- Alomone Labs Ro 25-6981 maleate inhibits NMDA receptor channels expressed in Xenopus oocytes.A. Representative time course of NR1/NR2A currents, elicited by transient stimulations with 100 µM glutamate + 100 µM glycine every 50 sec, while membrane potential was held at -80 mV. 3 min application (indicated by bar) of 100 µM Ro 25-6981 maleate (#R-180) significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control and of 100 µM Ro 25-6981 maleate (as indicated).
Ro 25-6981 maleate is a highly potent and selective antagonist of GluN2B-containing NMDA receptors. The compound is an activity dependent antagonist of the receptor and demonstrates 5000 times fold selectivity for NR2B-containing receptors over NR2A-containing receptors1. Ro 25-6981 demonstrates an IC50 value of 0.009 µM towards NR2B-containing receptors and an IC50 of 52 µM towards NR2A-containing receptors1.
Ro 25-6981 protects cultured cortical neurons against glutamate toxicity and has anti-depressant and anti-inflammatory effects. It can suppress ischemic brain injury by regulating autophagy-related proteins during ischemia1,2.
NMDA receptors are composed of NR1 including eight different splice variants and NR2A-D. They are activated by the co-agonists glutamate and glycine1,2.