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Purity: ≥98%
Naspm 3HCl (1-Naphthylacetyl spermine trihydrochloride), the trihydrochloride salt of Naspm, is a synthetic analog of Joro spider toxin and a calcium permeable AMPA (CP-AMPA) receptors antagonist.
| Targets |
NASPM trihydrochloride (1-Naphthylacetyl spermine) selectively blocks inwardly rectifying, Ca²⁺-permeable AMPA-type glutamate receptors that lack or have low expression of the GluR2 subunit (IC₅₀ = 0.33 µM at −60 mV). It has no effect on outwardly rectifying, Ca²⁺-impermeable AMPA receptors containing GluR2.
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| ln Vitro |
The Ca2+-permeable and inward rectifying AMPA receptors expressed in type II neurons are specifically inhibited by NASPM. On type I neurons' AMPA receptors, it has no impact. With an IC50 value of 0.33 µM, NASPM inhibits AMPA receptors in type II neurons at -60 mV. Applications and voltages affect how well NASPM blocks Ca2+ permeable AMPA receptors [1].
NASPM selectively suppressed kainate-induced currents in type II cultured rat hippocampal neurons, which express inwardly rectifying and Ca²⁺-permeable AMPA receptors, in a dose-dependent manner (IC₅₀ = 0.33 µM, Hill coefficient = 0.94) at a holding potential of −60 mV. The suppression reached a steady state after 15–25 ionophoretic applications of kainate, reducing the response to 11.0 ± 0.7% of control. The blockade was use-dependent and voltage-dependent; no suppression was observed at membrane potentials more positive than +40 mV. The effect was partially reversible after washing (recovery to 43.7 ± 4.5% of control). In type I neurons (expressing GluR2-containing AMPA receptors), NASPM had no effect (98.5 ± 1.1% of control). Intermediate neurons showed intermediate sensitivity. [1] |
| Enzyme Assay |
The study utilized whole-cell patch-clamp recordings to assess the blocking effect of NASPM on AMPA receptors. Cultured rat hippocampal neurons were voltage-clamped at various holding potentials. Kainate, a non-desensitizing AMPA receptor agonist, was applied ionophoretically to the soma using high-resistance glass electrodes filled with 100 mM kainate solution. Current responses were recorded before, during, and after bath application of NASPM. The rectification index (RI) was calculated to classify neurons into type I (RI > 1.0), type II (RI < 0.25), and intermediate (0.25 ≤ RI ≤ 1.0). The voltage dependence of blockade and recovery was tested by shifting membrane potential during drug application. [1]
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| Cell Assay |
Primary hippocampal neurons were cultured from 17–19-day-old rat embryos and used for electrophysiology 8–14 days after plating. Whole-cell recordings were performed using patch pipettes filled with an internal solution containing CsCl, EGTA, and HEPES. The external solution contained NaCl, KCl, CaCl₂, glucose, HEPES, TTX, and bicuculline. To test the effect of NASPM, the drug was bath-applied and solution exchange was controlled via peristaltic pumps. Kainate was applied ionophoretically every 3 seconds. Current responses were filtered at 1 kHz and digitized at 2 kHz. The degree of blockade was quantified as the percentage reduction in peak current amplitude compared to control. [1]
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| References | |
| Additional Infomation |
NASPM is a synthetic analogue of Joro spider venom (JSTX-3), but with a more compact molecular structure and reversible blocking effect compared to the near-irreversible effect of JSTX. It is a non-competitive antagonist that antagonizes Ca²⁺-permeable AMPA receptors. This drug can serve as a useful pharmacological tool for studying the physiological and pathological roles of these receptors in the central nervous system (CNS), such as their role in synaptic plasticity, ischemia, and excitotoxic neuronal death. [1]
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| Molecular Formula |
C22H34N4O
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|---|---|
| Molecular Weight |
370.53156
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| Exact Mass |
478.203
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| CAS # |
1049731-36-3
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| Related CAS # |
Naspm;122306-11-0
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| PubChem CID |
16219727
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| Appearance |
White to off-white solid powder
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| LogP |
6.925
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
30
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| Complexity |
391
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JNEOJAUJWOPWJS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H34N4O.3ClH/c23-12-6-15-24-13-3-4-14-25-16-7-17-26-22(27)18-20-10-5-9-19-8-1-2-11-21(19)20;;;/h1-2,5,8-11,24-25H,3-4,6-7,12-18,23H2,(H,26,27);3*1H
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| Chemical Name |
N-[3-[4-(3-aminopropylamino)butylamino]propyl]-2-naphthalen-1-ylacetamide;trihydrochloride
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| Synonyms |
Naspm trihydrochloride; 1-Naphthylacetyl spermine trihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~104.19 mM)
DMSO : ~6.4 mg/mL (~13.34 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (208.37 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6988 mL | 13.4942 mL | 26.9884 mL | |
| 5 mM | 0.5398 mL | 2.6988 mL | 5.3977 mL | |
| 10 mM | 0.2699 mL | 1.3494 mL | 2.6988 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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