| 货号 | 2333/50 |
| 别名 | (3,4-Dihydro-2H-pyrano[2,3-b]quinol |
| 供应商 | Tocris |
| 生物活性 | Sub-nanomolar potent, non-competitive mGlu1 antagonist (Ki = 0.34 nM). Inhibits glutamate-induced Ca2+ response at the human mGlu1 receptor with an IC50 value of 0.55 nM. Selective over mGlu5 (> 400-fold) and displays no activity at mGlu2, mGlu3, mGlu4, mGlu6, AMPA or NMDA receptors (IC50 > 10 μM). Centrally active following systemic administration. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 325.41 |
| 分子式 | C20H23NO3 |
| 可溶性/溶解性 | Soluble to 100 mM in ethanol and to 25 mM in DMSO |
| CAS号 | 409345-29-5 |
| 参考文献 | Xieet al (2010) Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats. Psychopharmacology (Berl). 208 1. PMID: 19847405. Mabireet al (2005) Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 48 2134. PMID: 15771457. Steckleret al (2005) Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 164 52. PMID: 16043241. Lavreysenet al (2004) JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 47 961. PMID: 15555631. |