| 生物活性： |
靶点：Opioid Receptor
通路：GPCR & G Protein;Neuronal Signaling
背景说明：是一种μ-opioid receptor激动剂。
生物活性：Tianeptine 是一种选择性的 5-HT 的摄取促进剂。[1]
In Vitro：Using radioligand binding and cell-based functional assays，including bioluminescence resonance energy transfer-based assays for G-protein activation and cAMP accumulation，we identified tianeptine as an efficacious MOR 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). Tianeptine was also a full δ-opioid receptor(DOR)agonist，although with much lower potency(EC50 Human of 37.4±11.2 μM and EC50 Mouse of 14.5±6.6 μM for G-protein activation). [1]
In Vivo：Administration of 5-HTP(20 mg/kg i.v.)increased plasma corticosterone levels to a similar extent in rats pretreated either with saline or tianeptine(10 mg/kg i.p.，60 min beforehand). Tianeptine preferentially activates 5-HT reuptake in central serotonergic neurones.[1]
数据来源文献：[1]. Broqua P，et al. 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.
[2]. 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.
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| 其它标识： |
MDL：MFCD00865376
SMILES：CN1C2=CC=CC=C2C(C3=C(S1(=O)=O)C=C(C=C3)Cl)NCCCCCCC(=O)O
InChIKey：JICJBGPOMZQUBB-UHFFFAOYSA-N
InChI：InChI=1S/C21H25ClN2O4S/c1-24-18-9-6-5-8-16(18)21(23-13-7-3-2-4-10-20(25)26)17-12-11-15(22)14-19(17)29(24，27)28/h5-6，8-9，11-12，14，21，23H，2-4，7，10，13H2，1H3，(H，25，26)
PubChem CID：68870
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| 基本信息： |
CAS：72797-41-2
中文名称：噻萘普汀
英文名称：Tianeptine
别名：S-1574;JNJ-39823277;TPI-1062
分子式：C21H25ClN2O4S
分子量：436.95
规格：25mg
溶解性：Soluble in DMSO(Need ultrasonic)
纯度：≥98%
外观(性状)：White to off-white Solid
储存条件：Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
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| 靶点： |
Opioid Receptor |
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