5.04479
JNJ 16259685 - CAS 409345-29-5 - Calbiochem
Synonym(s):
JNJ 16259685 - CAS 409345-29-5 - Calbiochem, (3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
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About This Item
assay
≥98% (TLC)
Quality Level
form
solid
potency
0.55 nM IC50
0.34 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white to off-white
solubility
DMSO: 25 mM
storage temp.
2-8°C
General description
An extremely potent, non-competitive antagonist for mGlu receptor subtype 1 (Ki = 0.34 nM; IC50 = 0.55 nM). 400-fold more selective for mGlu1 than for mGlu5 and no interaction with mGlu2, mGlu3, mGlu4, mGlu6, AMPA or NMDA receptors (IC50 >10 µM). Centrally active following systemic administration. Widely used for studying substance abuse, learning and memory, and neural plasticity.
Biochem/physiol Actions
Primary Target
mGlu₁
mGlu₁
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lavreysen, H., et al. 2004. Neuropharmacology.47, 961.
Steckler, T., et al. 2005. Psychopharmacology.179, 198.
Steckler, T., et al. 2005. Behav. Brain. Res.164, 52.
Mabire, D., et al. 2005. J. Med. Chem.48, 2134.
Fukunaga, I., et al. 2007. Br. J. Pharmacol.151, 870.
Knopfel, T., et al. 2007. Br. J. Pharmacol.151, 723.
Achat-Mendes, C., et al. 2012. J. Pharmacol. Exp. Ther.343, 214.
Steckler, T., et al. 2005. Psychopharmacology.179, 198.
Steckler, T., et al. 2005. Behav. Brain. Res.164, 52.
Mabire, D., et al. 2005. J. Med. Chem.48, 2134.
Fukunaga, I., et al. 2007. Br. J. Pharmacol.151, 870.
Knopfel, T., et al. 2007. Br. J. Pharmacol.151, 723.
Achat-Mendes, C., et al. 2012. J. Pharmacol. Exp. Ther.343, 214.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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