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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CC1=NC2=NC(CCC)=NN2C(O)=C1NS(C3=CC=C(C4CCCCC4)C=C3)(=O)=O
生化／生理作用
GNE-9278 is a selective NMDAR, but not AMPAR, positive allosteric modulator (PAM fold enhancement Emax/EC50 = 5.5/0.74 μM/2A, 8.4/3.07 μM/2B,10.2/0.47 μM/2C, 7.9/0.32 μM/2D of gly EC50 (50 μM)-induced Ca++ influx in HEK293 co-expressing GluN1 & respective GluN2 subunit; Emax/EC50 = 4.6/3.2 μM/2A,12.4/15.7 μM/2B, 9.1/6.6 μM/2C, 14.9/6.7 μM/2D of 100 μM Glu-induced current in the presence of 50 μM gly using respective GluN1/GluN2 oocytes). GNE-9278 targets transmembrane domain (TMD) extracellular surface of agonist-bound NMDARs, stabilizing NMDARs in an activated state by slowing L-L-glu & gly off-rate.
Selective NMDAR, but not AMPAR, positive allosteric modulator (PAM) that targets TMD extracellular surface of ligand-bound NMDARs and slows L-Glu/Gly dissociation.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Tzu-Ming Wang et al.
Neuropharmacology, 121, 204-218 (2017-05-02)
Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission and are key nervous system drug targets. While diverse pharmacological tools have yielded insight into iGluR extracellular domain function, less is known about molecular mechanisms underlying the ion conduction gating process within
Erica S Burnell et al.
Journal of medicinal chemistry, 62(1), 3-23 (2018-02-16)
Excitatory activity in the CNS is predominately mediated by l-glutamate through several families of l-glutamate neurotransmitter receptors. Of these, the N-methyl-d-aspartate receptor (NMDAR) family has many critical roles in CNS function and in various neuropathological and psychiatric conditions. Until recently
Ioana Neagoe et al.
Stem cell research, 28, 105-114 (2018-02-18)
Abnormal signaling pathways mediated by N-methyl-d-aspartate receptors (NMDARs) have been implicated in the pathogenesis of various CNS disorders and have been long considered as promising points of therapeutic intervention. However, few efforts have been previously described concerning evaluation of therapeutic
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