Overview
- Evans, R.H. et al. (1982) Br. J. Pharmac. 75, 65.
Alomone Labs DL-AP7 inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes.A. Time course of NMDA currents elicited with 25 µM glutamate and 25 µM glycine, every 50 sec, while membrane potential was held at -80 mV. 200 µM DL-AP7 (#D-200), applied for 3 min as indicated, inhibited current amplitude. Note: Control was done with 1:500 1M NaOH for 3 min prior to DL-AP7 application. B. Superimposed current traces taken from experiment in A.
DL-AP7 (APH) is a competitive N-methyl-D-aspartate (NMDA) receptor antagonist. The mechanism of action of DL-AP7 is to compete with agonists over the recognition site of the NMDA receptor in order to prevent the receptor’s activation.
Several studies have shown that NMDA receptor blockade evokes changes of systemic pressure; DL-AP7 administration may increase blood pressure. This finding indicates that peripherally, NMDA receptors may take part in regulating the cardiovascular system1,2.
NMDA receptors play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. NMDA receptors mediate several physiological functions including learning and memory formation, they play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease3.
