130 results match your criteria Toxicity Cyclic Antidepressants


Efficient Intracellular Delivery of Cell-Impermeable Cargo Molecules by Peptides Containing Tryptophan and Histidine.

Molecules 2018 Jun 26;23(7). Epub 2018 Jun 26.

Center for Targeted Drug Delivery, Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Harry and Diane Rinker Health Science Campus, Irvine, CA 92618, USA.

We have previously evaluated and reported numerous classes of linear and cyclic peptides containing hydrophobic and hydrophilic segments for intracellular delivery of multiple molecular cargos. Herein, a combination of histidine and tryptophan amino acids were designed and evaluated for their efficiency in intracellular delivery of cell-impermeable phosphopeptides and the anti-HIV drug, emtricitabine. Two new decapeptides, with linear and cyclic natures, both containing alternate tryptophan and histidine residues, were synthesized using Fmoc/tBu solid-phase chemistry. Read More

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http://www.mdpi.com/1420-3049/23/7/1536
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http://dx.doi.org/10.3390/molecules23071536DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100250PMC
June 2018
20 Reads
2.420 Impact Factor

Selective HCN1 block as a strategy to control oxaliplatin-induced neuropathy.

Neuropharmacology 2018 03 12;131:403-413. Epub 2018 Jan 12.

Department of Neuroscience, Psychology, Drug Research and Child Health - NEUROFARBA - Pharmacology and Toxicology Section, University of Florence, Florence, Italy.

Chemotherapy-Induced Peripheral Neuropathy (CIPN) is the most frequent adverse effect of pharmacological cancer treatments. The occurrence of neuropathy prevents the administration of fully-effective drug regimen, affects negatively the quality of life of patients, and may lead to therapy discontinuation. CIPN is currently treated with anticonvulsants, antidepressants, opioids and non-opioid analgesics, all of which are flawed by insufficient anti-hyperalgesic efficacy or addictive potential. Read More

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http://dx.doi.org/10.1016/j.neuropharm.2018.01.014DOI Listing
March 2018
1 Read

Effects of the antidepressant, mianserin, on early development of fish embryos at low environmentally relevant concentrations.

Ecotoxicol Environ Saf 2018 Apr 19;150:144-151. Epub 2017 Dec 19.

Shanghai Applied Radiation Institute, Shanghai University, Shanghai 200444, China. Electronic address:

Pharmaceuticals have been considered as emerging organic contaminants in the environment that might pose huge risk to the non-target aquatic organisms. Mianserin, a tetracyclic antidepressant, is present at low detectable concentrations in the aquatic environment; however, limited attention has been devoted to its potential adverse effects on the aquatic animals. In the present study, we first performed an acute toxicity test for mianserin exposure using zebrafish (Danio rerio) embryos during 4-124h post fertilization (hpf). Read More

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http://dx.doi.org/10.1016/j.ecoenv.2017.12.024DOI Listing
April 2018
14 Reads
2.760 Impact Factor

Reduction of cancer cell viability by synergistic combination of photodynamic treatment with the inhibition of the Id protein family.

J Photochem Photobiol B 2018 Jan 5;178:521-529. Epub 2017 Dec 5.

Department of Molecular Biology, University of Salzburg, Billrothstrasse 11, 5020 Salzburg, Austria. Electronic address:

The inhibitor of DNA binding and cell differentiation (Id) proteins are dominant negative regulators of the helix-loop-helix transcription factor family and play a key role during development as well as in vascular disorders and cancer. In fact, impairing the Id-protein activity in cancer cells reduces cell growth and even chemoresistance. Recently, we have shown that a synthetic Id-protein ligand (1Y) consisting of a cyclic nonapeptide can reduce the viability of the two breast cancer cell lines MCF-7 and T47D and of the bladder cancer cells T24 to about 50% at concentrations ≥100μM. Read More

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http://dx.doi.org/10.1016/j.jphotobiol.2017.11.038DOI Listing
January 2018
10 Reads

Venlafaxine Attenuates the Development of Morphine Tolerance and Dependence: Role of L-Arginine/Nitric Oxide/cGMP Pathway.

Endocr Metab Immune Disord Drug Targets 2018 ;18(4):362-370

Department of Pharmacology, School of Pharmacy, Toxicology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

Background: Severe pain reduces quality of life of patients with various diseases, often because chronic morphine therapy results in reduced analgesic effectiveness, or tolerance, leading to escalating doses and distressing adverse effects. Nitric oxide (NO) plays a role in morphine tolerance and dependence.

Objective: Venlafaxine, an antidepressant, is known to modulate nitric oxide (NO) pathway in nervous tissues. Read More

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http://dx.doi.org/10.2174/1871530318666171213153920DOI Listing
October 2018
5 Reads

Atrazine suppresses FSH-induced steroidogenesis and LH-dependent expression of ovulatory genes through PDE-cAMP signaling pathway in human cumulus granulosa cells.

Mol Cell Endocrinol 2018 02 30;461:79-88. Epub 2017 Aug 30.

Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, Serbia.

Atrazine (ATR) alters female reproductive functions in different animal species. Here, we analyzed whether ATR disturbs steroidogenic and ovulatory processes in hormone-stimulated human cumulus granulosa cells and mechanism of its action. Results showed that treatment of human cumulus granulosa cells with 20 μM ATR for 48 h resulted in lower FSH-stimulated estradiol and progesterone production. Read More

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http://dx.doi.org/10.1016/j.mce.2017.08.015DOI Listing
February 2018
4 Reads

The resolution of acute inflammation induced by cyclic AMP is dependent on annexin A1.

