Overview
- Volkmann, R.A. et al. (2016) PLoS ONE 11, e0148129.
- Alomone Labs MPX-004 inhibits NMDA receptor channels expressed in Xenopus oocytes.A. Time course of NR1/NR2A currents, elicited by transient stimulations with 200 µM glutamate and 200 µM glycine every 100 sec, while membrane potential was held at -80 mV. 100 nM MPX-004 (#M-280), applied for 7 min (bar), significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control and of 100 nM MPX-004 (as indicated).
- Volkmann, R.A. et al. (2016) PLoS ONE 11, e0148129.
- Cercato, M.C. et al. (2017) Front. Behav. Neurosci. 10, 242.
MPX-004 is a synthetic compound that acts as a potent and selective GluN2A-containing NMDA receptor antagonist with an IC50 value of 79 nM in HEK cells1.
MPX-004 is a pyrazine-containing antagonist with optimal halogen substituents on the phenylsulfonamide aryl ring. It is used as a pharmacological tool for studying the physiology of NMDA receptors containing the GluN2A subunit1.
NMDA receptors are heterotetramers composed by 2 GluN1 obligatory subunits and 2 GluN2 (A-D) or GluN3 (A-B) regulatory subunits. GluN2A is the most abundant subunit in the mammalian CNS. Physiological and genetic evidence show that GluN2A-containing receptors are involved in autism, schizophrenia, childhood epilepsy and neurodevelopmental disorders such as Rett Syndrome1,2.
MPX-004 (#M-280) is a highly pure, synthetic, and biologically active compound.
Applications
Citations
- Mouse primary hippocampal neurons.
Chan, K. et al. (2020) Nat. Commun. 11, 1403.