Cart
sales@molnova.com
NMDAR
N-Methyl-D-aspartate receptors (NMDARs) are broadly distributed in the central nervous system (CNS), where they mediate excitatory signaling. NMDAR-mediated neurotransmission (NMDARMN) is the molecular engine of learning, memory and cognition, which are the basis for high cortical function. The involvement of NMDARMN has been demonstrated in a variety of CNS disorders, including schizophrenia, depression, posttraumatic stress disorder, aging, mild cognitive impairment (MCI) and Alzheimer’s dementia, attention deficit hyperactivity disorder, amyotrophic lateral sclerosis, and anti-NMDAR encephalitis. “Correction” or “resetting” the NMDARMN in these CNS disorders is a potential therapeutic approach. NMDAR distinguishes itself in two ways.
First, it is both ligand-gated and voltage-dependent; second, it requires co-activation by two agonists: glutamate or aspartate and either D-serine or glycine. Most NMDAR heterotetramers are composed of two NR1 and two NR2 subunits. Activation of NMDAR requires binding of both glutamate/aspatate to the NR2 subunit and its co-agonist, glycine/D-serine, to the NR1 subunit. D-serine/glycine binding is not only necessary for receptor activation; it also increases the affinity of the receptor for glutamate and modulates receptor function by decreasing receptor desensitization while promoting receptor turnover via internalization.
References
1.Tsai GE. Adv Pharmacol. 2016;76:257–309.
First, it is both ligand-gated and voltage-dependent; second, it requires co-activation by two agonists: glutamate or aspartate and either D-serine or glycine. Most NMDAR heterotetramers are composed of two NR1 and two NR2 subunits. Activation of NMDAR requires binding of both glutamate/aspatate to the NR2 subunit and its co-agonist, glycine/D-serine, to the NR1 subunit. D-serine/glycine binding is not only necessary for receptor activation; it also increases the affinity of the receptor for glutamate and modulates receptor function by decreasing receptor desensitization while promoting receptor turnover via internalization.
References
1.Tsai GE. Adv Pharmacol. 2016;76:257–309.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
NMDAR
-
R-(+)-EU-1180-453
catalog no : M36292
cas no: 2488764-06-1
R-(+)-EU-1180-453 is a novel GluN2C/D selective NMDAR-positive modulator for the study of neurological disorders.
-
Alaproclate
catalog no : M36270
cas no: 60719-82-6
Alaproclate is a non-competitive NMDA receptor antagonist and a new selective 5-HT uptake inhibitor for the study of depression and dementia.
-
Orphenadrine
catalog no : M36262
cas no: 83-98-7
Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.
-
N-Methyl-DL-aspartic acid
catalog no : M35791
cas no: 17833-53-3
N-Methyl-DL-aspartic acid, a glutamate analogue and NMDA receptor agonist, is utilized in neurological disease research.
-
Neboglamine hydrochloride
catalog no : M35445
cas no: 2759182-59-5
Neboglamine (CR-2249, XY-2401) hydrochloride, an orally active positive modulator of the NMDA receptor glycine site, can be used in schizophrenia research .