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Tianeptine/噻奈普汀 {[allProObj[0].p_purity_real_show]}

货号:A173481 同义名: 噻萘普汀

Tianeptine is a unique tricyclic antidepressant, in contrast to SSRIs, which can increase serotonin uptake in the brain and reduce stress-induced atrophy of neuronal dendrites.

Tianeptine/噻奈普汀 化学结构 CAS号:72797-41-2
Tianeptine/噻奈普汀 化学结构
CAS号:72797-41-2
Tianeptine/噻奈普汀 3D分子结构
CAS号:72797-41-2
Tianeptine/噻奈普汀 化学结构 CAS号:72797-41-2
Tianeptine/噻奈普汀 3D分子结构 CAS号:72797-41-2
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Tianeptine/噻奈普汀 纯度/质量文件 产品仅供科研

货号:A173481 标准纯度: {[allProObj[0].p_purity_real_show]}
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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-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

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 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 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-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 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-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

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。

Tianeptine/噻奈普汀 生物活性

描述 Tianeptine, as an atypical antidepressant, reduces the survival and norepinephrine secretion of PC12 cells. Tianeptine treatment decreased high K+-stimulated secretion of norepinephrine and chromogranin A in PC12 cells and of epinephrine in the mouse pheochromocytoma MPC cells[3]. Tianeptine as an efficacious MOR (μ-opioid receptor ) agonist (Ki Human of 383±183 nM and EC50 Human of 194±70 nM  and EC50 Mouse of 641±120 nM for G-protein activation)[4]. Tianeptine (ED50=15) showed a less potent analgesic response compared to morphine (ED50=3.1). Studies showed the acute and chronic antidepressant-like behavioral effects of tianeptine in mice require MOR[5].

Tianeptine/噻奈普汀 参考文献

[1]Lee H, Im J, et al. Effects of tianeptine on symptoms of fibromyalgia via BDNF signaling in a fibromyalgia animal model. Korean J Physiol Pharmacol. 2017 Jul;21(4):361-370.

[2]Broqua P, Baudrie V, Chaouloff F. Differential effects of the novel antidepressant tianeptine on L-5-hydroxytryptophan (5-HTP)-elicited corticosterone release and body weight loss. Eur Neuropsychopharmacol. 1992 Jun;2(2):115-20.

[3]Makani V, Hall J, Qamar K, Jain P, Jang Y, Hensley K, Park JJ. Tianeptine interferes with microtubule organization and hormone secretion of pheochromocytoma cells. Mol Cell Endocrinol. 2013 Dec 5;381(1-2):175-87. doi: 10.1016/j.mce.2013.07.033. Epub 2013 Aug 7. PMID: 23933152; PMCID: PMC3796025.

[4]Gassaway MM, Rives ML, Kruegel AC, Javitch JA, Sames D. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. Transl Psychiatry. 2014 Jul 15;4(7):e411. doi: 10.1038/tp.2014.30. PMID: 25026323; PMCID: PMC4119213.

[5]Samuels BA, Nautiyal KM, Kruegel AC, Levinstein MR, Magalong VM, Gassaway MM, Grinnell SG, Han J, Ansonoff MA, Pintar JE, Javitch JA, Sames D, Hen R. The Behavioral Effects of the Antidepressant Tianeptine Require the Mu-Opioid Receptor. Neuropsychopharmacology. 2017 Sep;42(10):2052-2063. doi: 10.1038/npp.2017.60. Epub 2017 Mar 17. PMID: 28303899; PMCID: PMC5561344.

Tianeptine/噻奈普汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.44mL

2.29mL

1.14mL

22.89mL

4.58mL

2.29mL

Tianeptine/噻奈普汀 技术信息

CAS号72797-41-2
分子式C21H25ClN2O4S
分子量 436.95
SMILES Code O=C(O)CCCCCCNC(C1=CC=C(Cl)C=C12)C3=CC=CC=C3N(C)S2(=O)=O
MDL No. MFCD00865376
别名 噻萘普汀
运输蓝冰
InChI Key JICJBGPOMZQUBB-UHFFFAOYSA-N
Pubchem ID 68870
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

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