BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation[1].
Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease[1].
threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity[1][2][3].
TAT-GluA2 3Y is an inhibitor of AMPA receptor endocytosis. TAT-GluA2 3Y induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. TAT-GluA2 3Y also exhibits antinociceptive effects in a rat model of neuropathic pain. TAT-GluA2 3Y rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.
Ifenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site[1][2].
Memantine-d6 hydrochloride is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].
CP-465022 Maleate 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[1][2].
L-Phenylalanine-3-13C ((S)-2-Amino-3-phenylpropionic acid-3-13C) is the 13C-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 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[1][2][3][4].
NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor[1].
RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.
24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
L-Glutamic acid-5-13C is the 13C-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
NS-102 is a selective kainate (GluK2) receptors antagonist. NS-102 is a potent GluR6/7 receptor antagonist[1][2][3].
Transcrocetin (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
L-701252 is a potent antagonist of glycine site NMDA receptor with an IC50 of 420 nM. L-701252 provides a small degree of neuroprotection in global cerebral ischaemia[1].
1-Aminocyclobutanecarboxylic acid is a NMDA receptor partial agonist acting at the glycine site, NR1[1].
Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
Felbamate-d5 is the deuterium labeled Felbamate[1]. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA)[2][3].
Linalool-d3 is the deuterium labeled Linalool[1]. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity[2].Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome[3].
Arcaine (sulfate) is a glutamate NMDA receptor inhibitor[1].
Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
Efinopegdutide (JNJ-64565111) is a potent dual glucagon-like peptide-1 (GLP-1)/glucagon receptor (GluR) agonist, which activates both the GLP-1 and glucagon receptors. Efinopegdutide can be used in research of nonalcoholic steatohepatitis (NASH)[1].
Zelquistinel is a N-methyl-D-aspartate (NMDA) receptor partial agonist used for the research of depression, anxiety and other related psychiatric disorders[1].
Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist. Target: NMDARapastinel is a robust cognitive enhancer and facilitates hippocampal long-term potentiation (LTP) of synaptic transmission in slices.
Glycine-2-13C,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
(S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist[1][2].
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].
6-Hydroxykynurenic acid (6-HKA) is a derivative of kynurenic acid (KYNA) and can be isolated from Ginkgo leaves. 6-Hydroxykynurenic acid is a low-affinity NMDAR antagonist (IC50: 59 μM)[1].
L-Glutamic acid-d3 is the deuterium labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.