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噻奈普汀

规格或纯度: ≥98%

CAS编号: 66981-73-5
分子式: C₂₁H₂₅ClN₂O₄S
分子量: 436.96
PubChem编号: 68870

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货号 (SKU)	包装规格	是否现货	价格	数量
T127334-5mg	5mg	现货
T127334-10mg	10mg	现货
T127334-50mg	50mg	现货
T127334-250mg	250mg	现货

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基本描述

规格或纯度	≥98%
英文名称	Tianeptine
别名	噻奈普汀
英文别名	dioxide; tianeptineacid; coaxil
生化机理	Tianeptine, a tricyclic compound, is a selective facilitator of 5-HT uptake in vitro and in vivo. Additionally, Tianeptine is reported to act as a selective inhibitor of dopamine uptake and is similar to amineptine. Tianeptine does not have a noted effect on monoamine uptake. In a study utilizing purified synaptosomes from rat brain, Tianeptine was reported to enhance serotonin uptake in selective brain regions. Purified synaptosomes were obtained from rats and incubated with tritium-labeled 5-H and Tianeptine in vitro . The synaptosomes were then analyzed for uptake and release of 5-HT via a liquid scintillation counter.
运输条件	常规运输
备注	卖完停产，不再备货
产品介绍	A selective facilitator of serotonin uptake. A selective facilitator of serotonin uptake.

名称和标识符

IUPAC Name	7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid
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)
InChi Key	JICJBGPOMZQUBB-UHFFFAOYSA-N
Canonical SMILES	CN1C2=CC=CC=C2C(C3=C(S1(=O)=O)C=C(C=C3)Cl)NCCCCCCC(=O)O
分子式	C₂₁H₂₅ClN₂O₄S
PubChem CID	68870
分子量	436.96

数据库链接

PubChem CID	68870
CAS Registry No.	66981-73-5
Wikipedia	Tianeptine
ChEMBL Ligand	CHEMBL1289110
DrugCentral Ligand	2650

化学和物理性质

溶解性	Soluble in Dichloromethane, Methanol and Water.

安全信息

象形图	Health Hazard
信号词	Warning
危险声明	H373: Causes damage to organs through prolonged or repeated exposure H361: Suspected of damaging fertility or the unborn child H362: May cause harm to breast-fed children
预防措施声明	P280,P405,P501,P264,P260,P270,P263,P203,P318,P319

关联配体

Ligand ID	7558
名称	tianeptine
别名	Stablon®
类别	Synthetic organic
学名	7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid
生物活性评价	In electrophysiology experiments using mouse hippocampal slices, 100 μM tianeptine increases the amplitude of isolated AMPA receptor mediated fEPSPs (field excitatory post-synaptic potentials) by approximately 163% after 60 min administration . As there appears to be no publicly available bioactivity data for this drug at its human molecular target(s) we have not mapped a primary drug target in this instance.
评价	Chemically tianeptine can be classified as a tricyclic antidepressant (TCA), but evidence suggests that it has a quite different pharmacological mechanism of action compared to typical TCAs .

参考文献

1. Kasper S, McEwen BS. (2008) Neurobiological and clinical effects of the antidepressant tianeptine.. CNS Drugs, 22 (1): (15-26). [PMID:18072812]
2. Svenningsson P, Bateup H, Qi H, Takamiya K, Huganir RL, Spedding M, Roth BL, McEwen BS, Greengard P. (2007) Involvement of AMPA receptor phosphorylation in antidepressant actions with special reference to tianeptine.. Eur J Neurosci, 26 (12): (3509-17). [PMID:18088278]
3. McEwen BS, Chattarji S. (2004) Molecular mechanisms of neuroplasticity and pharmacological implications: the example of tianeptine.. Eur Neuropsychopharmacol, 14 Suppl 5 (13): (S497-502). [PMID:15550348]
4. Brink CB, Harvey BH, Brand L. (2006) Tianeptine: a novel atypical antidepressant that may provide new insights into the biomolecular basis of depression.. Recent Pat CNS Drug Discov, 1 (1): (29-41). [PMID:18221189]
5. McEwen BS, Chattarji S, Diamond DM, Jay TM, Reagan LP, Svenningsson P, Fuchs E. (2010) The neurobiological properties of tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation.. Mol Psychiatry, 15 (3): (237-49). [PMID:19704408]
6. Szegedi V, Juhász G, Zhang X, Barkóczi B, Qi H, Madeira A, Kapus G, Svenningsson P, Spedding M, Penke B. (2011) Tianeptine potentiates AMPA receptors by activating CaMKII and PKA via the p38, p42/44 MAPK and JNK pathways.. Neurochem Int, 59 (8): (1109-22). [PMID:22056552]

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