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
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Beta Amyloid(69)
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Chloride Channel(34)
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CRM1(5)
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Glutamate Transporter(1)
GlyT(13)
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iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
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NMDAR
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R-(+)-EU-1180-453
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Alaproclate
产品货号 : 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
产品货号 : 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.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease. -
N-Methyl-DL-aspartic acid
产品货号 : M35791
cas no: 17833-53-3
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Neboglamine hydrochloride
产品货号 : M35445
cas no: 2759182-59-5
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