Product overview

Name JNJ 16259685
Description Potent, selective, non-competitive mGlu1 antagonist
Purity >98%
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Biological Data

Biological description

Potent, selective and non-competitive mGlu1 receptor antagonist (Ki = 0.34 nM at mGlu1a). 

Displays no activity at mGlu2, mGlu3, mGlu4, mGlu6, NMDA or AMPA receptors (IC50 = >10 μM). Blood-brain barrier permeable.

Inhibits glutamate-induced Ca2+ mobilization (IC50 = 3.24 nM at recombinant rat mGlu1a receptor).

Decreases drug and alcohol addiction behaviours in rodents. 

Solubility & Handling

Storage instructions +4°C
Solubility overview Soluble in ethanol (100mM) and in DMSO (25mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Molecular Weight 325.41
Chemical structure JNJ 16259685  [409345-29-5] Chemical Structure
Molecular Formula C20H23NO3
CAS Number 409345-29-5
PubChem identifier 11313361
SMILES COC1CCC(CC1)C(=O)C2=CC3=CC4=C(N=C3C=C2)OCCC4
InChi InChI=1S/C20H23NO3/c1-23-17-7-4-13(5-8-17)19(22)14-6-9-18-16(11-14)12-15-3-2-10-24-20(15)21-18/h6,9,11-13,17H,2-5,7-8,10H2,1H3
InChiKey QOTAQTRFJWLFCR-UHFFFAOYSA-N
Appearance Off-white solid

References for JNJ 16259685

References are publications that support the biological activity of the product
  • mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions.

    Lum EN et al (2014) Neuropharmacology 79 : 679-87.
  • Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats.

    Xie X et al (2010) Psychopharmacology (Berl) 208(1) : 1-11.
  • Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.

    Mabire D et al (2005) J Med Chem 48(6) : 2134-53.
  • JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist.

    Lavreysen H et al (2004) Neuropharmacology 47(7) : 961-72.
Publications
These publications cite the use of JNJ 16259685 purchased from Hello Bio:
  • Long-term synaptic depression triggers local biogenesis of autophagic vesicles in dendrites and requires autophagic degradation

    Kallergi et al. (2020) bioRxiv preprint : 1-46

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