Overview
- Acker, T.M. et al. (2011) Mol. Pharmacol. 80, 782.
Alomone Labs DQP-1105 inhibits NMDA receptor channels expressed in Xenopus oocytes.A. Representative time course of NR1/NR2C currents, elicited by transient stimulations with 50 µM glutamate + 50 µM glycine every 50 sec, while membrane potential was held at -80 mV, and reversibly inhibited by 2 µM and 20 µM DQP-1105 (#D-210). B. Superimposed current traces from the recording shown in A, following application of control, 2 µM and 20 µM DQP-1105. Transient stimulation is indicated by an arrow.
DQP-1105 is a potent and noncompetitive antagonist of GluN2D and GluN2C-containing N-methyl-d-aspartate (NMDA) receptors displaying IC50 values of 2.7 µM and 8.5 µM towards NR2D and NR2C-containing receptors, respectively1. DQP-1105 exhibits significant selectivity towards these receptors over NR2B and NR2A-containing receptors. DQP-105 inhibits the pregating step without changing the stability of the open pore conformation.
NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. They play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. NMDA receptors mediate physiological functions such as learning and memory formation, glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease2.
