GRINA Inhibitors
GRINA inhibitors, by and large, target the NMDA receptor, a crucial ionotropic receptor in neural systems responsible for synaptic plasticity. As GRINA is an integral component of this receptor, inhibiting the broader NMDA receptor activity effectively diminishes GRINA's function. The chemical constituents that serve as these inhibitors display a spectrum of functionalities, from non-competitive to competitive antagonism, and some exhibit selectivity toward specific subunits of the receptor.
For instance, compounds like Ketamine and MK-801 operate as non-competitive antagonists. They obstruct the ion channel in the NMDA receptor, effectively hampering ion flow and downstream signaling. In contrast, AP5 and AP7 act as competitive antagonists, binding to the glutamate site on the receptor, thereby preventing the natural ligand from initiating the receptor's activity. Additionally, some compounds showcase preference for particular subunits, like Ifenprodil, which has an affinity for the GluN2B subunit. This level of specificity provides a nuanced modulation of NMDA receptor function..
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Memantine hydrochloride | 41100-52-1 | sc-203628 | 50 mg | $68.00 | 4 | |
Memantine acts as a low-affinity, voltage-dependent non-competitive antagonist at the NMDA receptor. It blocks the receptor under certain conditions, suppressing the role of GRINA within the complex. | ||||||
Ifenprodil hemitartrate | 23210-58-4 | sc-203601B sc-203601 sc-203601A | 5 mg 10 mg 50 mg | $39.00 $61.00 $142.00 | ||
Ifenprodil selectively targets and inhibits the GluN2B subunit-containing NMDA receptors. By inhibiting specific receptor subtypes, the activity and role of GRINA in those receptors is affected. | ||||||
Agmatine sulfate | 2482-00-0 | sc-202920 sc-202920A | 100 mg 500 mg | $69.00 $178.00 | ||
Agmatine, an endogenous neuromodulator, can obstruct the NMDA receptor. This blockade affects the receptor's functionality, including that of GRINA. | ||||||
D(−)-2-Amino-5-phosphonovaleric acid (D-AP5) | 79055-68-8 | sc-200434 | 5 mg | $95.00 | 2 | |
AP5, a competitive antagonist, binds directly to the glutamate recognition site on the NMDA receptor, thereby suppressing its activation. This impacts the receptor's functionality and, by extension, GRINA's role. | ||||||
1-Adamantylamine | 768-94-5 | sc-251475 sc-251475A | 1 g 25 g | $38.00 $144.00 | ||
Amantadine, as a low-affinity non-competitive antagonist, blocks the NMDA receptor. This blockage diminishes receptor activity, impacting GRINA's functional role. | ||||||
Kynurenic acid | 492-27-3 | sc-202683 sc-202683A sc-202683B | 250 mg 1 g 5 g | $25.00 $56.00 $135.00 | 6 | |
Kynurenic acid is an endogenous modulator that can act as a non-selective antagonist on the NMDA receptor. Its antagonistic activity disrupts receptor function, suppressing GRINA's role within it. | ||||||