An antagonist of mGluR1a
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JNJ-16259685

Item No. 35377

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)(cis-4-methoxycyclohexyl)-methanone
CAS Number
409345-29-5
Molecular Formula
C20H23NO3
Formula Weight
325.4
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: slightly solubleDMSO: slightly soluble
SMILES
CO[C@@H]1CC[C@H](C(C2=CC(C=C(CCCO3)C3=N4)=C4C=C2)=O)CC1
InChi Code
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/t13-,17+
InChi Key
QOTAQTRFJWLFCR-XFHMXUHZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $124

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    10 mg

    $229

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    25 mg

    $523

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    Product Description

    JNJ-16259685 is an antagonist of metabotropic glutamate receptor 1a (mGluR1a; Ki = 0.34 nM in CHO(dHFr-) cell membranes expressing the rat receptor).1 It is selective for mGluR1a over mGluR5, -2, -3, -4, and -6, as well as a panel of neurotransmitter receptors, ion channels, and transporters, at 10 µM. JNJ-16259685 inhibits glutamate-induced inositol phosphate accumulation in primary rat cerebellar neurons with an IC50 value of 1.73 nM. It increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, when administered at doses of 2.5, 5, or 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lavreysen, H., Wouters, R., Bischoff, F., et al. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 47(7), 961-972 (2004).

    2. Steckler, T., Lavreysen, H., Oliveira, A.M., et al. Effects of mGlu1 receptor blockade on anxiety-related behaviour in the rat lick suppression test. Psychopharmacology (Berl.) 179(1), 198-206 (2005).