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https://www.readbyqxmd.com/read/28742625/online-sales-of-unscheduled-pharmaceutical-agents-a-case-report-of-tianeptine-use-in-the-united-states
#1
Swapnil Gupta, Ryan Wallace, Jordan Sloshower
: Tianeptine is a tricyclic antidepressant that stimulates mu-opioid receptors at high doses. It is marketed and used across Europe and Latin America as an antidepressant, but is not approved by the Food and Drug Administration for use in the United States. In the United States, tianeptine is sold through online health stores as a cognition enhancer, dietary supplement, or as research chemical. We report the case of a 36-year-old man with a history of major depressive disorder, responsive to sertraline, who turned to the unmonitored use of tianeptine purchased online to treat residual feelings of apathy and boredom...
July 24, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28706449/effects-of-tianeptine-on-symptoms-of-fibromyalgia-via-bdnf-signaling-in-a-fibromyalgia-animal-model
#2
Hwayoung Lee, Jiyun Im, Hansol Won, Wooyoung Nam, Young Ock Kim, Sang Won Lee, Sanghyun Lee, Ik-Hyun Cho, Hyung-Ki Kim, Jun-Tack Kwon, Hak-Jae Kim
Previous reports have suggested that physical and psychological stresses may trigger fibromyalgia (FM). Stress is an important risk factor in the development of depression and memory impairments. Antidepressants have been used to prevent stress-induced abnormal pain sensation. Among various antidepressants, tianeptine has been reported to be able to prevent neurodegeneration due to chronic stress and reverse decreases in hippocampal volume. To assess the possible effect of tianeptine on FM symptoms, we constructed a FM animal model induced by restraint stress with intermittent cold stress...
July 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/28541419/acute-toxicity-from-intravenous-use-of-the-tricyclic-antidepressant-tianeptine
#3
Sara K Dempsey, Justin L Poklis, Kacie Sweat, Kirk Cumpston, Carl E Wolf
Tianeptine (7-[([3-chloro-6,11]-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl) amino] heptanoic acid S, S dioxide) is a tricyclic compound prescribed as an antidepressant in European countries, but is not currently approved for use in the United States. There are few published case reports of tianeptine intoxication. Presented is the first case of acute toxicity associated with the intravenous use of tianeptine. A 36-year-old male intentionally injected tianeptine powder intravenously to "help him see into the future"...
May 24, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28535568/tianeptine-reduces-mechanical-allodynia-in-spinal-nerve-ligated-and-chemotherapy-induced-neuropathic-mice
#4
Seong Min Han, Young Hoon Kim, Hyeon Uk Jo, Jung Ah Kwak, Hue Jung Park
BACKGROUND: Spinal nerve-ligated neuropathy and chemotherapy-induced neuropathy produce a persistent tactile allodynia in mice. Tianeptine is an antidepressant that exhibits structural similarities to tricyclic antidepressants but has distinct neurochemical properties. OBJECTIVE: Here we examined the effects of intraperitoneal (i.p.) tianeptine on allodynia in spinal nerve-ligated and chemotherapy-induced neuropathic mice. STUDY DESIGN: A randomized, experimental trial...
May 2017: Pain Physician
https://www.readbyqxmd.com/read/28450192/do-the-accelerating-actions-of-tianeptine-and-l-arginine-on-cortical-spreading-depression-interact-an-electrophysiological-analysis-in-young-and-adult-rats
#5
Luciana Maria Silva de Seixas Maia, Angela Amancio-Dos-Santos, Paula Catirina Pereira da Silva Germano, Anna Carolina Santos Marinho Falcão, Desirré Duda-de-Oliveira, Rubem Carlos Araújo Guedes
In the rat, we previously demonstrated that serotonin-enhancing drugs impair cortical spreading depression (CSD) and that l-arginine (arginine) treatment enhances CSD. Here, we investigated the interaction between topical application of the serotonin uptake enhancer tianeptine and systemic arginine administration on CSD. From postnatal day 7-28, female Wistar rats (n=40) received by gavage 300mg/Kg/day arginine (n=20) or water (n=20). Half of the arginine- or water-treated rats underwent CSD recording at 30-40days of age (young), while the other half was recorded at 90-120days (adult)...