J Biol Chem 2017 08 27;292(33):13758-13773. Epub 2017 Jun 27.

From the Programa de Pós-Graduação em Biologia Celular, Departamento de Morfologia, Instituto de Ciências Biológicas,

Annexin A1 (AnxA1) is a glucocorticoid-regulated protein known for its anti-inflammatory and pro-resolving effects. We have shown previously that the cAMP-enhancing compounds rolipram (ROL; a PDE4 inhibitor) and BtcAMP (a cAMP mimetic) drive caspase-dependent resolution of neutrophilic inflammation. In this follow-up study, we investigated whether AnxA1 could be involved in the pro-resolving properties of these compounds using a model of LPS-induced inflammation in BALB/c mice. Read More

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http://www.jbc.org/lookup/doi/10.1074/jbc.M117.800391
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http://dx.doi.org/10.1074/jbc.M117.800391DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5566529PMC
August 2017
9 Reads

Rapid Access to Oxazine Fused Furocoumarins and in vivo and in silico Studies of theirs Biological Activity.

Med Chem 2017 ;13(7):625-632

Laboratory of Medicinal Chemistry, Novosibirsk Institute of Organic Chemistry, P.O. Box: 630090, Novosibirsk. Russian Federation.

Background: The synthesis of 1,2-oxazine-fused linear furocoumarins was performed involving the transition metal catalysis reaction of plant coumarin oreoselone derivatives.

Objective And Method: The Pd-catalyzed desulfonative cross-coupling reactions of 2-(tosyl)oreoselone with terminal alkynes and the successive treatment of the obtained 2-(arylethynyl)furocoumarins with an excess of hydroxylamine gave the expected (Z,E)-3-(hydroxyimino)-2-(arylethynyl)furocoumarins with an (Z:E) ratio of about 1:0.5. Read More

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http://dx.doi.org/10.2174/1573406413666170601114527DOI Listing
December 2017
18 Reads

Assessment of the Neuroprotective Effects of Arginine-Rich Protamine Peptides, Poly-Arginine Peptides (R12-Cyclic, R22) and Arginine-Tryptophan-Containing Peptides Following In Vitro Excitotoxicity and/or Permanent Middle Cerebral Artery Occlusion in Rats.

Neuromolecular Med 2017 Sep 18;19(2-3):271-285. Epub 2017 May 18.

Perron Institute for Neurological and Translational Science, QEII Medical Centre, 8 Verdun St, Nedlands, WA, 6009, Australia.

We have demonstrated that arginine-rich and poly-arginine peptides possess potent neuroprotective properties with arginine content and peptide positive charge being particularly critical for neuroprotective efficacy. In addition, the presence of other amino acids within arginine-rich peptides, as well as chemical modifications, peptide length and cell-penetrating properties also influence the level of neuroprotection. Against this background, we have examined the neuroprotective efficacy of arginine-rich protamine peptides, a cyclic (R12-c) poly-arginine peptide and a R22 poly-arginine peptide, as well as arginine peptides containing tryptophan or other amino acids (phenylalanine, tyrosine, glycine or leucine) in in vitro glutamic acid excitotoxicity and in vivo rat permanent middle cerebral artery occlusion models of stroke. Read More

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http://dx.doi.org/10.1007/s12017-017-8441-2DOI Listing
September 2017
19 Reads

Involvement of Akt/GSK3β/CREB signaling pathway on chronic omethoate induced depressive-like behavior and improvement effects of combined lithium chloride and astaxanthin treatment.

Neurosci Lett 2017 05 30;649:55-61. Epub 2017 Mar 30.

Department of Neurology, Affiliated Hospital of Qingdao University, Qingdao 266003, China. Electronic address:

Chronic organophosphorus pesticides (OP) exposure is associated with an increased risk of depression, and there is an urgent need to find an effective treatment for the depressive-like symptoms caused by OP. The main purpose of this study was to investigate whether combined lithium chloride (LiCl) and astaxanthin (AST) treatment would manifest synergetic antidepressant effects on mice with chronic OP exposure, and to determine the role of the Akt/GSK3β/CREB signaling pathway. Our results showed that chronic omethoate exposure significantly increased immobility time in behavioral tests and induced neuron damage in HE staining. Read More

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http://dx.doi.org/10.1016/j.neulet.2017.03.048DOI Listing
May 2017
14 Reads

Galanin contributes to monoaminergic dysfunction and to dependent neurobehavioral comorbidities of epilepsy.

Exp Neurol 2017 03 22;289:64-72. Epub 2016 Dec 22.

Department of Pediatrics, David Geffen School of Medicine, University of California, Los Angeles (UCLA), Los Angeles, CA, USA; Children's Discovery and Innovation Institute, UCLA, Los Angeles, CA, USA. Electronic address:

Status epilepticus (SE) in rats, along with chronic epilepsy, leads to the development of behavioral impairments resembling depressive disorder and/or attention deficit/hyperactivity disorder (ADHD), thus reflecting respective comorbidities in epilepsy patients. Suppressed neurotransmitter tone in the raphe nucleus (RN)-prefrontal cortex (PFC) serotonergic pathway and in the locus coeruleus (LC)-PFC noradrenergic pathway underlies depressive- and impulsive-like behavioral deficits respectively. We examined possible mechanisms leading to the monoamine dysfunction in brainstem efferents, namely modulatory effects of the neuropeptide galanin on serotonin (5-HT) and norepinephrine (NE) signaling. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00144886163041
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http://dx.doi.org/10.1016/j.expneurol.2016.12.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5285493PMC
March 2017
13 Reads

Efficacy of phosphodiesterase-4 inhibitors in juvenile Batten disease (CLN3).

