Tandospirone (SM-3997) 是一种高效、选择性的5-HT1A受体部分激动剂,其Ki值为 27 nM。Tandospirone 具有抗焦虑和抗抑郁作用。Tandospirone 可用于中枢神经系统疾病及其潜在机制的研究。
生物活性 | Tandospirone (SM-3997) is a potent and selective5-HT1Areceptor partial agonist, with aKiof 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms[1][2][3]. |
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体外研究 (In Vitro) | Tandospirone is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, α1-adrenergic, α2-adrenergic and dopamine D1 and D2 receptors (Kivalues ranging from 1300 to 41000 nM) than 5-HT1A[1]. Tandospirone is essentially inactive at 5-HT1Breceptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors[1]. Tandospirone activates postsynaptic 5-HT1Areceptor coupled with G-protein (Gi/o), resulting in inhibition of protein kinase A (PKA)-mediated protein phosphorylation and neuronal activity[1].
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体内研究 (In Vivo) | Tandospirone (10-80 mg/kg; i.p.) inhibits freezing behavior in the conditioned fear stress-induced freezing behavior rat model[3]. Tandospirone exhibits the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours[3].
Animal Model: | Seven-week-old male Sprague-Dawley rats (260-300 g), conditioned fear stress-induced freezing behavior rat model[3] | Dosage: | 10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg | Administration: | Intraperitoneal injection | Result: | Inhibited freezing behavior in a dose-dependent manner. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 16.67 mg/mL(43.47 mM;Need ultrasonic) H2O : 0.1 mg/mL(0.26 mM;Need ultrasonic) 配制储备液 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL |
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此方案可获得 ≥ 2.5 mg/mL (6.52 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.52 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.52 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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