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KI1087Biphenylindanone AQuoteQuote

Chemical Characteristic

Product NameBiphenylindanone A
CAS No.866823-73-6
Molecular Weight 454.56
FormulaC30H30O4
Chemical Name(S)-3'-(((2-cyclopentyl-6,7-dimethyl-1-oxo-2,3-dihydro-1H-inden-5-yl)oxy)methyl)-[1,1'-biphenyl]-4-carboxylic acid
Smilesc1(ccc(cc1)C(=O)O)c1cc(ccc1)COc1cc2CC(C(=O)c2c(c1C)C)C1CCCC1
Chemical Structure

Biological activities

Biphenyl-indanone A is a selective metabotropic glutamate receptor (mGluR)2 positive allosteric modulator. Biphenyl-indanone A produces a maximal potentiation of approximately 3.5-fold in CHO cells, with an EC50 value of 33.2 nM. Biphenyl-indanone A also produces a concentration dependent potentiation of the glutamate response of HEK293A cells expressing rmGluR2/Gqi5 with a maximal potentiation of approximately 6-fold and an EC50 value of 98 nM.[1] Biphenyl-indanone A attenuates serotonin-induced increased in spontaneous excitatory postsynaptic currents in the mPFC, mimicking the effect of the mGlu2/3 receptor agonist(DCG-IV). In addition, biphenyl-indanone A reduces (-)DOB-induced head twitch behavior and Fos expression in mPFC. [2] Biphenyl-indanone A potentiates agonist-induced inhibition of excitatory synaptic transmission at the medial perforant path-dentate gyrus synapse in rat hippocampal slices. Biphenyl-indanone A decreases stress-induced hyperthermia in mice. [1]

Protocols

Biphenyl-indanone A is dissolved in 100% DMSO and then serially diluted into assay buffer containing 0.1% bovine serum albumin for a 5?stock in 0.5% DMSO. [1]

References

[1] Galici R, et al. Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J Pharmacol Exp Ther. 2006, 318(1): 173-185.
[2] Benneyworth MA, et al. A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. Mol Pharmacol. 2007, 72(2): 477-484.

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