GRIN3 Inhibitors
GRIN3 inhibitors encompass a specific category of chemical compounds designed to modulate the activity of the GRIN3 protein, which forms a subunit of the NMDA (N-methyl-D-aspartate) receptor complex. As part of the receptor, GRIN3 plays a critical role in the excitatory neurotransmission in the central nervous system, contributing to processes such as synaptic plasticity, learning, and memory. The inhibitors function by binding to the GRIN3 subunit, thereby altering the receptor's configuration and attenuating the ionic flux through the receptor channels. This action effectively reduces the excitatory neurotransmissions that are mediated by NMDA receptors, which are pivotal in glutamatergic signaling. The precise modulation by GRIN3 inhibitors is characterized by their ability to interfere with the calcium and sodium ion channel permeability, which is essential for the normal function of the NMDA receptor. As a result, these inhibitors are able to curtail the excitatory potential that is often associated with the NMDA receptor activity.
The chemical architecture of GRIN3 inhibitors is varied, with each compound exhibiting a unique affinity and selectivity towards the GRIN3 subunit. The structural diversity allows for specificity in the inhibition of the NMDA receptor function, bypassing the potential for widespread inhibition that could occur with less selective agents. The molecular interactions of GRIN3 inhibitors with the receptor subunit are complex, involving not only the blocking of the ion channel but also affecting the receptor's allosteric sites, which can modulate receptor activity indirectly. By targeting different regulatory sites on the GRIN3 subunit, these inhibitors are capable of fine-tuning the receptor activity, including altering the kinetics of receptor opening and closing or changing the receptor's sensitivity to its natural ligand, glutamate. This specificity enables a more controlled approach to modulating the intricate signaling processes in which the NMDA receptor is involved, highlighting the sophisticated nature of these inhibitory compounds.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Memantine hydrochloride | 41100-52-1 | sc-203628 | 50 mg | $69.00 | 4 | |
Memantine is an NMDA receptor antagonist that specifically targets the NMDA subtype receptors, such as GRIN3. By binding to the receptor, it blocks the action of glutamate, which is the principal excitatory neurotransmitter in the central nervous system. This blockade of glutamate prevents the influx of calcium ions, which would otherwise lead to activation of the receptor and downstream signaling. | ||||||
Dextromethorphan | 125-71-3 | sc-278927 sc-278927A sc-278927B | 10 g 100 g 500 g | $177.00 $1156.00 $5208.00 | 3 | |
Dextromethorphan acts as an NMDA receptor antagonist. By inhibiting the NMDA receptor, to which GRIN3 contributes, dextromethorphan can diminish neuronal excitation and the resultant calcium signaling. | ||||||
Ifenprodil hemitartrate | 23210-58-4 | sc-203601B sc-203601 sc-203601A | 5 mg 10 mg 50 mg | $39.00 $61.00 $142.00 | ||
Ifenprodil is a selective inhibitor of NMDA receptors containing the GRIN3 subunit. It allosterically modulates the receptor, resulting in reduced calcium influx through the receptor channel, leading to decreased neuronal excitatory activity. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $48.00 | ||
Zinc is an endogenous modulator of NMDA receptors and can selectively inhibit receptor subtypes containing the GRIN3 subunit by binding to a specific site on the receptor, thus inhibiting its activity. | ||||||
Felbamate | 25451-15-4 | sc-203579 sc-203579A | 10 mg 50 mg | $101.00 $373.00 | ||
Felbamate functions as an NMDA receptor antagonist, with a preferential effect on receptors containing the GRIN3 subunit. It acts at a modulatory site distinct from the glutamate-binding site, leading to reduced excitatory neurotransmission. | ||||||
Riluzole | 1744-22-5 | sc-201081 sc-201081A sc-201081B sc-201081C | 20 mg 100 mg 1 g 25 g | $20.00 $193.00 $213.00 $317.00 | 1 | |
Riluzole indirectly inhibits NMDA receptors by inactivating voltage-dependent sodium channels, which can suppress glutamate release into the synaptic cleft. This reduction in available glutamate can lead to decreased activation of NMDA receptors, including those with the GRIN3 subunit. | ||||||
L-701,324 | 142326-59-8 | sc-361224 sc-361224A | 10 mg 50 mg | $161.00 $624.00 | 1 | |
L-701,324 is an antagonist at the glycine modulatory site of the NMDA receptor. By inhibiting this site, it can reduce the activity of NMDA receptors including those containing the GRIN3 subunit, as the presence of glycine is necessary for receptor activation. | ||||||