NASPM specifically inhibits the inwardly rectifying and Ca2+-permeable AMPA receptors present in type II neurons, while it does not affect AMPA receptors in type I neurons. At -60 mV, NASPM exhibits an IC50 value of 0.33 µM for suppressing AMPA receptors in type II neurons. The blocking effect of NASPM on Ca2+-permeable AMPA receptors is both use and voltage-dependent [1].
体外研究
NASPM specifically inhibits the inwardly rectifying and Ca2+-permeable AMPA receptors present in type II neurons, while it does not affect AMPA receptors in type I neurons. At -60 mV, NASPM exhibits an IC50 value of 0.33 µM for suppressing AMPA receptors in type II neurons. The blocking effect of NASPM on Ca2+-permeable AMPA receptors is both use and voltage-dependent [1].
Naspm 3HCl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bergmann glia
100 μM
Used to verify the blocking effect of NASP on Ca2+-permeable AMPA receptors, finding that 100 μM NASP effectively blocked AMPA-induced currents in Bergmann glial cells.
J Physiol. 2007 Oct 1;584(Pt 1):89-96.
Hippocampal neurons
30 µM
From 6 DIV to 13 DIV, twice a day (at 9 am and 5 pm)
NASPM treatment restored the spine dynamics of Rab39b KO neurons to be comparable to WT conditions
Mol Psychiatry. 2021 Nov;26(11):6531-6549.
HEK293 cells
100 μM
The block of GluA1 by NASPM was unaffected by the type of auxiliary subunit, achieving complete block of outward currents
Elife. 2023 Apr 12;12:e66765.
PV-FSI
100 µM
>5 min
Blocking cortical activation of PV-FSIs, mimicking and occluding the effect of mecamylamine on SPN spike latency
Elife. 2022 May 17;11:e75829.
Cultured brainstem neurons
5 μM
NASPM dose-dependently blocked the NTG-enhanced Ca2+ influx
Neuropharmacology. 2018 May 1;133:462-469.
Naspm 3HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
GluA2 knockout mice
Intracellular
100 μM
Not explicitly mentioned
In neurons from GluA2 KO mice, NASPM completely blocked the outward component of synaptic currents, whereas spermine could not
To evaluate the effect of naspm on NTX-induced mechanical hypersensitivity, it was found that naspm dose-dependently inhibited NTX-induced mechanical hypersensitivity.
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