Naspm trihydrochloride 是Joro蜘蛛毒素的合成类似物，具有拮抗CP-AMPA受体的活性。

Naspm trihydrochloride is a synthetic analogue of Joro spider toxin and is an antagonist of calcium permeable AMPA (CP-AMPA) receptors.

NASPM selectively suppressed the inwardly rectifying and Ca(2+)-permeable AMPA receptors expressed in type II neurons. It had no effect on AMPA receptors in type I neurons. The blocking effect of NASPM on the Ca(2+)-permeable AMPA receptors was use and voltage-dependent. When the effect of NASPM reached a steady state, current responses induced by ionophoretic applications of kainate, a non-desensitizing agonist of AMPA receptors, in type II neurons were suppressed by NASPM in a dose-dependent manner at -60 mV (IC50 0.33 microM, and Hill coefficient 0.94). The response to kainate recovered partially after washing out NASPM. NASPM did not affect the Ca(2+)-permeable AMPA receptors when the neuronal membrane was held at potentials more positive than +40 mV. Furthermore, the blockade by NASPM which was attained at negative potentials was transiently removed by shifting membrane potential to +60 mV for 5 s together with a single ionophoretic application of kainate.

1049731-36-3

C22H37Cl3N4O

479.92

1-Naphthylacetyl spermine trihydrochloride

H2O:50 mg/mL (104.19 mM),Need ultrasonic
DMSO:6.4 mg/mL (13.34 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years