Cutamesine Dihydrochloride

製品コードS2917 バッチS291701

印刷

化学情報

Chemical Structure Synonyms SA4503 dihydrochloride, AGY94806 dihydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H32N2O2.2HCl
分子量 441.43 CAS No. 165377-44-6
Solubility (25°C)* 体外 Water 88 mg/mL (199.35 mM)
DMSO 22 mg/mL (49.83 mM)
Ethanol 11 mg/mL (24.91 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Cutamesine dihydrochloride (SA4503 dihydrochloride,AGY94806 dihydrochloride) is a potent Sigma-1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
in vitro

SA 4503 has weak binding affinities for sigma 1 adrenergic, dopamine D, serotonin (5-HT)1A, 5-HT2, histamine H, muscarinic M1, and muscarinic M2 receptors at a concentration of 10 μM. GTP weaks SA 4503-induced inhibition of (+)-[3H]pentazocine binding in rat brain membranes. SA 4503 inhibits specific (+)-[3H]pentazocine binding in a competitive manner. [1]
in vivo

SA 4503 (0.03 mg/kg-1 mg/kg s.c.) attenuates the dizocilpine (0.15 mg/kg i.p.) and L-NAME (100 mg/kg i.p.)-induced memory deficits following a bell-shaped curve in both the Y-maze for spatial working memory and step-down type passive avoidance test in mice. Progesterone (2 mg/kg s.c.) blocks the SA 4503 effects in the dizocilpine- and L-NAME-amnesia models, in accordance with the purported neurosteroids/sigma1 receptors interaction. [2] SA 4503 (100 nM-300 nM) increases the electrically evoked release of acetylcholine in hippocampal but not striatal slices of rats. Concentrations below 100 nM does not alter the electrically evoked release of acetylcholine in either brain area. [3] SA 4503 (1 mg/kg i.p. bid) produces a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons in rats. SA 4503 (1 mg/kg i.p. repeat ) produces a significant increase in the number of spontaneously active VTA DA neurons. The repeated administration of SA 4503 produces a greater alteration of the firing pattern of spontaneously active VTA compared to SNC DA neurons. [4] Repeated treatment with SA 4503 (0.3 mg/kg) ameliorates the behavioral deficits in olfactory bulbectomized rats resembling depression symptoms in the open-field test, sexual behavior test, and cued and contextual fear-conditioning test. SA 4503 displays advantages over desipramine in the sexual behavior test. SA 4503 also reverses the decrease in the protein expression of NMDA receptor subunit (NR)1, but not NR2A or NR2B, in the prefrontal cortex, hippocampus, and amygdala of olfactory bulbectomized rats. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
The sigma 1 receptor subtype is labeled using (+)-[3H]pentazocine, while the sigma 2 receptor subtype is labeled using 1,3-[3H]di(2-tolyl)guanidine ([3H]DTG) in the presence of 200 nM (+)-pentazocine. The reaction is initiated by addition of 0.2 mL of the membrane preparation to the mixture containing 3H-ligands, and unlabeled sigma receptor ligands in a final volume of 1.0 mL. Incubations are carried out at 37 ℃ for 150 min in the (+ )-[3H]pentazocine binding study and at 25℃ for 90 min in the [3H]DTG binding study.
動物実験 動物モデル Male Swiss mice
投薬量 1 mg/kg
投与方法 Subcutaneous injection

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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