April 25, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28362353/ergosteryl-2-naphthoate-an-ergosterol-derivative-exhibits-antidepressant-effects-mediated-by-the-modification-of-gabaergic-and-glutamatergic-systems
#6
Mingzhu Lin, Haijun Li, Yan Zhao, Enbo Cai, Hongyan Zhu, Yugang Gao, Shuangli Liu, He Yang, Lianxue Zhang, Guosheng Tang, Ruiqing Wang
Phytosterols are a kind of natural component including sitosterol, campesterol, avenasterol, ergosterol (Er) and others. Their main natural sources are vegetable oils and their processed products, followed by grains, by-products of cereals and nuts, and small amounts of fruits, vegetables and mushrooms. In this study, three new Er monoester derivatives were obtained from the reflux reaction with Er: organic acids (furoic acid, salicylic acid and 2-naphthoic acid), 1-Ethylethyl-3-(3-dimethyllaminopropyl) carbodiimide hydrochloride (EDCI) and 4-dimethylaminopyridine (DMAP) in dichloromethane...
March 31, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28359918/the-effects-of-desipramine-fluoxetine-or-tianeptine-on-changes-in-bulbar-bdnf-levels-induced-by-chronic-social-instability-stress-and-inflammation
#7
Marta M Nowacka-Chmielewska, Daniela Kasprowska, Monika Paul-Samojedny, Anna M Bielecka-Wajdman, Jarosław J Barski, Andrzej Małecki, Ewa Obuchowicz
BACKGROUND: Stress is a major predisposing factor in the development of psychiatric disorders and potential source of augmented inflammatory processes in the brain. Increasing body of evidence shows an important role of alterations in the olfactory bulbs (OBs) function in stress-related disorders. The aim of the present study was to investigate the impact of antidepressants on the alterations of brain-derived neurotrophic factor (BDNF) induced by lipopolysaccharide (LPS) in female rats subjected to chronic social instability stress (CSIS)...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28352358/alterations-in-vegf-expression-induced-by-antidepressant-drugs-in-female-rats-under-chronic-social-stress
#8
Marta Maria Nowacka-Chmielewska, Monika Paul-Samojedny, Anna Maria Bielecka-Wajdman, Jarosław Jerzy Barski, Ewa Obuchowicz
Vascular endothelial growth factor (VEGF) is thought to serve a role in neurogenesis and the stress response. Although a definite link between the action of antidepressants and VEGF has not been identified, it is assumed that VEGF, as a neurotrophic factor, serves an important role in the effects of antidepressant treatment. To examine this, the present study subjected adult female rats to four weeks of social instability stress and measured the effect of antidepressant treatment on the expression of VEGF. Firstly, endocrine markers of stress and body weight were measured in parallel with behavioral tests prior to and following subjection to stress...
February 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28303899/the-behavioral-effects-of-the-antidepressant-tianeptine-require-the-mu-opioid-receptor
#9
Benjamin Adam Samuels, Katherine M Nautiyal, Andrew C Kruegel, Marjorie R Levinstein, Valerie M Magalong, Madalee M Gassaway, Steven G Grinnell, Jaena Han, Michael A Ansonoff, John E Pintar, Jonathan A Javitch, Dalibor Sames, René Hen
Depression is a debilitating chronic illness that affects around 350 million people worldwide. Current treatments, such as selective serotonin reuptake inhibitors, are not ideal because only a fraction of patients achieve remission. Tianeptine is an effective antidepressant with a previously unknown mechanism of action. We recently reported that tianeptine is a full agonist at the mu opioid receptor (MOR). Here we demonstrate that the acute and chronic antidepressant-like behavioral effects of tianeptine in mice require MOR...
April 19, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28223757/attenuation-of-dickkopf-1-induced-hair-growth-inhibition-in-cultured-human-hair-follicles-by-tianeptine
#10
Hyun Sik Jeong, Mi Hee Kwack, Moon Kyu Kim, Jung Chul Kim, Young Kwan Sung
No abstract text is available yet for this article.
