JNJ 16259685

(HB0348)

Product overview

  • Name
    JNJ 16259685
  • Short description
    Potent, selective, non-competitive mGlu1 antagonist
  • 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. 

  • Biological action
    Antagonist
  • Purity
    >98%
  • Citations

Properties

  • 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]
  • 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

Storing and Using Your Product

  • 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.

References for JNJ 16259685

  • JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist.

    Lavreysen H et al (2004) Neuropharmacology 47(7) : 961-72.
    PubMedID: 15555631
  • 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.
    PubMedID: 19847405
  • mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions.

    Lum EN et al (2014) Neuropharmacology 79 : 679-87.
    PubMedID: 24467847
  • 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.
    PubMedID: 15771457