| 货号 | 11986-25mg |
| 描述 | The metabotropic glutamate receptor 2 (mGluR2) is a Gi/o-coupled receptor which is expressed on presynaptic nerve terminals and modulates the release of neurotransmitters like glutamate and GABA.1 Biphenylindanone A (BINA) is a positive allosteric modulator of mGluR2, stimulating the human and rat receptors with EC50 values of 33.2 and 96 nM, respectively.2 It has no effect on glutamate-induced activation of other mGluR types.2 BINA can be used on cells, tissues, or animals.2,3 Because of its selectivity for mGluR2, robust in vivo activity, and brain penetrance, BINA can be used to elucidate the role of mGluR2 in such diverse processes as psychosis, schizophrenia, and drug addiction.4,5,6 |
| 别名 | BINA;MRLSD 230; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tresadern, G.,Cid, J.M.,Macdonald, G.J., et al. Scaffold hopping from pyridones to imidazo[1,2-α]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor. Bioorganic & Medicinal Chemistry Letters 20(1), 175-179 (2010). 2.Galici, R.,Jones, C.K.,Hemstapat, K., et al. Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. Journal of Pharmacology and Experimental Therapeutics 318(1), 173-185 (2006). 3.Dhanya, R.P.,Sidique, S.,Sheffler, D.J., et al. Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats. Journal of Medicinal Chemistry 54(1), 342-353 (2011). 4.Benneyworth, M.A.,Xiang, Z.,Smith, R.L., et al. A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. Molecular Pharmacology 72(2), 477-484 (2007). 5.Hackler, E.A.,Byun, N.E.,Jones, C.K., et al. Selective potentiation of the metabotropic glutamate receptor subtype 2 blocks phencyclidine-induced hyperlocomotion and brain activation. Neuroscience 168, 209-218 (2010). 6.Jin, X.,Semenova, S.,Yang, L., et al. The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats. Neuropsychopharmacology 35(10), 2021-2036 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 454.6 |
| 分子式 | C30H30O4 |
| CAS号 | 866823-73-6 |
| 稳定性 | ≥ 2 years |
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