iGluR Antagonist

Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

UBP310 is a selective GluR5 antagonist, with a K_d of 130 nM.

Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.

L-Phenylalanine (Standard) is the analytical standard of L-Phenylalanine. This product is intended for research and analytical applications. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.

Phaseic acid is a Abscisic acid terpenoid catabolite that can able to activate a subset of Abscisic acid repectors. Phaseic acid is a plant hormone associated with photosynthesis arrest and abscission. Phaseic acid is the antagonist for NMDA-type glutamate receptor (NMDAR) that inhibits NMDAR currents with an IC₅₀ of 34.37 μM. Phaseic acid reduces intracellular calcium influx, and exhibits neuroprotective effect.

NS-102 is a selective kainate (GluK2) receptor antagonist. NS-102 is a potent GluR6/7 receptor antagonist.

Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of ^[3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation.

NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC₅₀ of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier.

Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM). Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC₅₀ of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.

UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a K_b value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist.

Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with K_i and IC ₅₀ of 8.1 nM and 3.6 nM, respectively.

L-Phenylalanine-¹⁵N is the ¹⁵N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a K_i of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

UBP301 hydrochloride is a potent and selective antagonist of kainate receptor with IC₅₀ and K_D of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has ～30-fold selectivity of kainate receptor over AMPA receptor. UBP301 hydrochloride is the derivative of willardiine.

DQP-1105 is a potent noncompetitive NMDA receptor antagonist. DQP-1105 inhibits GluN2C- and GluN2D-containing receptors (IC₅₀=7.0 and 2.7 μM, respectively). The IC₅₀ values are at least 50-fold lower than those for recombinant GluN2A-, GluN2B-, GluA1-, or GluK2-containing receptors.

GluN2B-NMDAR antagonist-1 is an orally active GluN2B-NMDAR antagonist. GluN2B-NMDAR antagonist-1 has neuroprotective activity. GluN2B-NMDAR antagonist-1 can be used for research of ischemic injury.

Nylidrin hydrochloride (Buphenine hydrochloride) is an orally active β-adrenergic agonist. Nylidrin hydrochloride antagonizes NR1_A/2B NMDA receptors (IC₅₀ = 0.18 μM in Xenopus oocytes). Nylidrin hydrochloride reduces the levels of NP, HA, and M1. Nylidrin hydrochloride has antiviral activity against multiple H1N1 subtype influenza A viruses. Nylidrin hydrochloride improves hemorrhagic shock and anti-allergic effects.

CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC₅₀ of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.

Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist.

Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a K_i value of 27.7?μM.