Ann Neurol 2016 12 23;80(6):909-923. Epub 2016 Nov 23.

Department of Pathology and Microbiology, University of Nebraska Medical Center, Omaha, NE.

Objective: Juvenile neuronal ceroid lipofuscinosis (JNCL), or juvenile Batten disease, is a pediatric lysosomal storage disease caused by autosomal recessive mutations in CLN3, typified by blindness, seizures, progressive cognitive and motor decline, and premature death. Currently, there is no treatment for JNCL that slows disease progression, which highlights the need to explore novel strategies to extend the survival and quality of life of afflicted children. Cyclic adenosine monophosphate (cAMP) is a second messenger with pleiotropic effects, including regulating neuroinflammation and neuronal survival. Read More

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http://dx.doi.org/10.1002/ana.24815DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5215570PMC
December 2016
77 Reads

LPA1 Mediates Antidepressant-Induced ERK1/2 Signaling and Protection from Oxidative Stress in Glial Cells.

J Pharmacol Exp Ther 2016 Nov 7;359(2):340-353. Epub 2016 Sep 7.

Laboratory of Cellular and Molecular Pharmacology, Section of Neurosciences and Clinical Pharmacology, Department of Biomedical Sciences, University of Cagliari, Cagliari, Italy (M.C.O., S.D., P.O.)

Antidepressants have been shown to affect glial cell functions and intracellular signaling through mechanisms that are still not completely understood. In the present study, we provide evidence that in glial cells the lysophosphatidic acid (LPA) receptor LPA mediates antidepressant-induced growth factor receptor transactivation, ERK1/2 signaling, and protection from oxidative stress. Thus, in C6 glioma cells and rat cortical astrocytes, ERK1/2 activation induced by either amitriptyline or mianserin was antagonized by Ki16425 and VPC 12249 (S), which block LPA and LPA receptors, and by AM966, which selectively blocks LPA Cell depletion of LPA with siRNA treatment markedly reduced antidepressant- and LPA-induced ERK1/2 phosphorylation. Read More

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http://dx.doi.org/10.1124/jpet.116.236455DOI Listing
November 2016
12 Reads

Discovery of N-Alkyl Catecholamides as Selective Phosphodiesterase-4 Inhibitors with Anti-neuroinflammation Potential Exhibiting Antidepressant-like Effects at Non-emetic Doses.

ACS Chem Neurosci 2017 01 13;8(1):135-146. Epub 2016 Oct 13.

Department of Neuropharmacology and Novel Drug Discovery, School of Pharmaceutical Sciences, Southern Medical University , Guangzhou 510515, China.

Depression involving neuroinflammation is one of the most common disabling and life-threatening psychiatric disorders. Phosphodiesterase 4 (PDE4) inhibitors produce potent antidepressant-like and cognition-enhancing effects. However, their clinical utility is limited by their major side effect of emesis. Read More

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http://dx.doi.org/10.1021/acschemneuro.6b00271DOI Listing
January 2017
8 Reads

Improvement of daptomycin production via increased resistance to decanoic acid in Streptomyces roseosporus.

J Biosci Bioeng 2016 Oct 29;122(4):427-33. Epub 2016 Jul 29.

Center for Nutraceutical and Pharmaceutical Materials, Myongji University, Yongin 449728, South Korea. Electronic address:

Daptomycin, a cyclic anionic lipopeptide compound produced by Streptomyces roseosporus, is used to treat skin infections caused by multi-drug resistant gram-positive pathogens. The biosynthesis of daptomycin is initiated by the condensation of decanoic acid (DA, a 10-carbon unit fatty acid) and the N-terminal l-tryptophan. So, the addition of DA to the fermentation medium is essential for increasing daptomycin production. Read More

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http://dx.doi.org/10.1016/j.jbiosc.2016.03.026DOI Listing
October 2016
8 Reads

Involvement of PI3K/Akt/FoxO3a and PKA/CREB Signaling Pathways in the Protective Effect of Fluoxetine Against Corticosterone-Induced Cytotoxicity in PC12 Cells.

J Mol Neurosci 2016 Aug 13;59(4):567-78. Epub 2016 Jul 13.

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.

The selective serotonin reuptake inhibitor fluoxetine is neuroprotective in several brain injury models. It is commonly used to treat major depressive disorder and related conditions, but its mechanism of action remains incompletely understood. Activation of the phosphatidylinositol-3-kinase/protein kinase B/forkhead box O3a (PI3K/Akt/FoxO3a) and protein kinase A/cAMP-response element binding protein (PKA/CREB) signaling pathways has been strongly implicated in the pathogenesis of depression and might be the downstream target of fluoxetine. Read More

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http://dx.doi.org/10.1007/s12031-016-0779-7DOI Listing
August 2016
37 Reads

Desipramine improves depression-like behavior and working memory by up-regulating p-CREB in Alzheimer's disease associated mice.

J Integr Neurosci 2016 Jun 23;15(2):247-60. Epub 2016 Jun 23.

† Department of Physiology, Shanxi Medical University, Taiyuan, China.

Aggregation of amyloid [Formula: see text] protein (A[Formula: see text] and progressive loss of memory are the main characteristics of Alzheimer's disease (AD). It is noteworthy that approximately 40% of AD patients have depressive symptom. The close correlation between cognitive deficits and mental depression suggests a possibility that antidepression treatment might be beneficial to cognitive improvement in AD. Read More

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http://dx.doi.org/10.1142/S021963521650014XDOI Listing
June 2016
27 Reads

Antidepressant-like Effects of ZBH2012001, a Novel Potent Serotonin and Norepinephrine Reuptake Inhibitor.

