJ-16259685

Chemical Structure : JNJ-16259685

CAS No.: 409345-29-5

JNJ-16259685 (JNJ16259685)

Catalog No.: PC-42138Not For Human Use, Lab Use Only.

JNJ-16259685 (JNJ16259685) is a highly potent, selective, non-competitive and centrally active mGluR1 antagonist with Ki of 0.34 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JNJ-16259685 (JNJ16259685) is a highly potent, selective, non-competitive and centrally active mGluR1 antagonist with Ki of 0.34 nM.
JNJ-16259685 shows no agonist, antagonist or PAM activity toward rat mGlu2/3/4/6 receptors (IC50>10 uM) and does not bind to AMPA, NMDA receptor and other neurotransmitter receptors.
JNJ-16259685 inhibits glutamate-induced Ca2+ mobilization for rat and human mGluR1 with IC50 of 3.24 and 1.21 nM, inhibits glutamate-mediated inositol phosphate production with IC50 of 1.73 nM.
JNJ-16259685 attenuates drug context-induced reinstatement of cocaine seeking in rats.

Physicochemical Properties

M.Wt 325.4015
Formula C20H23NO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Methanone, (3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)(cis-4-methoxycyclohexyl)-

References

1. Lavreysen H, et al. Neuropharmacology. 2004 Dec;47(7):961-72.

2. Mabire D, et al. J Med Chem. 2005 Mar 24;48(6):2134-53.

3. Xie X, et al. Psychopharmacology (Berl). 2010 Jan;208(1):1-11.

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