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].
RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.
NS-102 is a selective kainate (GluK2) receptors antagonist. NS-102 is a potent GluR6/7 receptor antagonist[1][2][3].
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].
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.
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.
NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.
HBT1 is a novel potent AMPA receptor potentiator with lower agonistic effect compared with LY451395 and OXP1.
(S)-(-)-HA 966 ((-)-HA 966), a γ-Hydroxybutyrate-like agent, is weakly active as an NMDA-receptor antagonist. (S)-(-)-HA 966 possesses muscle relaxant action and prevents enhanced mesocorticolimbic dopamine metabolism and behavioral correlates of restraint stress, conditioned fear[1][2].
MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research[1].
L-Glutamic acid-d5 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.
TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM[1].
ATPA is a selective glutamate receptor GluR5 activator with EC50s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), respectively[1].
Cis-piperidine-2,3-dicarboxylic acid is a non-specific antagonist of NMDA, AMPA and kainate ionotropic receptors and a partial agonist for NMDA receptors. Cis-piperidine-2,3-dicarboxylic acid can be used in blocking general excitatory synaptic transmissions[1].
NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research[1].
Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease[1][2].
LY-466195 is a competitive antagonist of GLUK5 receptor.
GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1[1][2].
CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD)[1][2].
6-Methoxy-2-naphthoic acid is an NMDA receptor modulator extracted from patent WO 2012019106 A2.
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine[1].
NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research[1].
Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD)[1][2][3].
CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.IC50 value: 45.4 ± 4.2 nM/63.4 ± 5.6 nM(GluA2i/GluA2o) [1]Target: AMPAR modulatorCMPDA was nearly equipotent at modulating the two isoforms of GluA2 receptors, whereas CMPDB displayed a modest preference for the flip splice variant. Similar to CX614, CMPDA slowed the rate of deactivation of GluA2o receptors approximately 2-fold but had no effect on GluA2i receptor deactivation [1].
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.
Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM [1]Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays [2].in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation [3].
CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit. IC50 value: 2.7 μM (EC50, for NR2C) and 2.8 μM (EC50, NR2D)Target: NMDA receptorCIQ increases channel opening frequency of recombinant NR2Cor NR2D containing receptors by two-fold (EC50 = 2.7 and 2.8 μM, respectively), with no effect on NR2A or NR2B subtypes. CIQ does not alter the EC50 values for glutamate or glycine on channel opening. CIQ increases channel opening efficiency and enhances NMDA receptor responses. CIQ reduces associated behaviours in schizophrenia models and potentially enhances dopamine release in Parkinson's disease models.
Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist[1].
Nevadistinel (NYX-458; NYX-3054) 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].