CNS Neurosci Ther 2016 08 20;22(8):700-6. Epub 2016 May 20.

Department of New Drug Evaluation, Beijing Institute of Pharmacology and Toxicology, Beijing, China.

Aims: The present study was conducted to evaluate the antidepressant-like effects of ZBH2012001, a novel potential serotonin and norepinephrine reuptake inhibitor (SNRI).

Methods: Competitive binding assays, calcium flow, and cAMP detection methods were used to determine the affinity of ZBH2012001 for serotonin transporters (SERTs) and norepinephrine transporters (NETs), as well as its selectivity over dopamine transporters (DATs) and 16 other G-protein-coupled receptors (GPCRs) or iron channels. The antidepressant-like effects of ZBH2012001 were determined using the tail suspension test, forced swim test, and learned helplessness paradigm. Read More

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http://dx.doi.org/10.1111/cns.12567DOI Listing
August 2016
19 Reads

Antidepressant therapies inhibit inflammation and microglial M1-polarization.

Pharmacol Ther 2016 07 18;163:82-93. Epub 2016 Apr 18.

Neuroscience Research, NIBR, Fabrikstrasse 22-3.001.02, Basel 4002, Switzerland.

Macrophages and their counterparts in the central nervous system, the microglia, detect and subsequently clear microbial pathogens and injured tissue. These phagocytic cells alter and adapt their phenotype depending on their prime activity, i.e. Read More

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http://dx.doi.org/10.1016/j.pharmthera.2016.04.001DOI Listing
July 2016
7 Reads

Preorganized Peptide Scaffolds as Mimics of Phosphorylated Proteins Binding Sites with a High Affinity for Uranyl.

Inorg Chem 2015 Dec 19;54(23):11557-62. Epub 2015 Nov 19.

Université Grenoble Alpes , INAC-SCIB, F-38000 Grenoble, France.

Cyclic peptides with two phosphoserines and two glutamic acids were developed to mimic high-affinity binding sites for uranyl found in proteins such as osteopontin, which is believed to be a privileged target of this ion in vivo. These peptides adopt a β-sheet structure that allows the coordination of the latter amino acid side chains in the equatorial plane of the dioxo uranyl cation. Complementary spectroscopic and analytical methods revealed that these cyclic peptides are efficient uranyl chelating peptides with a large contribution from the phosphorylated residues. Read More

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http://dx.doi.org/10.1021/acs.inorgchem.5b02249DOI Listing
December 2015
15 Reads

Antidepressant drugs specifically inhibiting noradrenaline reuptake enhance recognition memory in rats.

Behav Neurosci 2015 Dec 26;129(6):701-8. Epub 2015 Oct 26.

Department of Physiology and Pharmacology, Karolinska Institutet.

Patients suffering from major depression often experience memory deficits even after the remission of mood symptoms, and many antidepressant drugs do not affect, or impair, memory in animals and humans. However, some antidepressant drugs, after a single dose, enhance cognition in humans (Harmer et al., 2009). Read More

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http://dx.doi.org/10.1037/bne0000100DOI Listing
December 2015
9 Reads

The Analgesic Effect of Rolipram, a Phosphodiesterase 4 Inhibitor, on Chemotherapy-Induced Neuropathic Pain in Rats.

Anesth Analg 2015 Sep;121(3):822-8

From the *Department of Pain Medicine, The University of Texas MD Anderson Cancer Center, Houston, Texas; †Department of Anesthesiology, Perioperative Medicine, and Pain Management, University of Miami, LM Miller School of Medicine, Miami, Florida; and ‡Department of Biostatistics, Florida International University, Miami, Florida.

Background: Chemotherapy-induced neuropathic pain is a significant side effect of chemotherapeutic agents. Currently, there are no effective analgesics for chemotherapy-induced neuropathic pain. Rolipram is a selective phosphodiesterase 4 inhibitor, which increases intracellular cyclic AMP in nerve and immune cells. Read More

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http://dx.doi.org/10.1213/ANE.0000000000000853DOI Listing
September 2015
9 Reads

Blockade of phosphodiesterase 4 reverses morphine-induced ventilatory disturbance without loss of analgesia.

Life Sci 2015 Apr 2;127:32-8. Epub 2015 Mar 2.

Laboratory of Neuropharmacology, School of Pharmacy, Aichi Gakuin University, Nagoya 464-8650, Japan. Electronic address:

Aims: Ventilatory disturbance is a fatal side-effect of opioid analgesics. Separation of analgesia from ventilatory depression is important for therapeutic use of opioids. It has been suggested that opioid-induced ventilatory depression results from a decrease in adenosine 3',5'-cyclic monophosphate content in the respiratory-related neurons. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00243205150009
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http://dx.doi.org/10.1016/j.lfs.2015.02.006DOI Listing
April 2015
3 Reads

Essential oil of Syzygium aromaticum reverses the deficits of stress-induced behaviors and hippocampal p-ERK/p-CREB/brain-derived neurotrophic factor expression.

Planta Med 2015 Feb 15;81(3):185-92. Epub 2015 Jan 15.

Department of Chemical and Pharmaceutical Engineering, College of Chemical Engineering, Huaqiao University, Xiamen, Fujian Province, P. R. China.

Syzygium aromaticum has been widely used in traditional medicine. Our study investigated the safety and antidepressant-like effects of the essential oil of S. aromaticum after acute or long-term treatment. Read More

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http://dx.doi.org/10.1055/s-0034-1396150DOI Listing
February 2015
11 Reads

Alteration in brain-derived neurotrophic factor (BDNF) after treatment of mice with herbal mixture containing Euphoria longana, Houttuynia cordata and Dioscorea japonica.

