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Images JNJ 16259685 product vial image | Hello Bio
JNJ 16259685 product vial image | Hello Bio 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.
Chemical Data Chemical name (3,4-Dihydro-2H -pyrano[2,3-b ]quinolin-7-yl)-(cis -4-methoxycyclohexyl)-methanone
Chemical structure
Molecular Formula C20 H23 NO3
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:
SCA44- and SCAR13-associated GRM1 mutations affect metabotropic glutamate receptor 1 function through distinct mechanisms Hellyer et al (2023) bioRxiv https://www.biorxiv.org/content/10.1101/2023.07.05.545810v1.abstract
Dendritic autophagy degrades postsynaptic proteins and is required for long-term synaptic depression in mice Kallergi E et al (2022) Nat Commun 13(1) : 680 Bidirectional regulation of synaptic SUMOylation by Group 1 metabotropic glutamate receptors Pronot M et al (2022) Cell Mol Life Sci 79(7) : 378 Long-term synaptic depression triggers local biogenesis of autophagic vesicles in dendrites and requires autophagic degradation Kallergi et al. (2020) bioRxiv preprint : 1-46
Potent, selective, non-competitive mGlu1 antagonist
![JNJ 16259685 [409345-29-5] Chemical Structure](https://cdn.hellobio.com/media/catalog/product//h/b/hb0348.png "JNJ 16259685 [409345-29-5]")
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