| Description | CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of mGluR1b |
| In vitro | CPCCOEt 在人类mGluR1b (hmGluR1b) 中，选择性抑制了由谷氨酸诱导的细胞内钙浓度增加，表观IC50为6.5 μM，同时在hmGluR2、-4a、-5a、-7b以及-8a上表现出至高100 μM也无激动或拮抗活性。此外，在hmGluR5a的同源位置引入Thr815和Ala818后，由CPCCOEt 完全抑制(IC50 = 6.6 μM)[1]。 |
| In vivo | 在大鼠小脑片上进行的浦肯野细胞全细胞电压记录显示，CPCCOEt在阻断mGlu1受体的浓度(100 μM)[2]下，增强了攀爬纤维反应。 |
| Target activity | mGluR1b (human):6.5 μM |
| molecular weight | 247.25 |
| Molecular formula | C13H13NO4 |
| CAS | 179067-99-3 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90.0 mg/mL (364.0 mM), Sonication is recommended. |
| References | 1. Litschig S, et al. CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. Mol Pharmacol. 1999 Mar;55(3):453-61. 2. Fukunaga I, Yeo CH, Batchelor AM. The mGlu1 antagonist CPCCOEt enhances the climbing fibre response in Purkinje neurones independently of glutamate receptors. Neuropharmacology. 2007 Feb;52(2):450-8. |