| 货号 | 11992-1mg |
| 描述 | Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).1,2 While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.1 Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).3 Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivoandin vitro(EC50 = 95 nM).1,4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Knoflach, F.,Mutel, V.,Jolidon, S., et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site. Proceedings of the National Academy of Sciences of the United States of America 98(23), 13402-13407 (2001). 2.Hemstapat, K.,de Paulis, T.,Chen, Y., et al. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Molecular Pharmacology 70(2), 616-626 (2006). 3.Sheffler, D.J., and Conn, P.J. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology 55(4), 419-427 (2008). 4.Salt, T.E.,Jones, H.E.,Andolina, I.M., et al. Potentiation of sensory responses in ventrobasal thalamus in vivo via selective modulation of mGlu1 receptors with a positive allosteric modulator. Neuropharmacology 62(4), 1695-1699 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | 22 |
| 纯度 | ≥98% |
| 计算分子量 | 325.4 |
| 分子式 | C19H19NO4 |
| CAS号 | 302841-89-0 |
| 稳定性 | ≥ 2 years |
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