What drugs are NMDA receptor antagonists?
Commercially available NMDA-receptor antagonists include ketamine, dextromethorphan, memantine, and amantadine. The opioids methadone, dextropropoxyphene, and ketobemidone are also antagonists at the NMDA receptor.
What is NR2A?
NR2A – Glutamate receptor – Homo sapiens (Human) – NR2A gene & protein.
What is a non competitive NMDA receptor antagonist?
Competitive NMDA antagonists bind directly to the glutamate site of the NMDA receptor to inhibit the action of glutamate. Non-competitive antagonists block the NMDA-associated ion channel in a use-dependent manner. Other sites on the NMDA receptor susceptible to antagonism are the glycine site and the polyamine site.
What does NMDA antagonist treat?
NMDA (short for N-methyl-D-aspartate) receptor antagonists are a class of drugs that may help treat Alzheimer’s disease, which causes memory loss, brain damage, and, eventually, death.
What happens when you antagonize NMDA receptors?
NMDA receptor antagonists induce a state called dissociative anesthesia, marked by catalepsy, amnesia, and analgesia.
How are NMDAR antagonists different from NR2A antagonists?
This form of LTD is blocked by antagonists of NR2B-containing NMDARs but is not prevented by an antagonist of NR2A-containing NMDARs. In contrast, LTP and depotentiation show the opposite sensitivity to subtype-selective NMDA receptor antagonists.
How does the nr2a-nr2b ratio affect NMDAR?
These changes in NR2A-NR2B ratio may explain the effects on the decay kinetics of NMDAR-mediated synaptic responses that occur during development ( Hestrin, 1992; Monyer et al., 1994; Flint et al., 1997 ).
What are the subunits of the NMDAR system?
NMDARs are heteromers (for review, see Dingledine et al., 1999; Cull-Candy et al., 2001) composed of two essential NR1 subunits ( Behe et al., 1995) and two or three NR2 subunits ( Premkumar and Auerbach, 1997; Laube et al., 1998 ). There are four NR2 subunits (A-D), but the NR2A and NR2B subunits predominate in the fore-brain.
How are NMDA receptors involved in learning and memory?
NMDA receptor (NMDAR)-dependent long-term potentiation (LTP) and long-term depression (LTD) are forms of synaptic plasticity that may be critically involved in learning and memory ( Bliss and Collingridge, 1993; Bear and Abraham, 1996; Kemp and Bashir, 2001 ).