Overview
- Edman, S. et al. (2012) Neuropharmacology 63, 441.
- Bettini, E. et al. (2010) J. Pharmacol. Exp. Ther. 335, 636.
Alomone Labs TCN 201 inhibits NMDA receptor channels expressed in Xenopus oocytes.A. Time course of NR1/NR2A currents, elicited by transient stimulations with 100 µM glutamate and 100 µM glycine every 100 sec, while membrane potential was held at -80 mV. Application of 1 µM TCN 201 (#T-190) for 5 min (green), significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control (black) and of 1 µM TCN 201 (green).
- Edman, S. et al. (2012) Neuropharmacology 63, 441.
- Black, S.A. et al. (2014) Front. Cell. Dev. Biol. 2, 45.
TCN 201, a sulphonamide derivative, acts as a selective and potent NMDA (methyl-D-aspartate) receptor antagonist. This compound displays a high selectivity for GluN1/GluN2A-containing NMDAR receptors over GluN1/GluN2B containing receptors and acts in a non-competitive manner. The degree of its antagonism is dependent on the concentration of the GluN1-site co-agonist, glycine or D-serine, and is independent of the glutamate concentration1. TCN 201 can be used to estimate and to clarify the contribution of NMDAR subunit and its composition and function.
NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. NMDAR plays 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. They play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease2.
TCN 201 (#T-190) is a highly pure, synthetic, and biologically active compound.
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