噻奈普汀

**噻奈普汀**
臨床資料
商品名（英语：Drug nomenclature）	Stablon, Coaxil, others
其他名稱	S-1574; JNJ-39823277; TPI-1062
AHFS/Drugs.com	国际药品名称
给药途径	口服
ATC碼	N06AX14 (WHO) ;
法律規範狀態
法律規範	In general: Rx-only; US: not FDA approved, schedule 1 in MN, schedule 2 in OK, MI & AL; AU: S4; Others: controlled in FR, BH, SG);
藥物動力學數據
生物利用度	99%
血漿蛋白結合率	95%
药物代谢	Hepatic
生物半衰期	2.5–3 hours; 4–9 hours (elderly)
排泄途徑	尿：65%; 大便：15%
识别信息
	IUPAC命名法 7-[(3-Chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid; ;
CAS号	72797-41-2 ; 30123-17-2（钠盐）; 1224690-84-9（硫酸盐）
PubChem CID	68870;
IUPHAR/BPS	7558;
ChemSpider	62102 ;
UNII	0T493YFU8O;
KEGG	D02575 ;
ChEBI	CHEBI:91749;
ChEMBL	ChEMBL1289110 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID7048295 ;
ECHA InfoCard	100.069.844、100.131.750
化学信息
化学式	C21H25ClN2O4S
摩尔质量	436.95 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES Clc1cc2c(cc1)C(c3c(N(C)S2(=O)=O)cccc3)NCCCCCCC(=O)O;
	InChI InChI=1S/C21H24ClN2NaO4S/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) ; Key:JICJBGPOMZQUBB-UHFFFAOYSA-N ;

噻奈普汀是一种非典型抗抑郁药（英语：atypical antidepressant），主要用于重性抑郁疾患的治疗，也可以用来治疗焦虑、气喘和大肠激躁症。^[1]^[2]^[3]

噻奈普汀具有抗抑郁和抗焦虑作用，^[9]且镇静性、抗胆碱剂作用和心血管副作用相对较少。^[7]^[10]人们已发现它是μ-阿片受体（英语：μ-opioid receptor）的非典型激动剂，而对δ-阿片受体（英语：δ-opioid receptor）和κ-阿片受体（英语：κ-opioid receptor）的影响可忽略不计。^[11]^[12]^[13]

噻奈普汀由法国医学研究学会于1960年代发现并获得专利。今天，噻奈普汀在法国获得批准，由Laboratoires Servier（英语：Laboratoires Servier） SA生产和销售。它还在许多其它欧洲国家以商品名Coaxil，以及在亚洲（包括新加坡）和拉丁美洲以商品名Stablon和Tatinol销售，但噻奈普汀不在澳大利亚、加拿大、新西兰、英国或美国销售。^[14]^[15]

参考资料[编辑]

^ ^1.0 ^1.1 Elks J. The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014: 1195– [2022-03-03]. ISBN 978-1-4757-2085-3. （原始内容存档于2020-08-31）.
^ ^2.0 ^2.1 Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000: 1024– [2022-03-03]. ISBN 978-3-88763-075-1. （原始内容存档于2020-09-07）.
^ ^3.0 ^3.1 Tianeptine. [2022-03-03]. （原始内容存档于2012-01-25）.
^ Tianeptine – AdisInsight. AdisInsight. Springer. [31 January 2016]. （原始内容存档于2022-03-03）.
^ 存档副本. [2022-03-03]. （原始内容存档于2020-12-13）.
^ ^6.0 ^6.1 ^6.2 Royer RJ, Albin H, Barrucand D, Salvadori-Failler C, Kamoun A. Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors. Clinical Neuropharmacology. 1988, 11 (Suppl 2): S90–6. PMID 3180120.
^ ^7.0 ^7.1 ^7.2 ^7.3 ^7.4 ^7.5 ^7.6 Wagstaff AJ, Ormrod D, Spencer CM. Tianeptine: a review of its use in depressive disorders. CNS Drugs. March 2001, 15 (3): 231–59. PMID 11463130. doi:10.2165/00023210-200115030-00006.
^ Carlhant D, Le Garrec J, Guedes Y, Salvadori C, Mottier D, Riche C. Pharmacokinetics and bioavailability of tianeptine in the elderly. Drug Investigation. September 1990, 2 (3): 167–172. S2CID 56502717. doi:10.1007/BF03259191.
^ Defrance R, Marey C, Kamoun A. Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials (PDF). Clinical Neuropharmacology. 1988, 11 (Suppl 2): S74–82. PMID 2902922. （原始内容 (PDF)存档于4 April 2016）.
^ Kasper S, McEwen BS. Neurobiological and clinical effects of the antidepressant tianeptine. CNS Drugs. 2008, 22 (1): 15–26. PMID 18072812. S2CID 30330824. doi:10.2165/00023210-200822010-00002.
^ Gassaway MM, Rives ML, Kruegel AC, Javitch JA, Sames D. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. Translational Psychiatry. July 2014, 4 (7): e411. PMC 4119213 . PMID 25026323. doi:10.1038/tp.2014.30.
^ Berridge KC, Kringelbach ML. Affective neuroscience of pleasure: reward in humans and animals. Psychopharmacology. August 2008, 199 (3): 457–80. PMC 3004012 . PMID 18311558. doi:10.1007/s00213-008-1099-6.
^ El Zahran T, Schier J, Glidden E, Kieszak S, Law R, Bottei E, et al. Characteristics of Tianeptine Exposures Reported to the National Poison Data System - United States, 2000-2017. MMWR. Morbidity and Mortality Weekly Report. August 2018, 67 (30): 815–818. PMC 6072055 . PMID 30070980. doi:10.15585/mmwr.mm6730a2.
^ Akiki T. The etiology of depression and the therapeutic implications. Glob. J. Med. Res. [2022-03-03]. ISSN 2249-4618. （原始内容存档于2016-11-03）.
^ Tianeptine Sodium. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). 5 December 2011 [2 December 2013].

