| 货号 | 13852-50mg |
| 描述 | Metabotropic glutamate receptors (mGluR1-8) are G protein-coupled receptors that function to modulate brain excitatory signaling via presynaptic, postsynaptic, and glial mechanisms.1 DL-AP3 is a competitive mGluR1 antagonist that demonstrates a Ki value of 298 μM and an IC50 value of 1mM for rat mGluR1α when challenged with glutamate.2 DL-AP3 can antagonize excitatory amino acid-induced phosphoinositide hydrolysis, induce Ca2+ mobilization in rat hippocampal slices, and inhibit phosphoserine phosphatase in rat brain cortex.1,3 At concentrations from 10-300 μM DL-AP3 has been used to characterize the role of mGluR in long-term potentiation in the hippocampus in a model of learning and memory, the release of glutamate in Parkinson’s disease, and the increased activity of mGluR implicated in fragile X syndrome.4,5,6 |
| 别名 | DL-2-Amino-3-Phosphonopropionic Acid;NSC 30078; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Schoepp, D.D. Unveiling the functions of presynaptic metabotropic glutamate receptors in the central nervous system. Journal of Pharmacology and Experimental Therapeutics 299(1), 12-20 (2001). 2.Schoepp, D.D.,Jane, D.E. and Monn, J.A. Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38(10), 1431-1476 (1999). 3.Hawkinson, J.E.,Acosta-Burruel, M. and Wood, P.L. The metabotropic glutamate receptor antagonist L-2-amino-3-phosphonopropionic acid inhibits phosphoserine phosphatase. European Journal of Pharmacology 307, 219-225 (1996). 4.Otani, S.,Connor, J.A. and Levy, W.B. Long-term potentiation and evidence for novel synaptic association in CA1 stratum oriens of rat hippocampus. Learning & Memory 2, 101-106 (1995). 5.Hao, L.,Ding, J.H. and Hu, G. Group I mGluR ligands fail to affect 6-hydroxydopamine-induced death and glutamate release of PC12 cells. Acta.Pharmacol.Sin. 24(7), 641-645 (2003). 6.Xu, Z.H.,Yang, Q.,Feng, B., et al. Group I mGluR antagonist rescues the deficit of D1- induced LTP in a mouse model of fragile X syndrome. Molecular Neurodegeneration 7(1), (2012). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 169.1 |
| 分子式 | C3H8NO5P |
| CAS号 | 5652-28-8 |
| 稳定性 | ≥ 2 years |
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