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G蛋白偶联受体/G蛋白
神经信号通路
/ 5-羟色胺受体 / Tandospirone/坦度螺酮

Tandospirone/坦度螺酮 {[allProObj[0].p_purity_real_show]}

货号：A437039 同义名： SM-3997

Tandospirone is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1-adrenergic, α2-adrenergic, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).

Tandospirone/坦度螺酮 化学结构 CAS号：87760-53-0
Tandospirone/坦度螺酮 化学结构
CAS号：87760-53-0
Tandospirone/坦度螺酮 3D分子结构
CAS号：87760-53-0
Tandospirone/坦度螺酮 化学结构 CAS号：87760-53-0
Tandospirone/坦度螺酮 3D分子结构 CAS号：87760-53-0
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Tandospirone/坦度螺酮 纯度/质量文件 产品仅供科研

货号：A437039 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		98%
Venlafaxine ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		98%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

 		98%
Tropisetron ✔ 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron HCl dihydrate ✔ 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

 		++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tandospirone/坦度螺酮 生物活性

描述 Tandospirone (SM-3997) is a potent and selective partial agonist of the 5-HT1A receptor, with a Ki of 27 nM, exhibiting anxiolytic and antidepressant properties. It is explored for its applications in central nervous system disorders and their mechanisms[1][2][3].

Tandospirone/坦度螺酮 动物研究

Animal study Tandospirone, at doses ranging from 10 to 80 mg/kg administered intraperitoneally, reduces freezing behavior in rats subjected to conditioned fear stress-induced freezing[3].Tandospirone's anxiolytic effects are observable based on plasma concentrations at 0.5 hours post-administration, but not at 4 hours[3].

Tandospirone/坦度螺酮 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03667677 Hypertension ... 展开 >>Anxiety 收起 << Phase 4 Not yet recruiting July 1, 2020 China, Beijing ... 展开 >> Beijing Friendship Hospital of Capital Medical University Beijing, Beijing, China Beijing Haidian Section of Peking University Third Hospital Beijing, Beijing, China Xuanwu Hospital of Capital Medical University Beijing, Beijing, China China, Chongqing Yongchuan Hospital of Chongqing Medical University Chongqing, Chongqing, China China, Giangsu Zhongda Hospital of Southeast University Nanjing, Giangsu, China China, Hebei Kailuan General Hospital Tangshan, Hebei, China China, Shanxi the First Affiliated Hospital of Shanxi Medical University Taiyuan, Shanxi, China 收起 <<
NCT01614041 Generalized Anxiety Disorder Phase 4 Unknown December 2017 China ... 展开 >> Shanghai Tongji Hospital Recruiting Shanghai, China, 200065 Contact: Wenyuan Wu, MD 收起 <<
NCT03151382 Alzheimer Disease ... 展开 >> Cognitive Function 收起 << Phase 4 Not yet recruiting June 30, 2018 -

Tandospirone/坦度螺酮 参考文献

[1]Hamik A, et al. Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites. Biol Psychiatry. 1990 Jul 15;28(2):99-109.

[2]Xuefei Huang, et al. Role of tandospirone, a 5-HT1A receptor partial agonist, in the treatment of central nervous system disorders and the underlying mechanisms. Oncotarget. 2017 Nov 24; 8(60): 102705–102720.

[3]Kyoko Nishitsuji, et al. The pharmacokinetics and pharmacodynamics of tandospirone in rats exposed to conditioned fear stress. Eur Neuropsychopharmacol. 2006 Jul;16(5):376-82.

Tandospirone/坦度螺酮 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL

Tandospirone/坦度螺酮 技术信息

CAS号87760-53-0
分子式C21H29N5O2
分子量 383.49
SMILES Code O=C1[C@]2([H])[C@]([C@H]3CC[C@@H]2C3)([H])C(N1CCCCN(CC4)CCN4C5=NC=CC=N5)=O
MDL No. MFCD00904852
别名 SM-3997
运输蓝冰
InChI Key CEIJFEGBUDEYSX-FZDBZEDMSA-N
Pubchem ID 91273
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Tandospirone/坦度螺酮 |Tandospirone/坦度螺酮 | SM-3997 | 87760-53-0 | 5-羟色胺受体 | Tandospirone/坦度螺酮 纯度/质量文件 | Tandospirone/坦度螺酮 亚型比较 | Tandospirone/坦度螺酮 生物活性 | Tandospirone/坦度螺酮 临床数据 | Tandospirone/坦度螺酮 参考文献 | Tandospirone/坦度螺酮 实验方案 | Tandospirone/坦度螺酮 技术信息

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