Molecular structure of JNJ 16259685, CAS Number: 409345-29-5
JNJ 16259685 (CAS 409345-29-5)
See product citations (3)
Alternate Names:
(3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Application:
JNJ 16259685 is a non-compeitive antagonist at the mGluR-1
CAS Number:
409345-29-5
Purity:
≥98%
Molecular Weight:
325.4
Molecular Formula:
C20H23NO3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
JNJ 16259685 is a sub-nanomolar potent, non-competitive mGluR-1 antagonist (Ki=0.34nM). Inhibits glutamate-induced Ca2+ response at the human mGluR-1 (IC50=0.55nM). Selective over mGluR-5 (>400-fold). Displays no activity at mGluR-2, mGluR-3, mGluR-4, mGluR-6, AMPA or NMDA receptors (IC50 > 10 muM). JNJ 16259685 is an inhibitor of mGluR-1a and mGluR-1b.
JNJ 16259685 (CAS 409345-29-5) References
- Regulation of motivation to self-administer ethanol by mGluR5 in alcohol-preferring (P) rats. | Besheer, J., et al. 2008. Alcohol Clin Exp Res. 32: 209-21. PMID: 18162077
- Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. | Shin, JH., et al. 2008. Proc Natl Acad Sci U S A. 105: 746-50. PMID: 18174329
- Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. | Salah, A. and Perkins, KL. 2008. Neuropharmacology. 55: 47-54. PMID: 18538357
- Optical measurement of mGluR1 conformational changes reveals fast activation, slow deactivation, and sensitization. | Marcaggi, P., et al. 2009. Proc Natl Acad Sci U S A. 106: 11388-93. PMID: 19549872
- Role of the metabotropic glutamate receptor subtype 1 in the harmaline-induced tremor in rats. | Kolasiewicz, W., et al. 2009. J Neural Transm (Vienna). 116: 1059-63. PMID: 19551466
- Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain. | Fujinaga, M., et al. 2011. Bioorg Med Chem. 19: 102-10. PMID: 21172734
- Metabotropic glutamate receptors: their therapeutic potential in anxiety. | Spooren, W., et al. 2010. Curr Top Behav Neurosci. 2: 391-413. PMID: 21309118
- Estrogen receptors and type 1 metabotropic glutamate receptors are interdependent in protecting cortical neurons against β-amyloid toxicity. | Spampinato, SF., et al. 2012. Mol Pharmacol. 81: 12-20. PMID: 21984253
- A late phase of LTD in cultured cerebellar Purkinje cells requires persistent dynamin-mediated endocytosis. | Linden, DJ. 2012. J Neurophysiol. 107: 448-54. PMID: 22049330
- Binge alcohol drinking by mice requires intact group 1 metabotropic glutamate receptor signaling within the central nucleus of the amygdala. | Cozzoli, DK., et al. 2014. Neuropsychopharmacology. 39: 435-44. PMID: 23966068
- mGluR1 within the nucleus accumbens regulates alcohol intake in mice under limited-access conditions. | Lum, EN., et al. 2014. Neuropharmacology. 79: 679-87. PMID: 24467847
- Protein Kinase C Epsilon Activity in the Nucleus Accumbens and Central Nucleus of the Amygdala Mediates Binge Alcohol Consumption. | Cozzoli, DK., et al. 2016. Biol Psychiatry. 79: 443-51. PMID: 25861702
- Effects of Group I metabotropic glutamate receptor antagonists on sensitivity to reinforcer magnitude and delayed reinforcement in a delay-discounting task in rats: Contribution of delay presentation order. | Yates, JR., et al. 2017. Behav Brain Res. 322: 29-33. PMID: 28088471
Inhibitor of:
mGluR-1a, and mGluR-1b.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
JNJ 16259685, 5 mg | sc-202670 | 5 mg | $104.00 | |||
JNJ 16259685, 25 mg | sc-202670A | 25 mg | $422.00 |