Daru 2014 Nov 28;22:77. Epub 2014 Nov 28.

School of Biomedical Sciences, Charles Sturt University, Bathurst, NSW, 2795, Australia.

Background: Literature data indicate that brain-derived neurotrophic factor (BDNF), cyclic-AMP response element-binding protein (CREB) and phospho-CREB (pCREB) may have a place in depression. BDNF belongs to the neurotrophin family that plays an important role in proliferation, survival and differentiation of different cell populations in the mammalian nervous system. The herbal mixture used in the present study consists of Euphoria longana, Houttuynia cordata and Dioscorea japonica. Read More

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http://dx.doi.org/10.1186/s40199-014-0077-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4268823PMC
November 2014
8 Reads

Ethanol suppresses PGC-1α expression by interfering with the cAMP-CREB pathway in neuronal cells.

PLoS One 2014 6;9(8):e104247. Epub 2014 Aug 6.

Department of Neurology, University of Texas Medical Branch, Galveston, Texas, United States of America.

Alcohol intoxication results in neuronal apoptosis, neurodegeneration and manifest with impaired balance, loss of muscle coordination and behavioral changes. One of the early events of alcohol intoxication is mitochondrial (Mt) dysfunction and disruption of intracellular redox homeostasis. The mechanisms by which alcohol causes Mt dysfunction, disrupts cellular redox homeostasis and triggers neurodegeneration remains to be further investigated. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0104247PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4123904PMC
November 2015
18 Reads

Effects of (+)-8-OH-DPAT on the duration of immobility during the forced swim test and hippocampal cell proliferation in ACTH-treated rats.

Pharmacol Biochem Behav 2014 Jul 13;122:240-5. Epub 2014 Apr 13.

Department of Clinical Pharmacy, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 2-5-1 Shikata-cho, Kita-ku, Okayama 700-8558, Japan.

In the present study, we examined the effect of ACTH on the immobilization of rats in the forced swim test and hippocampal cell proliferation after administration of the 5-HT1A receptor agonist, R-(+)-8-hydroxy-2-di-n-propylamino tetralin ((+)-8-OH-DPAT). Chronic treatment with (+)-8-OH-DPAT (0.01-0. Read More

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http://dx.doi.org/10.1016/j.pbb.2014.04.003DOI Listing
July 2014
5 Reads

Hippocampal HDAC4 contributes to postnatal fluoxetine-evoked depression-like behavior.

Neuropsychopharmacology 2014 Aug 25;39(9):2221-32. Epub 2014 Mar 25.

Department of Biological Sciences, Tata Institute of Fundamental Research, Mumbai, India.

Fluoxetine treatment in adulthood evokes antidepressant and anxiolytic responses. Paradoxically, postnatal fluoxetine (PNFlx) induces persistent depression- and anxiety-like behaviors. The mechanistic underpinnings of this paradox remain poorly understood. Read More

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http://dx.doi.org/10.1038/npp.2014.73DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4104341PMC
August 2014
7 Reads

Neuroprotective effects of 3,6'-disinapoyl sucrose through increased BDNF levels and CREB phosphorylation via the CaMKII and ERK1/2 pathway.

J Mol Neurosci 2014 Aug 4;53(4):600-7. Epub 2014 Feb 4.

Department of Clinical Pharmacology, Pharmacy Care Center, Chinese PLA General Hospital, No. 28 FuXing Road, Beijing, 100853, People's Republic of China.

3,6'-Disinapoyl sucrose (DISS) is an oligosaccharide ester natural product originating from the root of wild Polygala tenuifolia. Our previous reports suggested that DISS can have neuroprotective effects and antidepressive activity in rats, at least in part, by increased expression of cyclic AMP response element (CRE)-binding protein (CREB) and its downstream target protein, brain-derived neurotrophic factor (BDNF). The aim of the present study was to explore the mechanism of DISS-modulated BDNF and CREB expression. Read More

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http://dx.doi.org/10.1007/s12031-013-0226-yDOI Listing
August 2014
9 Reads

Methylene blue used in the treatment of refractory shock resulting from drug poisoning.

Clin Toxicol (Phila) 2014 Jan 24;52(1):63-5. Epub 2013 Dec 24.

Department of Emergency Medicine, Monash Health , Melbourne , Australia.

Background: Methylene blue inhibits the nitric oxide-cyclic guanosine monophosphate (NO-cGMP) pathway, decreasing vasodilation and increasing responsiveness to vasopressors. It is reported to improve haemodynamics in distributive shock from various causes including septicaemia and post-cardiac surgery. Reports of use in overdose are limited. Read More

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http://dx.doi.org/10.3109/15563650.2013.870343DOI Listing
January 2014
10 Reads

The mode of action (MOA) approach reveals interactive effects of environmental pharmaceuticals on Mytilus galloprovincialis.

Aquat Toxicol 2013 Sep 19;140-141:249-56. Epub 2013 Jun 19.

University of Bologna, Interdepartment Centre for Environmental Science Research, via S. Alberto 163, 48123 Ravenna, Italy.

Aquatic organisms are unintentionally exposed to a large number of pharmaceutical residues in their natural habitats. Ecotoxicological studies have agreed that these compounds are not harmful to aquatic organisms, as their environmental concentrations are typically too low. However, recent reports have shown biological effects at such low concentrations when biological endpoints related to the therapeutic effects are assessed. Read More

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http://dx.doi.org/10.1016/j.aquatox.2013.06.005DOI Listing
September 2013
8 Reads

Atrazine acts as an endocrine disrupter by inhibiting cAMP-specific phosphodiesterase-4.

