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desipramine

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https://www.readbyqxmd.com/read/29161812/acute-amino-acid-d-serine-administration-similar-to-ketamine-produces-antidepressant-like-effects-through-the-identical-mechanisms
#1
I-Hua Wei, Kuang-Ti Chen, Mang-Hung Tsai, Ching-Hsiang Wu, Hsien-Yuan Lane, Chih-Chia Huang
D-serine is an amino acid and can work as an agonist at the glycine sites of N-methyl-D-aspartate receptor (NMDAR). Interestingly, both types of glutamatergic modulators, NMDAR enhancers and blockers, can improve depression through common targets, namely alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionaic acid receptors (AMPARs) and mammalian target of rapamycin (mTOR). To elucidate the cellular signaling pathway underlying this counterintuitive observation, we activated NMDARs in rats by using D-serine. Saline, ketamine (NMDAR antagonist), and desipramine (tricyclic antidepressant) were used as controls...
November 22, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29136551/efficient-and-relatively-safe-emulsification-microextraction-using-a-deep-eutectic-solvent-for-influential-enrichment-of-trace-main-anti-depressant-drugs-from-complicated-samples
#2
Ahmad Ghoochani Moghadam, Maryam Rajabi, Alireza Asghari
In this research work, an efficient, facile, prompt, and relatively safe enrichment procedure, named as air agitated-emulsification microextraction based on a low density-deep eutectic solvent (AA-EME-LD-DES), was applied for the first time to separate trace amounts of the drugs escitalopram, desipramine, and imipramine from complex sample solutions. This bio-degradable and cheap choline chloride-based extracting agent was readily prepared by the easy blending process at the ambient temperature, resulting in a eutectic liquid mixture with distinct features...
September 28, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29134326/inhibition-of-the-voltage-dependent-k-current-by-the-tricyclic-antidepressant-desipramine-in-rabbit-coronary-arterial-smooth-muscle-cells
#3
Sung Eun Shin, Hongliang Li, Jin Ryeol An, Mi Seon Seo, Sung Hun Na, Won-Kyo Jung, Amy L Firth, Kwon-Soo Ha, Eun-Taek Han, Seok-Ho Hong, Il-Whan Choi, Won Sun Park
We describe the effect of a tricyclic antidepressant drug desipramine on voltage-dependent K(+) (Kv) currents in freshly isolated rabbit coronary arterial smooth muscle cells using a conventional whole-cell patch clamp technique. Application of desipramine rapidly decreased the Kv current amplitude in a concentration-dependent manner, with an IC50 value of 5.91 ± 0.18 μM and a Hill coefficient of 0.61 ± 0.09. The steady-state inactivation curves of the Kv channels were not affected by desipramine. However, desipramine shifted the steady-state inactivation curves toward a more negative potential...
November 13, 2017: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/29129597/cocaine-and-desipramine-elicit-distinct-striatal-noradrenergic-and-behavioral-responses-in-selectively-bred-obesity-resistant-and-obesity-prone-rats
#4
Peter J Vollbrecht, Kathryn M Nesbitt, Omar S Mabrouk, Aaron M Chadderdon, Emily M Jutkiewicz, Robert T Kennedy, Carrie R Ferrario
Previous studies have demonstrated a role for norepinephrine (NE) in energy regulation and feeding, and basal differences have been observed in hypothalamic NE systems in obesity-prone vs. obesity-resistant rats. Differences in the function of brain reward circuits, including in the nucleus accumbens (NAc), have been shown in obesity-prone vs. obesity-resistant populations, leading many researchers to explore the role of striatal dopamine in obesity. However, alterations in NE transmission also affect NAc mediated behaviors...
November 9, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29068103/desipramine-induced-lysosomal-vacuolization-is-independent-of-autophagy
#5
Hirofumi Sawai
Desipramine, a commonly used antidepressant drug, induced cytosolic vacuolization in L929 cells. The level of LC3-II was elevated and that of p62 was reduced in desipramine-treated L929 cells, indicating the induction of autophagy by desipramine. Surprisingly, massive vacuolization was observed in desipramine-treated L929 cells in the presence of LY294002, an inhibitor of autophagy. On the other hand, bafilomycin A1, an inhibitor of vacuolar type H(+) ATPase, almost completely inhibited vacuolization in desipramine- or desipramine/LY294002-treated L929 cells...
