Overview
- Schoepp, D.D. et al. (1991) Eur. J. Pharmacol. 203, 237.
- Chen, P.E. et al. (2005) Mol. Pharmacol. 67, 1470.
Alomone Labs (RS)-(Tetrazol-5-yl)glycine activates NMDA receptors expressed in Xenopus oocytes.A. Representative time course of NR1/NR2A current activation by 3.5 min applications of 0.4 μM, 2 μM and 10 μM (RS)-(Tetrazol-5-yl)glycine (#T-205), as indicated, in the presence of 50 μM glycine (top dotted line), at membrane holding potential of -60 mV. B.Representative current traces of NR1/NR2A, elicited by transient stimulations with control and with 10 µM and 25 µM (RS)-(Tetrazol-5-yl)glycine (as indicated), in the presence of 10 μM glycine, while membrane potential was held at -60 mV.
(RS)-(Tetrazol-5-yl)glycine is a synthetic compound that acts as highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist. The compound is significantly more potent than NMDA or glutamate. When given to neonatal rats, (RS)-(Tetrazol-5-yl) glycine was found to be highly potent convulsant1.
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. They also mediate physiological functions such as learning and memory formation and participate in glutamate excitotoxicity2.
(RS)-(Tetrazol-5-yl)glycine inhibits [3H]glutamate binding to rat brain NMDA receptors with an IC50 value of 36 nM1. in vitro studies show that (RS)-(Tetrazol-5-yl)glycine can activate NR1/NR2A NMDA receptors with an EC50 value of 1.77 µM3.