Toxicol Appl Pharmacol 2012 Nov 27;265(1):19-26. Epub 2012 Sep 27.

Section on Cellular Signaling, Program in Developmental Neuroscience, NICHD, NIH, Bethesda, MD, USA.

Atrazine, one of the most commonly used herbicides worldwide, acts as an endocrine disruptor, but the mechanism of its action has not been characterized. In this study, we show that atrazine rapidly increases cAMP levels in cultured rat pituitary and testicular Leydig cells in a concentration-dependent manner, but less effectively than 3-isobutyl-1-methylxanthine, a competitive non-specific inhibitor of phosphodiesterases (PDEs). In forskolin (an activator of adenylyl cyclase)- and probenecid (an inhibitor of cyclic nucleotide transporters)-treated cells, but not in 3-isobutyl-1-methylxanthine-treated cells, atrazine further increased cAMP levels, indicating that inhibition of PDEs accounts for accumulation of cAMP. Read More

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http://dx.doi.org/10.1016/j.taap.2012.09.019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4181665PMC
November 2012
6 Reads

Rolipram promotes remyelination possibly via MEK-ERK signal pathway in cuprizone-induced demyelination mouse.

Exp Neurol 2012 Oct 24;237(2):304-11. Epub 2012 Jul 24.

Department of Neurology, the First Affiliated Hospital of Harbin Medical University, Ha'erbin 150001, China.

Objective: Rolipram, a 3'-5'-cyclic adenosine monophosphate (cAMP)-dependent phosphodiesterase 4 (PDE4) inhibitor, has long been studied for its immune modulating effects in the treatment of experimental autoimmune encephalomyelitis (EAE). In the current study, we investigated the effects of rolipram on remyelination after cuprizone- or lysolecithin-induced demyelination and the signal transduction pathways potentially modulating this response.

Materials And Methods: Cuprizone-induced demyelination in mice and lysolecithin (LPC)-induced demyelination in rat cerebellum slice culture were treated with rolipram. Read More

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http://dx.doi.org/10.1016/j.expneurol.2012.07.011DOI Listing
October 2012
13 Reads

Inhibition of chlorine-induced lung injury by the type 4 phosphodiesterase inhibitor rolipram.

Toxicol Appl Pharmacol 2012 Sep 2;263(2):251-8. Epub 2012 Jul 2.

Department of Environmental and Occupational Health Sciences, School of Public Health and Information Sciences, University of Louisville, Louisville, KY, USA.

Chlorine is a highly toxic respiratory irritant that when inhaled causes epithelial cell injury, alveolar-capillary barrier disruption, airway hyperreactivity, inflammation, and pulmonary edema. Chlorine is considered a chemical threat agent, and its release through accidental or intentional means has the potential to result in mass casualties from acute lung injury. The type 4 phosphodiesterase inhibitor rolipram was investigated as a rescue treatment for chlorine-induced lung injury. Read More

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http://dx.doi.org/10.1016/j.taap.2012.06.017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3422440PMC
September 2012
8 Reads

Delayed-onset seizure and cardiac arrest after amitriptyline overdose, treated with intravenous lipid emulsion therapy.

Pediatrics 2012 Aug 2;130(2):e432-8. Epub 2012 Jul 2.

Department of Medical Toxicology, Banner Good Samaritan Medical Center, Phoenix, Arizona, USA.

In recent years, intravenous lipid emulsion (ILE) therapy has emerged as a new rescue antidote for treatment of certain toxicities, including cyclic antidepressants, and as the primary treatment of toxic manifestations after local anesthetic exposure. We present a case of a 13-year-old girl who developed delayed seizures and cardiac arrest after amitriptyline ingestion. As part of the treatment, she was treated with ILE therapy. Read More

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http://pediatrics.aappublications.org/cgi/doi/10.1542/peds.2
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http://dx.doi.org/10.1542/peds.2011-2511DOI Listing
August 2012
9 Reads

Drug-eluting microfibrous patches for the local delivery of rolipram in spinal cord repair.

J Control Release 2012 Aug 23;161(3):910-7. Epub 2012 May 23.

UC Berkeley & UCSF Joint Graduate Program in Bioengineering, Berkeley/San Francisco, CA, USA.

Spinal cord injury (SCI) remains a major challenge for regenerative medicine. Following SCI, axon growth inhibitors and other inflammatory responses prevent functional recovery. Previous studies have demonstrated that rolipram, an anti-inflammatory and cyclic adenosine monophosphate preserving small molecule, improves spinal cord regeneration when delivered systemically. Read More

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http://dx.doi.org/10.1016/j.jconrel.2012.05.034DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3698241PMC
August 2012
10 Reads

Antidepressant-like and neuroprotective effects of Aloysia gratissima: investigation of involvement of L-arginine-nitric oxide-cyclic guanosine monophosphate pathway.

J Ethnopharmacol 2011 Sep 8;137(1):864-74. Epub 2011 Jul 8.

Biochemistry Department, Biological Sciences Center, Federal University of Santa Catarina, Florianópolis 88040-900, SC, Brazil.

Ethnopharmacological Relevance: Aloysia gratissima (Gill. et Hook) Tronc. (Verbenaceae) is used traditionally for the treatment of headache, bronchitis, and nervous systems disorders including depression. Read More

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http://dx.doi.org/10.1016/j.jep.2011.07.009DOI Listing
September 2011
8 Reads

The phosphodiesterase-4 inhibitor rolipram reverses Aβ-induced cognitive impairment and neuroinflammatory and apoptotic responses in rats.

Int J Neuropsychopharmacol 2012 Jul 9;15(6):749-66. Epub 2011 Jun 9.

