Ro 67-7476 是一种有效的 mGluR1 正变构调节剂，可在表达大鼠 mGluR1a 的 HEK293 细胞中增强谷氨酸诱导的钙释放，EC50 为 60.1 nM。 Ro 67-7476 是一种有效的 P-ERK1/2 激动剂，在没有外源添加的谷氨酸 (EC50=163.3 nM) 的情况下激活 ERK1/2 磷酸化。
| Cas No. | 298690-60-5 |
| 化学名 | (S)-2-(4-fluorophenyl)-1-tosylpyrrolidine |
| Canonical SMILES | FC1=CC=C(C=C1)[C@H](CCC2)N2S(=O)(C3=CC=C(C)C=C3)=O |
| 分子式 | C17H18FNO2S |
| 分子量 | 319.39 |
| 溶解度 | DMSO: 30 mg/ml |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. Displays no activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM.target: mGlu1 EC 50: 60.1 nM(1) Ro 67-7476 (10 μM) can directly block the GIRK channel (to 67 ± 2% of control). (2) Ro 67-7476 enhance the glutamate-induced current in all chimeric receptors containing the transmembrane (TM) region of rmGlu1a (R1, R1-R5N, R1-R5C, and R5-R1TM) but not in those containing the TM region of rmGlu5a (R5, R5-R1N, R5-R1C, and R1-R5TM.(3) The application of Ro 67-7476 (3 μM) produced no effect alone but resulted in a marked potentiation of the mGlu1 EPSC amplitude. References:
[1]. Hemstapat K 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. Mol Pharmacol. 2006 Aug, 70(2), 616-26
[2]. Knoflach F et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7. |
