Biological Activity |
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 uM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively. IC50 & Target: EC50: 0.13 uM (mGlu4), 0.29 uM (mGlu8), 1.0 uM (mGlu6), 249 uM (mGlu7)[1]. In Vivo: Paw withdrawal threshold in response to 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. Intrathecal injection of 5 to 30 ug of L-APB significantly increases the paw withdrawal threshold in response to 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[2]. |