Department of Pharmacology, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China.

β-amyloid (Aβ) peptides play an important role in cognition deficits, neuroinflammation, and apoptosis observed in Alzheimer's disease (AD). Activation of cyclic AMP (cAMP) signalling enhances memory and inhibits inflammatory and apoptotic responses. However, it is not known whether inhibition of phosphodiesterase-4 (PDE4), a critical controller of intracellular cAMP concentrations, affects AD-associated neuroinflammatory and apoptotic responses and whether these responses contribute to deficits of memory mediated by cAMP signalling. Read More

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https://academic.oup.com/ijnp/article-lookup/doi/10.1017/S14
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http://dx.doi.org/10.1017/S1461145711000836DOI Listing
July 2012
26 Reads

Curcumin prevents corticosterone-induced neurotoxicity and abnormalities of neuroplasticity via 5-HT receptor pathway.

J Neurochem 2011 Sep 18;118(5):784-95. Epub 2011 Jul 18.

J. Crayton Pruitt Family Department of Biomedical Engineering, University of Florida, Gainesville, Florida 32611, USA.

Curcumin, a major active component of Curcuma longa, possesses antioxidant and neuroprotective activities. The present study explores the mechanisms underlying the neuroprotective effect of curcumin against corticosterone and its relation to 5-hydroxy tryptamine (5-HT) receptors. Exposure of cortical neurons to corticosterone results in decreased mRNA levels for three 5-HT receptor subtypes, 5-HT(1A), 5-HT(2A) and 5-HT(4), but 5-HT(1B,) 5-HT(2B), 5-HT(2C), 5-HT(6) and 5-HT(7) receptors remain unchanged. Read More

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http://dx.doi.org/10.1111/j.1471-4159.2011.07356.xDOI Listing
September 2011
6 Reads

Low-level laser therapy (LLLT) acts as cAMP-elevating agent in acute respiratory distress syndrome.

Lasers Med Sci 2011 May 24;26(3):389-400. Epub 2010 Dec 24.

Research and Development Institute - IP&D, Av. Shishima Hifumi, 2911 - Urbanova, Po Box 12244-00, São José dos Campos, SP, Brazil.

The aim of this work was to investigate if the low-level laser therapy (LLLT) on acute lung inflammation (ALI) induced by lipopolysaccharide (LPS) is linked to tumor necrosis factor (TNF) in alveolar macrophages (AM) from bronchoalveolar lavage fluid (BALF) of mice. LLLT has been reported to actuate positively for relieving the late and early symptoms of airway and lung inflammation. It is not known if the increased TNF mRNA expression and dysfunction of cAMP generation observed in ALI can be influenced by LLLT. Read More

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http://dx.doi.org/10.1007/s10103-010-0874-xDOI Listing
May 2011
7 Reads

Allopregnanolone prevents and suppresses oxaliplatin-evoked painful neuropathy: multi-parametric assessment and direct evidence.

Pain 2011 Jan 10;152(1):170-81. Epub 2010 Nov 10.

Université de Strasbourg, Bâtiment 3 de la Faculté de Médecine, Strasbourg, France.

Oxaliplatin (OXAL) is a platinum-based drug used for the treatment of colorectal, lung, breast and ovarian cancers. OXAL does not cause renal or hematologic toxicity. However, OXAL induces neuropathic pain which hampers the chemotherapy success. Read More

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http://content.wkhealth.com/linkback/openurl?sid=WKPTLP:land
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http://dx.doi.org/10.1016/j.pain.2010.10.015DOI Listing
January 2011
8 Reads

Inhibition of phosphodiesterase-4 reverses memory deficits produced by Aβ25-35 or Aβ1-40 peptide in rats.

Psychopharmacology (Berl) 2010 Oct 17;212(2):181-91. Epub 2010 Jul 17.

Department of Pharmacology, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, Guangdong, 510515, People's Republic of China.

Rationale: Cyclic AMP signaling plays an important role in memory loss associated with Alzheimer's disease (AD). However, little is known about whether inhibition of phosphodiesterase-4 (PDE4), which increases intracellular cAMP, reverses β-amyloid peptide (Aβ)-induced memory deficits.

Objective: Experiments were performed to demonstrate the effect of the PDE4 inhibitor rolipram on memory impairment produced by Aβ1-40 (Aβ40) or its core fragment Aβ25-35. Read More

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http://link.springer.com/content/pdf/10.1007/s00213-010-1943
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http://link.springer.com/10.1007/s00213-010-1943-3
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http://dx.doi.org/10.1007/s00213-010-1943-3DOI Listing
October 2010
51 Reads

Alterations of pre- and postsynaptic noradrenergic signaling in a rat model of adriamycin-induced cardiotoxicity.

J Nucl Cardiol 2010 Apr 25;17(2):254-63. Epub 2010 Feb 25.

National Cardiac PET Centre, Division of Cardiology (Department of Medicine), University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, K1Y 4W7, Canada.

Background: Altered sympathetic nervous system signaling is known to play a role in the cardiotoxicity of the anthracycline chemotherapeutic agents, but the interaction of pre- and postsynaptic function is not well understood.

Methods And Results: Our aim was to study the noradrenergic signaling in an established rat model of adriamycin cardiotoxicity (15 mg/kg administered i.p. Read More

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http://link.springer.com/10.1007/s12350-009-9190-x
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http://dx.doi.org/10.1007/s12350-009-9190-xDOI Listing
April 2010
7 Reads

Synthesis and thermodynamic characterization of small cyclic antimicrobial arginine and tryptophan-rich peptides with selectivity for Gram-negative bacteria.