October 25, 2017: Cell Biology International
https://www.readbyqxmd.com/read/29054969/%C3%AE-mangostin-protects-against-high-glucose-induced-apoptosis-of-human-umbilical-vein-endothelial-cells
#6
Yanli Luo, Minxiang Lei
Diabetic vascular complications result from high glucose -induced vascular endothelial cell dysfunction. There is an emerging need for novel drugs with vascular endothelial cell -protective effects for the treatment of diabetic vascular complications. This study aimed to investigate the protective effect of α-mangostin against high-glucose-induced apoptosis of cultured human umbilical vein endothelial cells (HUVECs). HUVECs were treated with glucose to induce apoptosis. The expression of the apoptosis-related proteins, Bcl-2, Bax and cleaved caspase-3, were detected by Western blotting...
October 20, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/29044198/transgenic-mice-lacking-creb-and-crem-in-noradrenergic-and-serotonergic-neurons-respond-differently-to-common-antidepressants-on-tail-suspension-test
#7
Katarzyna Rafa-Zabłocka, Grzegorz Kreiner, Monika Bagińska, Justyna Kuśmierczyk, Rosanna Parlato, Irena Nalepa
Evidence exists that chronic antidepressant therapy enhances CREB levels and activity. Nevertheless, the data are not conclusive, as previous analysis of transgenic mouse models has suggested that CREB inactivation in fact contributes to antidepressant-like behavior. The aim of this study was to evaluate the role of CREB in this context by exploiting novel transgenic mouse models, characterized by selective ablation of CREB restricted to noradrenergic (Creb1(DBHCre)/Crem-/-) or serotonergic (Creb1(TPH2CreERT2)/Crem-/-) neurons in a CREM-deficient background to avoid possible compensatory effects of CREM...
October 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29038231/evaluation-of-clinical-drug-interaction-potential-of-clofazimine-using-static-and-dynamic-modeling-approaches
#8
Ramachandra Sangana, Helen Gu, Dung Yu Chun, Heidi J Einolf
The 2016 World Health Organization treatment recommendations for drug-resistant tuberculosis (DR-TB) positioned clofazimine as a core second-line drug. Being identified as a cytochrome P450 (CYP) inhibitor in vitro, a CYP-mediated drug interaction may be likely when clofazimine is co-administered with substrates of these enzymes. The CYP-mediated drug interaction potential of clofazimine was evaluated using both static (estimation of "R1" and area under the plasma concentration-time curve ratio [AUCR] values) and dynamic (physiologically based pharmacokinetic [PBPK]) modeling approaches...
October 16, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29030399/robust-lysosomal-calcium-signaling-through-channel-trpml1-is-impaired-by-lysosomal-lipid-accumulation
#9
Néstor Más Gómez, Wennan Lu, Jason C Lim, Kirill Kiselyov, Keith E Campagno, Yulia Grishchuk, Susan A Slaugenhaupt, Bruce A Pfeffer, Steven J Fliesler, Claire H Mitchell
The transient receptor potential cation channel mucolipin 1 (TRPML1) channel is a conduit for lysosomal calcium efflux, and channel activity may be affected by lysosomal contents. The lysosomes of retinal pigmented epithelial (RPE) cells are particularly susceptible to build-up of lysosomal waste products because they must degrade the outer segments phagocytosed daily from adjacent photoreceptors; incomplete degradation leads to accumulation of lipid waste in lysosomes. This study asks whether stimulation of TRPML1 can release lysosomal calcium in RPE cells and whether such release is affected by lysosomal accumulations...
October 13, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28987282/antidepressants-promote-formation-of-heterocomplexes-of-dopamine-d2-and-somatostatin-subtype-5-receptors-in-the-mouse-striatum
#10
Kinga Szafran-Pilch, Agata Faron-Górecka, Magdalena Kolasa, Dariusz Żurawek, Marta Szlachta, Joanna Solich, Maciej Kuśmider, Marta Dziedzicka-Wasylewska
The interaction between the dopaminergic and somatostatinergic systems is considered to play a potential role in mood regulation. Chronic administration of antidepressants influences release of both neurotransmitters. The molecular basis of the functional cooperation may stem from the physical interaction of somatostatin receptor subtypes and dopamine D2 receptors since they colocalize in striatal interneurons and were shown to undergo ligand-dependent heterodimerization in heterologous expression systems. In present study we adapted in situ proximity ligation assay to investigate the occurrence of D2-Sst5 receptor heterocomplexes, and their possible alterations in the striatum of mice treated acutely and repeatedly (21days) with antidepressant drugs of different pharmacological profiles (escitalopram and desipramine)...
