Tianeptine

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Chemical Structure| 72797-41-2 同义名 : 噻萘普汀
CAS号 : 72797-41-2
货号 : A173481
分子式 : C21H25ClN2O4S
纯度 : 99%
分子量 : 436.95
MDL号 : MFCD00865376
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
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

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.