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坦度螺酮柠檬酸盐 /Tandospirone citrate 98%

货号:A291243 同义名: 枸橼酸坦度螺酮 / SM-3997 citrate 产品仅供科研

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

Tandospirone citrate 化学结构 CAS号:112457-95-1
Tandospirone citrate 化学结构
CAS号:112457-95-1
Tandospirone citrate 3D分子结构
CAS号:112457-95-1
Tandospirone citrate 化学结构 CAS号:112457-95-1
Tandospirone citrate 3D分子结构 CAS号:112457-95-1
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Tandospirone citrate 纯度/质量文件

货号:A291243 标准纯度:98%
批次查询: 批次纯度:

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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 (human platelets), IC50: 240 μM

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

98%
Venlafaxine 98%
Fluvoxamine maleate 99%
Iloperidone 98%
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 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
WAY-100635 maleate +++

5-HT, IC50: 0.95 nM

99%
Latrepirdine 2HCl GluR 98+%
Fluoxetine hydrochloride 98%
Paroxetine hydrochloride AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

98% HPLC
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 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

99%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

98%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

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

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

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-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 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-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

98%
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 citrate 生物活性

描述 Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). IC50 Value: 27±5 nM(Ki)[3]. Tandospirone citrate (tandospirone) is an anti-anxiety drug that acts by combining with serotonin receptor (5-hydroxytryptamine-1 A [5-HT1A])[4]. Chronic treatment with tandospirone, at 0.2 and 1.0mg/kg/day, but not 2.0mg/kg/day, attenuated footshock stress-induced eLAC (extracellular lactate concentrations) elevation in the mPFC (medial prefrontal cortex)[5]. Rats were acutely administered tandospirone (0, 0.1, and 1 mg/kg, i.p.). Tandospirone decreased the number of premature responses, an index of impulsive action, in a dose-dependent manner[6].

Tandospirone citrate 参考文献

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

[2]Shimizu H, Tatsuno T, et al. Characterization of the putative anxiolytic SM-3997 recognition sites in rat brain. Life Sci. 1988;42(24):2419-27.

[3]Hamik A, Oksenberg D, Fischette C, Peroutka SJ. Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites. Biol Psychiatry. 1990 Jul 15;28(2):99-109

[4]Takei A, Honma S, Kawashima A, Yabe I, Fukazawa T, Hamada K, Hamada T, Tashiro K. Beneficial effects of tandospirone on ataxia of a patient with Machado-Joseph disease. Psychiatry Clin Neurosci. 2002 Apr;56(2):181-5

[5]Uehara T, Matsuoka T, Itoh H, Sumiyoshi T. Chronic treatment with tandospirone, a 5-HT(1A) receptor partial agonist, suppresses footshock stress-induced lactate production in the prefrontal cortex of rats. Pharmacol Biochem Behav. 2013 Nov 15;113:1-6

[6]Ohmura Y, Kumamoto H, Tsutsui-Kimura I, Minami M, Izumi T, Yoshida T, Yoshioka M. Tandospirone suppresses impulsive action by possible blockade of the 5-HT1A receptor. J Pharmacol Sci. 2013;122(2):84-92

Tandospirone citrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.69mL

1.74mL

0.87mL

17.37mL

3.47mL

1.74mL

Tandospirone citrate 技术信息

CAS号112457-95-1
分子式C27H37N5O9
分子量575.611
别名 枸橼酸坦度螺酮 ;SM-3997 citrate
运输蓝冰
存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

H2O: 30 mg/mL(52.12 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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