October 5, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28955042/acid-sphingomyelinase-inhibition-prevents-development-of-sepsis-sequelae-in-the-murine-liver
#11
Ha-Yeun Chung, C Julius Witt, Nayla Jbeily, Jorge Hurtado-Oliveros, Benjamin Giszas, Amelie Lupp, Markus H Gräler, Tony Bruns, Andreas Stallmach, Falk A Gonnert, Ralf A Claus
The molecular mechanisms of maladaptive response in liver tissue with respect to the acute and post-acute phase of sepsis are not yet fully understood. Long-term sepsis survivors might develop hepatocellular/hepatobiliary injury and fibrosis. Here, we demonstrate that acid sphingomyelinase, an important regulator of hepatocyte apoptosis and hepatic stellate cell (HSC) activation, is linked to the promotion of liver dysfunction in the acute phase of sepsis as well as to fibrogenesis in the long-term. In both phases, we observed a beneficial effect of partial genetic sphingomyelinase deficiency in heterozygous animals (smpd1(+/-)) on oxidative stress levels, hepatobiliary function, macrophage infiltration and on HSC activation...
September 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28916331/depressive-like-phenotype-induced-by-prenatal-dexamethasone-in-mice-is-reversed-by-desipramine
#12
Mirko Conti, Stefan Spulber, Marilena Raciti, Sandra Ceccatelli
Exposure to prenatal insults has been associated with an increased risk for neuropsychiatric disorders, including depression, but the mechanisms are still poorly understood. Persistent alterations of the HPA axis feedback mechanism as well as adult impaired neurogenesis are believed to play a relevant role in the etiology of depression. In addition, growing evidence points at epigenetic reprogramming as a key factor. We have previously shown that prenatal exposure to the synthetic glucocorticoid dexamethasone (DEX) impairs neurogenesis and leads to late onset of depression-like behavior that does not respond to the SSRI antidepressant fluoxetine (FLX)...
September 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28888484/prediction-of-human-efficacious-antidepressant-doses-using-the-mouse-forced-swim-test
#13
Eunice Yuen, Steven Swanson, Jeffrey M Witkin
The forced swim test (FST) is a commonly used preclinical animal behavioural model for prediction of antidepressant activity in humans. While the FST may qualitatively predict efficacy, less is known about the quantitative translation of FST data to human efficacious doses. Assessing quantitative translation allows better predictions of human efficacious doses and a higher chance of success in the drug development process. Dose-response and time-course FST experiments were carried out on mice using four marketed antidepressants (citalopram, desipramine, bupropion, desvenlafaxine) in addition to ketamine, all with varying mechanisms of action...
October 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28887185/role-of-monoaminergic-systems-and-ambient-temperature-in-bath-salts-constituent-3-4-methylenedioxypyrovalerone-mdpv-elicited-hyperthermia-and-locomotor-stimulation-in-mice
#14
REVIEW
Brenda M Gannon, Adrian Williamson, Kenner C Rice, William E Fantegrossi
3,4-Methylenedioxypyrovalerone (MDPV) is a common constituent of illicit bath salts products, and in vitro studies implicate monoamine transporters as mediators of its pharmacological effects. Locomotor and thermoregulatory effects of MDPV depend on ambient temperature, so the current studies aimed to gauge the involvement of dopamine (DA), norepinephrine (NE), and serotonin (5-HT) in MDPV-induced locomotor stimulation and hyperthermia in the mouse at different ambient temperatures. Mice were pretreated with the selective 5-HT-reuptake inhibitor fluoxetine (3 mg/kg), the NE-reuptake inhibitor desipramine (3 mg/kg), the DA-reuptake inhibitor bupropion (10 mg/kg), or saline, followed by 10 mg/kg MDPV while thermoregulation and locomotor activity were monitored via radiotelemetry...
September 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28843848/depressive-like-neurochemical-and-behavioral-markers-of-parkinson-s-disease-after-6-ohda-administered-unilaterally-to-the-rat-medial-forebrain-bundle
#15
Kinga Kamińska, Tomasz Lenda, Jolanta Konieczny, Anna Czarnecka, Elżbieta Lorenc-Koci
BACKGROUND: Although Parkinson's disease (PD) is characterized by progressive neurodegeneration of multiple neurotransmitter systems, 6-hydroxydopamine (6-OHDA) as a model substance is mainly used to selectively damage the nigrostriatal dopaminergic neurons and induce parkinsonian-like motor disturbances in rats. We hypothesized that high doses of this neurotoxin affecting other monoaminergic systems may also evoke the depressive-like behavior. METHODS: The impact of 6-OHDA (8, 12, 16μg/4μl) administered unilaterally into the medial forebrain bundle on the sucrose solution intake (a measure of anhedonia) and on the tissue levels of noradrenaline (NA), dopamine (DA) and serotonin (5-HT) in the striatum (STR), substantia nigra (SN), prefrontal cortex (PFC) and hippocampus (HIP) was examined in rats pretreated or non-pretreated with desipramine...