Authors:
Mojtaba Bagheri

Methods Mol Biol 2010 ;618:87-109

Leibniz Institute of Molecular Pharmacology (FMP), Berlin, Germany.

One promising strategy to combat the proliferation of bacteria resistance toward current antibiotics is the development of peptide-based drug. Among these compounds is a group of small cyclic peptides rich in arginine (Arg) and tryptophan (Trp) residues with selective toxicity toward Gram-negative bacteria. The small size of these peptides with improved toxicity toward Gram-negative bacteria makes them an interesting candidate to understand the forces responsible for their selectivity and paves the way to develop new therapeutics with potent activity toward multi-resistant Gram-negative bacteria. Read More

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http://link.springer.com/content/pdf/10.1007/978-1-60761-594
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http://link.springer.com/10.1007/978-1-60761-594-1_7
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http://dx.doi.org/10.1007/978-1-60761-594-1_7DOI Listing
April 2010
2 Reads

Action of a Novel PDE4 inhibitor ZL-n-91 on lipopolysaccharide-induced acute lung injury.

Int Immunopharmacol 2010 Apr 13;10(4):406-11. Epub 2010 Jan 13.

Zhejiang Respiratory Drugs Research Laboratory of State Foods & Drugs Administration of China, Medical School of Zhejiang University, Hangzhou 310058, China.

In the present study, we investigated the effect of classic PDE4 inhibitor rolipram and novel PDE4 inhibitor ZL-n-91 on LPS-induced acute lung injury (ALI) in mice and its mechanism. ALI was induced in ICR mice by instilling intratracheally with LPS, and mice were divided into seven groups: control (Saline), LPS group, ZL-n-91 (3 microg, 10 microg, and 30 microg kg(-1), ip), Rolipram (1.0 mg kg(-1), ip) and dexamethasone (0. Read More

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http://dx.doi.org/10.1016/j.intimp.2010.01.003DOI Listing
April 2010
5 Reads

Anti-depressant natural flavonols modulate BDNF and beta amyloid in neurons and hippocampus of double TgAD mice.

Neuropharmacology 2010 May 14;58(6):911-20. Epub 2009 Nov 14.

Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA.

Increasing evidence suggests that depression may be both a cause and consequence of neurological disorders such as Alzheimer's disease (AD), and that anti-depressants could provide an alternative strategy to current AD therapies. Association of side effect and herbal-drug interaction with conventional anti-depressant and St. John's wort warrant investigating new anti-depressant drugs. Read More

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http://dx.doi.org/10.1016/j.neuropharm.2009.11.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2838959PMC
May 2010
4 Reads

Intravenous lipid emulsion as antidote beyond local anesthetic toxicity: a systematic review.

Acad Emerg Med 2009 Sep;16(9):815-24

Hutt Hospital, Lower Hutt, New Zealand.

Objectives: The objective was to asses the efficacy of lipid emulsion as antidotal therapy outside the accepted setting of local anesthetic toxicity.

Methods: Literature was accessed through PubMed, OVID (1966-February 2009), and EMBASE (1947-February 2009) using the search terms "intravenous" AND ["fat emulsion" OR "lipid emulsion" OR "Intralipid"] AND ["toxicity" OR "resuscitation" OR "rescue" OR "arrest" OR "antidote"]. Additional author and conference publication searches were undertaken. Read More

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http://doi.wiley.com/10.1111/j.1553-2712.2009.00499.x
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http://dx.doi.org/10.1111/j.1553-2712.2009.00499.xDOI Listing
September 2009
3 Reads

Effects of dimethylaminoethanol pyroglutamate (DMAE p-Glu) against memory deficits induced by scopolamine: evidence from preclinical and clinical studies.

Psychopharmacology (Berl) 2009 Dec 16;207(2):201-12. Epub 2009 Sep 16.

CIC-UPCET, UMR CNRS-Université de la Méditerranée 6193, Hôpital de la Timone, 13385, Marseille cedex 5, France.

Rationale: Dimethylaminoethanol pyroglutamate (DMAE p-Glu) is a compound resulting from the reaction between dimethylaminoethanol (an indirect precursor of acetylcholine) and pyroglutamic acid (a cyclic derivative of glutamic acid having procholinergic properties and promnesic effects in both animals and man).

Objectives: The present study undertook preclinical and clinical evaluations to test a potential therapeutic utility for DMAE p-Glu in cognitive impairments related to central cholinergic deficit.

Materials And Methods: In preclinical study, DMAE p-Glu was studied in rats by intracerebral microdialysis in conscious freely moving animals, on performance of rats in the Morris water maze test of spatial memory, and on the deficit in passive avoidance behavior induced by scopolamine. Read More

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http://link.springer.com/content/pdf/10.1007/s00213-009-1648
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http://link.springer.com/10.1007/s00213-009-1648-7
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http://dx.doi.org/10.1007/s00213-009-1648-7DOI Listing
December 2009
12 Reads

Targeted inhibition of cyclic AMP phosphodiesterase-4 promotes brain tumor regression.

Clin Cancer Res 2008 Dec;14(23):7717-25

Department of Pediatrics, Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri 63110, USA.

Purpose: As favorable outcomes from malignant brain tumors remain limited by poor survival and treatment-related toxicity, novel approaches to cure are essential. Previously, we identified the cyclic AMP phosphodiesterase-4 (PDE4) inhibitor Rolipram as a potent antitumor agent. Here, we investigate the role of PDE4 in brain tumors and examine the utility of PDE4 as a therapeutic target. Read More

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http://dx.doi.org/10.1158/1078-0432.CCR-08-0827DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2615415PMC
December 2008
5 Reads