February 2017: Annals of Dermatology
https://www.readbyqxmd.com/read/28081469/anti-osteoporotic-effects-of-an-antidepressant-tianeptine-on-ovariectomized-rats
#11
Osama A Alkhamees, Abdulaziz S Al-Roujayee, Hatem M Abuohashish, Mohammed M Ahmed
In the current investigation, the potential alleviating effects of tianeptine against bone loss induced in ovariectomized (OVX) rats was determined. Two weeks following a bilateral ovariectomy operation, tianeptine treatment (12.5 and 25mg/kg/twice/d) was initiated and continued for twenty-eight consecutive days. Changes in serum and urinary bone turnover biomarkers and osteoclastogenesis-inducing factors were estimated. The femoral bone mineral content was estimated using inductively-coupled-plasma mass spectrometry...
March 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28063625/regulation-of-insulin-receptor-phosphorylation-in-the-brains-of-prenatally-stressed-rats-new-insight-into-the-benefits-of-antidepressant-drug-treatment
#12
Katarzyna Głombik, Joanna Ślusarczyk, Ewa Trojan, Katarzyna Chamera, Bogusława Budziszewska, Władysław Lasoń, Agnieszka Basta-Kaim
A growing body of evidence supports the involvement of disturbances in the brain insulin pathway in the pathogenesis of depression. On the other hand, data concerning the impact of antidepressant drug therapy on brain insulin signaling remain scare and insufficient. We determinated the influence of chronic treatment with antidepressant drugs (imipramine, fluoxetine and tianeptine) on the insulin signaling pathway of the brain of adult prenatally stressed rats. 3-month-old prenatally stressed and control rats were treated for 21 days with imipramine, fluoxetine or tianeptine (10mg/kg/day i...
February 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27862243/antidepressant-adherence-patterns-in-older-patients-use-of-a-clustering-method-on-a-prescription-database
#13
David Braunstein, Amélie Hardy, Quentin Boucherie, Elisabeth Frauger, Olivier Blin, Gaétan Gentile, Joëlle Micallef
According to the World Health Organization, depression will become the second most important cause of disability worldwide by 2020. Our objective was to identify patterns of adherence to antidepressant treatments in older patients using several indicators of adherence and to characterize these patterns in terms of medication exposure. We conducted a retrospective cohort study using the French National Health Insurance reimbursement database. Incident antidepressant users aged more than 65 were included from July 1, 2010, to June 30, 2011, and followed up for 18 months...
April 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27641318/effects-of-tianeptine-on-the-development-and-maintenance-of-mechanical-allodynia-in-a-rat-model-of-neuropathic-pain
#14
Bong Ha Heo, Jae Yun Shin, Keun Suk Park, Hyung Gon Lee, Jeong Il Choi, Myung Ha Yoon, Woong Mo Kim
We validate the analgesic efficacy of tianeptine by different administration routes and timing in a rat model of neuropathic pain. Neuropathic pain was induced by ligating the L5 and L6 spinal nerves in male Sprague-Dawley rats, and mechanical allodynia was assessed using von Frey filaments. The effects of orally administered tianeptine and pretreatment with tianeptine (intrathecally or intraperitoneally) on mechanical allodynia were assessed. Oral and preemptive intrathecal administration of tianeptine significantly increased the paw withdrawal threshold but preemptive intraperitoneal administration did not...
October 28, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27626082/effect-of-tianeptine-on-depressed-tinnitus-patients
#15
Soo Min Hwang, Sae Hee Lim, Dong Ju Oh, Sung Kyun Kim, Hak Hyun Jung, Gi Jung Im
BACKGROUND AND OBJECTIVES: Tianeptine is a tricyclic antidepressant that has a novel pharmacological property: it increases the reuptake of 5-hydroxytryptamine. Recent studies have reported that the prevalence of depression is greater in patients with tinnitus than in control subjects who do not have tinnitus. The purpose of this study was to assess the efficacy of tianeptine for the relief of tinnitus, especially in patients with depressive mood. SUBJECTS AND METHODS: Among a total of 52 tinnitus patients, 15 had depressive mood...
September 2016: Journal of Audiology & Otology
https://www.readbyqxmd.com/read/27604299/differential-effects-of-tianeptine-on-the-dorsal-hippocampal-volume-of-rats-submitted-to-maternal-separation-followed-by-chronic-unpredictable-stress-in-adulthood
#16
Antonella Pollano, María I Zalosnik, Patricia E Durando, Marta M Suárez
Early maternal separation (MS) may produce lasting effects in the dorsal hippocampus (DH) that can change its response to chronic stress in adulthood. Chronic stress affects DH morphology and function, but tianeptine (an anti-depressant) can reverse the stress-induced morphological impairments. Morphologic alterations of hippocampus can affect contextual memory. Therefore, we evaluated the effect of tianeptine in MS and chronically stressed rats, on: 1) volume of the DH and its areas using stereology, and 2) hippocampal dependent memory using a fear conditioning test...
