Naspm trihydrochloride

Research use only, not for human use.

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

Naspm trihydrochloride is a synthetic analogue of Joro spider toxin and is an antagonist of calcium permeable AMPA (CP-AMPA) receptors.(In Vitro):Naspm trihydrochloride 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 trihydrochloride on the Ca(2+)-permeable AMPA receptors was use and voltage-dependent. When the effect of Naspm trihydrochloride 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 trihydrochloride 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 trihydrochloride. Naspm trihydrochloride 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 trihydrochloride 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.

NASPM selectively suppresses the inwardly rectifying and Ca2+-permeable AMPA receptors expressed in type II neurons. It has no effect on AMPA receptors in type I neurons. At -60 mV, NASPM suppresses AMPA receptors in type II neurons with an IC50 value of 0.33 μM. The blocking effect of NASPM on the Ca2+-permeable AMPA receptors is use and voltage-dependent.

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1-Naphthylacetyl spermine trihydrochloride

Membrane Transporter/Ion Channel

iGluR

Human Endogenous Metabolite

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1049731-36-3

479.92

C22H37Cl3N4O

>98% (HPLC)

In Vitro:?H2O : 50 mg/mL (104.19 mM)

Cl.Cl.Cl.NCCCNCCCCNCCCNC(=O)Cc1cccc2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years