L-AP4 (L-APB) monohydrate 是一种有效的、代谢型谷氨酸受体 (mGluR) 的特异性激动剂，其对 mGlu₄, mGlu₈, mGlu₆ 和 mGlu₇ 受体的 EC₅₀ 值分别为 0.13, 0.29, 1.0, 249 μM。

L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC 50 s of 0.13, 0.29, 1.0, 249 μM for mGlu 4 , mGlu 8 , mGlu 6 and mGlu 7 receptors, respectively.

Solid

mGlu4 0.13 μM (EC50) mGlu8 0.29

L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunction.
Intrathecal injection of 30 μg of L-AP4 does not significantly alter the paw withdrawal latency in these normal rats.
Topical application of 5 to 50 μM L-AP4 to the spinal cord significantly inhibited the evoked response of neurons to touch, pressure, pinch, and von Frey filaments in a concentration-dependent fashion.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[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.