CGP-78608 

CGP 78608 is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC₅₀ of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC₅₀ in the low nM range (26.3 nM). CGP 78608 has anticonvulsant activities^[1][2].

CGP-78608 通过 GluN1 和 GluN3A 激动剂结合域 (ABD) 位点之间的亚基间变构效应降低 GluN1/GluN3A 受体的甘氨酸敏感性^[2]。
CGP 78608 减少或消除氨依赖性 cGMP 合成，这是氨神经毒性的致病因素^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CGP-78608 在小鼠电击诱发的惊厥试验中腹腔注射后表现出强效的抗惊厥作用^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

378.12

C₁₁H₁₃BrN₃O₅P

206648-13-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Catarzi D, et al. Competitive Gly/NMDA receptor antagonists. Curr Top Med Chem. 2006;6(8):809-21.  [Content Brief]

  [2]. Grand T, et al. Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat Commun. 2018 Nov 13;9(1):4769.  [Content Brief]

  [3]. Hilgier W, et al. A novel glycine site-specific N-methyl-D-aspartate receptor antagonist prevents activation of the NMDA/NO/CGMP pathway by ammonia. Brain Res. 2004 Jul 23;1015(1-2):186-8.  [Content Brief]