June 3, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28842312/desipramine-rescues-age-related-phenotypes-in-depression-like-rats-induced-by-chronic-mild-stress
#16
Xiaoxian Xie, Yangyang Chen, Qi Wang, Qichen Shen, Lingyan Ma, Liangfeng Huang, Tao Wu, Zhengwei Fu
AIMS: Our previous finding demonstrates that major depressive disorder can mediate accelerated aging in rats. Desipramine is a typical tricyclic antidepressant, and can provide neuroprotection and counteract depression-like behaviors. However, whether desipramine can rescue age-related phenotypes in depressed individuals is not understood. In the present study, we investigated the physiological function of desipramine on rescuing the age-related phenotypes in these animals. MAIN METHODS: The rats were induced by chronic mild stress paradigm, and the depression-like behaviors of rats were detected by sucrose intake test, open field test (OFT) and forced swimming test (FST)...
November 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/28769859/adverse-effects-of-antidepressants-for-chronic-pain-a-systematic-review-and-meta-analysis
#17
Carina Riediger, Tibor Schuster, Kristian Barlinn, Sarah Maier, Jürgen Weitz, Timo Siepmann
BACKGROUND: Antidepressants are widely used in the treatment of chronic pain. Applied doses are lower than those needed to unfold an antidepressive effect. While efficacy of antidepressants for chronic pain has been reported in large randomized-controlled trials (RCT), there is inconsistent data on adverse effects and tolerability. We aimed at synthesizing data from RCT to explore adverse effect profiles and tolerability of antidepressants for treatment of chronic pain. METHODS: Systematic literature research and meta-analyses were performed regarding side effects and safety of different antidepressants in the treatment of chronic pain according to Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28675459/stimulation-of-adrenergic-activity-by-desipramine-enhances-hematopoietic-stem-and-progenitor-cell-mobilization-along-with-g-csf-in-multiple-myeloma-a-pilot-study
#18
Aditi Shastri, Anjali Budhathoki, Stefan K Barta, Noah Kornblum, Olga Derman, Ramakrishna Battini, Radha Raghupathy, Amit K Verma, Paul S Frenette, Ira Braunschweig, Murali Janakiram
Hematopoietic stem cell (HSC) release is positively regulated by the sympathetic nervous system through the β3 adrenergic receptor. Preclinical studies have demonstrated that the combination of desipramine and G-CSF resulted in improved HSC mobilization. Here, we present the results of an open-label single-arm pilot study in patients with multiple myeloma undergoing autologous stem cell transplantation (ASCT) to assess the safety and efficacy of desipramine combined with G-SCF to induce HSC mobilization. The primary endpoint was safety of the combination including engraftment kinetics...
October 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/28662893/both-serotonergic-and-noradrenergic-systems-modulate-the-development-of-tolerance-to-chronic-stress-in-rats-with-lesions-of-the-serotonergic-neurons-of-the-median-raphe-nucleus
#19
A C Pereira, M C Carvalho, C M Padovan
Acute exposure to stress induces significant behavioural changes, while repeated exposure to the same stressor leads to the development of tolerance to stress. The development of tolerance appears to involve the serotonergic projections from the Median Raphe Nucleus (MnRN) to the dorsal Hippocampus (dH), since rats with lesions of this pathway does not develop tolerance to stress. Previous data from our laboratory showed that treatment with imipramine, a serotonin (5-HT) and noradrenaline (NA) reuptake inhibitor, lead to the development of tolerance...
June 27, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28645783/maerua-angolensis-stem-bark-extract-reverses-anxiety-and-related-behaviours-in-zebrafish-involvement-of-gabaergic-and-5-ht-systems
#20
Charles Kwaku Benneh, Robert Peter Biney, Priscilla Kolibea Mante, Augustine Tandoh, Donatus Wewura Adongo, Eric Woode
ETHNOPHARMACOLOGICAL RELEVANCE: Maerua angolensis DC (Capparaceae) has been employed in the management of several central nervous system (CNS) disorders including anxiety. This study evaluated the anxiolytic effects of the petroleum ether/ethyl acetate fraction stem bark extract and its possible mechanism(s) using zebrafish anxiety models. METHODS: Adult zebrafish, tested in the novel tank and light dark tests, have shown by previous authors to be sensitive to the anxiolytic effects of known anxiolytic drugs...
June 20, 2017: Journal of Ethnopharmacology
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