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. |
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](https://hellobio.com/media/catalog/product//h/b/hb0348.png "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 |
| Appearance | Off-white solid |
References for JNJ 16259685
References are publications that support the biological activity of the product
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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:
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Long-term synaptic depression triggers local biogenesis of autophagic vesicles in dendrites and requires autophagic degradation
Kallergi et al. (2020) bioRxiv preprint : 1-46
Technical guides
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