September 8, 2016: Stress: the International Journal on the Biology of Stress
https://www.readbyqxmd.com/read/27561095/anticonvulsant-activity-of-the-antidepressant-drug-tianeptine-against-pentylenetetrazole-induced-seizures-mitigates-cognitive-impairment-in-rats
#17
Kh Reeta, Pankaj Prabhakar, Yogendra K Gupta
Treatment of depression, a common comorbidity in patients with epilepsy, is restricted as certain antidepressants are considered to be proconvulsants. In contrast, anticonvulsant effects have been reported with some antidepressants. In the present study, the effect of tianeptine, an antidepressant, was evaluated against pentylenetetrazole (PTZ)-induced seizures, cognitive impairment and oxidative stress in rats. Tianeptine was administered in three doses (20, 40 and 80 mg/kg) 30 min before PTZ (60 mg/kg, intraperitoneally)...
October 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27392529/novel-series-of-tacrine-tianeptine-hybrids-synthesis-cholinesterase-inhibitory-activity-s100b-secretion-and-a-molecular-modeling-approach
#18
Marco Antonio Ceschi, Jessie Sobieski da Costa, João Paulo Bizarro Lopes, Viktor Saraiva Câmara, Leandra Franciscato Campo, Antonio César de Amorim Borges, Carlos Alberto Saraiva Gonçalves, Daniela Fraga de Souza, Eduardo Luis Konrath, Ana Luiza Martins Karl, Isabella Alvim Guedes, Laurent Emmanuel Dardenne
Tianeptine was linked to various 9-aminoalkylamino-1,2,3,4-tetrahydroacridines using EDC·HCl/HOBt to afford a series of tacrine-tianeptine hybrids. The hybrids were tested for their ability to inhibit AChE and BuChE and IC50 values in the nanomolar concentration scale were obtained. AChE molecular modeling studies of these hybrids indicated that tacrine moiety interacts in the bottom of the gorge with the catalytic active site (CAS) while tianeptine binds to peripheral anionic site (PAS). Furthermore, the compounds 2g and 2e were able to reduce the in vitro basal secretion of S100B, suggesting its therapeutic action in some cases or stages of Alzheimer's disease...
October 4, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27378793/neurotrophin-genes-and-antidepressant-worsening-suicidal-ideation-a-prospective-case-control-study
#19
Géraldine Voegeli, Nicolas Ramoz, Tatyana Shekhtman, Philippe Courtet, Philip Gorwood, John R Kelsoe
BACKGROUND: Antidepressant-worsening suicidal ideation is a rare but serious phenomenon. This study aimed to test for association between antidepressant-worsening suicidal ideation and polymorphisms of BDNF/NTRK2 neurotrophin pathway genes, known to be involved in depression and suicide. METHODS: This was a case-control study comparing patients with antidepressant-worsening suicidal ideation to patients without. Patients were collected from the GENESE cohort (3771 depressed tianeptine-treated outpatients)...
November 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27371898/traxoprodil-augments-the-antidepressant-like-activity-of-agomelatine-but-not-of-mianserin-or-tianeptine-in-the-forced-swim-test-in-mice
#20
Weronika Stasiuk, Anna Serefko, Aleksandra Szopa, Elżbieta Wyska, Katarzyna Świąder, Piotr Wlaź, Ewa Poleszak
BACKGROUND: The main objective of our study was to evaluate the influence of traxoprodil on the activity of the atypical antidepressant drugs (agomelatine, mianserin, tianeptine). METHODS: The forced swim test (FST) in mice was used to determine the antidepressant-like activity of the tested agents. Drugs levels in brain tissue were assessed by a high performance liquid chromatography method. RESULTS: Concurrent intraperitoneal administration of per se ineffective doses of traxoprodil (10mg/kg) and agomelatine (20mg/kg) shortened the immobility time of animals in the FST...
October 2016: Pharmacological Reports: PR
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