[Elks2014-1] 1.0 ^1.1 Elks J. The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014: 1195– [2022-03-03]. ISBN 978-1-4757-2085-3. （原始内容存档于2020-08-31）.

[IndexNominum2000-2] 2.0 ^2.1 Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000: 1024– [2022-03-03]. ISBN 978-3-88763-075-1. （原始内容存档于2020-09-07）.

[Drugs.com-3] 3.0 ^3.1 Tianeptine. [2022-03-03]. （原始内容存档于2012-01-25）.

[AdisInsight-4] Tianeptine – AdisInsight. AdisInsight. Springer. [31 January 2016]. （原始内容存档于2022-03-03）.

[5] 存档副本. [2022-03-03]. （原始内容存档于2020-12-13）.

[pmid3180120-6] 6.0 ^6.1 ^6.2 Royer RJ, Albin H, Barrucand D, Salvadori-Failler C, Kamoun A. Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors. Clinical Neuropharmacology. 1988, 11 (Suppl 2): S90–6. PMID 3180120.

[Tian2001-7] 7.0 ^7.1 ^7.2 ^7.3 ^7.4 ^7.5 ^7.6 Wagstaff AJ, Ormrod D, Spencer CM. Tianeptine: a review of its use in depressive disorders. CNS Drugs. March 2001, 15 (3): 231–59. PMID 11463130. doi:10.2165/00023210-200115030-00006.

[CarlhantLeGarrec1990-8] Carlhant D, Le Garrec J, Guedes Y, Salvadori C, Mottier D, Riche C. Pharmacokinetics and bioavailability of tianeptine in the elderly. Drug Investigation. September 1990, 2 (3): 167–172. S2CID 56502717. doi:10.1007/BF03259191.

[pmid2902922-9] Defrance R, Marey C, Kamoun A. Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials (PDF). Clinical Neuropharmacology. 1988, 11 (Suppl 2): S74–82. PMID 2902922. （原始内容 (PDF)存档于4 April 2016）.

[CNS2008-10] Kasper S, McEwen BS. Neurobiological and clinical effects of the antidepressant tianeptine. CNS Drugs. 2008, 22 (1): 15–26. PMID 18072812. S2CID 30330824. doi:10.2165/00023210-200822010-00002.

[pmid25026323-11] Gassaway MM, Rives ML, Kruegel AC, Javitch JA, Sames D. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. Translational Psychiatry. July 2014, 4 (7): e411. PMC 4119213 . PMID 25026323. doi:10.1038/tp.2014.30.

[12] Berridge KC, Kringelbach ML. Affective neuroscience of pleasure: reward in humans and animals. Psychopharmacology. August 2008, 199 (3): 457–80. PMC 3004012 . PMID 18311558. doi:10.1007/s00213-008-1099-6.

[pmid30070980-13] El Zahran T, Schier J, Glidden E, Kieszak S, Law R, Bottei E, et al. Characteristics of Tianeptine Exposures Reported to the National Poison Data System - United States, 2000-2017. MMWR. Morbidity and Mortality Weekly Report. August 2018, 67 (30): 815–818. PMC 6072055 . PMID 30070980. doi:10.15585/mmwr.mm6730a2.

[akiki-14] Akiki T. The etiology of depression and the therapeutic implications. Glob. J. Med. Res. [2022-03-03]. ISSN 2249-4618. （原始内容存档于2016-11-03）.

[MD-15] Tianeptine Sodium. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). 5 December 2011 [2 December 2013].

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]

[12]

[13]

[14]

[15]