SA 4503 dihydrochloride (Synonyms: AGY 94806, Cutamesine) |
| Catalog No.GC17088 |
Le dichlorhydrate SA 4503 (dichlorhydrate SA4503; dichlorhydrate AGY94806) est un puissant agoniste des récepteurs Sigma 1 avec une CI50 de 17,4 nM dans les membranes cérébrales de cobaye.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 165377-44-6
Sample solution is provided at 25 µL, 10mM.
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SA 4503 dihydrochloride is a highly selective σ1 receptor agonist with an IC50 value of 17nM[1]. The σ1 receptor is a molecular chaperone protein primarily located in the endoplasmic reticulum of central nervous system cells and plays a key role in maintaining cellular homeostasis, regulating ion channels (such as calcium and sodium channels), and providing neuroprotection[2, 3]. SA 4503 dihydrochloride is commonly used in the treatment and research of various neurological (such as Parkinson's disease and depression) and cardiovascular diseases[4, 5].
In vitro, pretreatment of mouse retinal photoreceptor 661W cells with SA 4503 dihydrochloride (10µM) for 1h before exposure to 2500 lux white light for 24h reduced light-induced cell mortality; however, this protective effect was blocked by the σ1 receptor antagonist BD-1047 (1µM)[6]. Treatment of NSC34 cells with SA 4503 dihydrochloride (10µM) for 3, 12, and 27h significantly upregulated the phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK) 1/2 but did not affect the protein expression of the σ1 receptor itself[7].
In vivo, subcutaneous administration of SA 4503 dihydrochloride (0.3mg/kg; once daily) for 16 days to olfactory bulbectomized (OB) rats reduced ambulation and rearing counts, significantly improving exploratory hyperactive behavior in the open-field test[8]. Oral administration of SA 4503 dihydrochloride (3 mg/kg; p.o.) to rats 24h, 5h, and 1h before testing significantly shortened the immobility time in the forced swimming test[9]. Treatment of rats with transient middle cerebral artery occlusion (tMCAO) with SA 4503 dihydrochloride (0.5mg/kg; once daily; 5 days; s.c.) starting from day 2 post-stroke, significantly increased the protein level of the microglia/macrophage activation marker IBA1 in the infarct core[4].
References:
[1] MATSUNO K, SENDA T, KOBAYASHI T, et al. SA4503, a novel cognitive enhancer, with σ1 receptor agonistic properties[J]. Behavioural brain research, 1997, 83(1-2): 221-224.
[2] MONNET F P. Sigma-1 receptor as regulator of neuronal intracellular Ca2+: clinical and therapeutic relevance[J]. Biology of the cell, 2005, 97(12): 873-883.
[3] RYSKAMP D A, KORBAN S, ZHEMKOV V, et al. Neuronal sigma-1 receptors: signaling functions and protective roles in neurodegenerative diseases[J]. Frontiers in neuroscience, 2019, 13: 474181.
[4] RUSCHER K, INACIO A R, VALIND K, et al. Effects of the sigma-1 receptor agonist 1-(3, 4-dimethoxyphenethyl)-4-(3-phenylpropyl)-piperazine dihydro-chloride on inflammation after stroke[J]. 2012.
[5] LUCAS G, RYMAR V V, SADIKOT A F, et al. Further evidence for an antidepressant potential of the selective δ1 agonist SA 4503: electrophysiological, morphological and behavioural studies[J]. International journal of neuropsychopharmacology, 2008, 11(4): 485-495.
[6] SHIMAZAWA M, SUGITANI S, INOUE Y, et al. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death against light-induced damage[J]. Experimental eye research, 2015, 132: 64-72.
[7] ONO Y, TANAKA H, TAKATA M, et al. SA4503, a sigma-1 receptor agonist, suppresses motor neuron damage in in vitro and in vivo amyotrophic lateral sclerosis models[J]. Neuroscience letters, 2014, 559: 174-178.
[8] WANG D, NODA Y, TSUNEKAWA H, et al. Role of N-methyl-D-aspartate receptors in antidepressant-like effects of σ1 receptor agonist 1-(3, 4-dimethoxyphenethyl)-4-(3-phenylpropyl) piperazine dihydrochloride (SA-4503) in olfactory bulbectomized rats[J]. The journal of pharmacology and experimental therapeutics, 2007, 322(3): 1305-1314.
[9] SKUZA G, ROGOZ Z. A potential antidepressant activity of SA4503, a selective σ1 receptor agonist[J]. Behavioural pharmacology, 2002, 13(7): 537-543.
| Cell experiment [1]: | |
Cell lines | Murine photoreceptor-derived 661W cells |
Preparation Method | The 661W cells were treated with 10μM SA 4503 dihydrochloride and incubated for 1h under a humidified atmosphere of 5% CO2 at 37℃. The cells were exposed to 2500 lux of white fluorescent light for 24h, then nuclear staining assays were performed. Hoechst 33342 stains the nuclei of all cells, whereas propidium iodide (PI) stains only dead cells. The cell death rate was calculated by double staining with two fluorescent dyes: Hoechst 33342 and PI. |
Reaction Conditions | 10μM; 1h and additional 24h |
Applications | Pretreatment with 10μM SA 4503 dihydrochloride protected against light-induced cell death. |
| Animal experiment [2]: | |
Animal models | tMCAO model rats |
Preparation Method | Starting on day 2 after MCAO, rats were injected daily with SA 4503 dihydrochloride (0.5mg/kg bodyweight; s.c.) for 5 consecutive days, and the protein levels of IBA1 in the infarct core was assessed by Western blot analysis. |
Dosage form | 0.5mg/kg; once daily; 5 days; s.c. |
Applications | A significant increase in the protein level of IBA1, a marker for microglia/macrophage activation, was observed in the infarct core following treatment with SA 4503 dihydrochloride. |
References: | |
| Cas No. | 165377-44-6 | SDF | |
| Synonymes | AGY 94806, Cutamesine | ||
| Chemical Name | 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride | ||
| Canonical SMILES | COC1=CC(CCN2CCN(CCCC3=CC=CC=C3)CC2)=CC=C1OC.Cl.Cl | ||
| Formula | C23H32N2O2.2HCl | M.Wt | 441.43 |
| Solubility | PBS (pH 7.2): 5 mg/ml | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2654 mL | 11.3268 mL | 22.6536 mL |
| 5 mM | 453.1 μL | 2.2654 mL | 4.5307 mL |
| 10 mM | 226.5 μL | 1.1327 mL | 2.2654 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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