| Description | L-APB is an effective and specific agonist for the group III mGluRs (EC50s: 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively). |
| In vivo | L-APB(5 to 30 μg; intrathecal injection) obviously enhances the paw withdrawal threshold in response to the application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. The maximal effect of L-APB appears within 45 min and gradually subsided in 120 min following intrathecal administration. Paw withdrawal threshold in response to the application of von Frey filaments before spinal nerve ligation is 22.6±2.4 g. The mechanical threshold decreases significantly (2.3±0.5 g, P<0.05) within 10 days after nerve ligation and remains stable for at least 8 weeks [2]. |
| Target activity | mGlu7:249 μM (EC50), mGlu4:0.13 μM (EC50), mGlu6:1.0 μM (EC50), mGlu8:0.29 μM (EC50) |
| Synonyms | L-APB, L-AP 4 |
| molecular weight | 183.1 |
| Molecular formula | C4H10NO5P |
| CAS | 23052-81-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 50 mg/mL (273.07 mM), Sonication is recommended. |
| References | 1. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989. 2. Chen SR, et al. Distinct roles of group III metabotropic glutamate receptors in control of nociception and dorsal horn neurons in normal and nerve-injured Rats. J Pharmacol Exp Ther. 2005 Jan;312(1):120-6. |