6,074,512 results match your criteria Pharmacology & Pharmacy [Journal]
Eur J Neurosci 2018 Dec 16. Epub 2018 Dec 16.
Department of Pharmacology and Systems Physiology, University of Cincinnati, Cincinnati, Ohio, USA.
Expression of the ciliary neurotrophic factor (CNTF) receptor essential ligand binding subunit, CNTF receptor α (CNTFRα), is induced in motor neurons and skeletal muscle following peripheral nerve lesion. We previously found muscle CNTFRα promotes motor neuron axon regeneration post-lesion. Both nerve lesion and CNTF administration activate motor neuron signal transducer and activator of transcription 3 (STAT3), a transcription factor implicated in axon growth, suggesting CNTF receptors may contribute to the lesion-induced STAT3 activation. Read More
Eur J Neurosci 2018 Dec 16. Epub 2018 Dec 16.
Department of Anatomy, Physiology, and Pharmacology, College of Medicine, University of Saskatchewan, 107 Wiggins Road, Saskatoon, Saskatchewan, S7N 5E5, Canada.
Traumatic brain injury (TBI) is a leading major cause of morbidity and mortality in youth and individuals under 45 year age. A wide variety of cellular and molecular mechanisms have been identified contributing to the pathogenesis of TBI. A better understanding of the pathophysiology behind TBI is essential for providing more effective treatment. Read More
Allergy 2018 Dec 16. Epub 2018 Dec 16.
Center of Allergy and Environment (ZAUM), Technical University of Munich and Helmholtz Center Munich, member of the German Center for Lung Research, 80802, Munich, Germany.
Background: Eicosanoid lipid mediators play key roles in type 2 immune responses, e.g. in allergy and asthma. Read More
Eur J Clin Invest 2018 Dec 16:e13061. Epub 2018 Dec 16.
National Medical Research Center for Preventive Medicine of the Ministry of Healthcare of Russian Federation, 10 Petroverigsky per., Building 3, Moscow, 101990, Russia.
Background: Nitric oxide (NO) is one of the key regulators of vascular function. Abnormal NO signaling is linked to various cardiovascular diseases. We studied associations between circulating levels of nitric oxide metabolites, nitrite and nitrate (NOx), and total and cardiovascular mortality in a prospective 8-year follow-up cohort study in 1869 patients aged over 55 years. Read More
Metab Brain Dis 2018 Dec 15. Epub 2018 Dec 15.
Department of Pharmacy, Institute of toxicology and pharmacology, Zhejiang Pharmaceutical College, Ningbo, 315000, China.
Fucoxanthin (FX), a natural carotenoid abundant in edible brown seaweeds, has been shown the great anti-oxidant, anti-inflammatory and anti-diabetic effects in vivo and in vitro. The present study was designed to investigate the effects of FX on lipopolysaccharide (LPS)-induced behavioral defects in mice. In depressive behavior tests, the increased immobility time of forced swimming test and tail suspension test by LPS treatment in mice, which were significantly reversed by FX treatment (200 mg/kg, i. Read More
Breast Cancer Res Treat 2018 Dec 15. Epub 2018 Dec 15.
Nottingham Breast Cancer Research Centre, Division of Cancer and Stem Cells, School of Medicine, University of Nottingham, Nottingham, UK.
Purpose: CD133/ prominin 1 is a cancer stem cell marker associated with cancer progression and patient outcome in a variety of solid tumours, but its role in invasive breast cancer (BC) remains obscure. The current study aims to assess the prognostic value of CD133 expression in early invasive BC.
Methods: CD133 mRNA was assessed in the METABRIC cohort and at the proteomic level using immunohistochemistry utilising a large well-characterised BC cohort. Read More
Naunyn Schmiedebergs Arch Pharmacol 2018 Dec 15. Epub 2018 Dec 15.
Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany.
Combining bortezomib with other anti-cancer drugs or glucocorticoids is more efficient in multiple myeloma than bortezomib alone. However, the molecular mechanism of this beneficial effect is largely unknown. To investigate the effects of these compounds on bortezomib's anti-proliferative potency and its intracellular accumulation and potency to inhibit the chymotrypsin-like proteasomal subunit, seven myeloma cell lines were investigated after exposure to bortezomib alone or either combined with adriamycin plus dexamethasone (PAD regimen) or melphalan plus prednisolone (VMP regimen), respectively. Read More
Int Orthop 2018 Dec 15. Epub 2018 Dec 15.
2nd Orthopaedics Department, Medical School, University of Athens, Athens, Greece.
Aim Of The Study: The purpose of this historic review is to summarize the life and work of Avicenna (980-1037) and his contribution to the diagnosis and treatment of spinal deformities and trauma.
Method: We conducted an extensive search in libraries as well as online in Pubmed and Google Scholar.
Results: Avicenna in his work Canon of Medicine combines the knowledge of ancient Greek and Roman physicians and surgeons and he combines them with the extensive of Arabic medicine and pharmacology. Read More
Gut 2018 Dec 15. Epub 2018 Dec 15.
Division of Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, Utrecht, The Netherlands.
Objective: Recent evidence suggesting an important role of gut-derived inflammation in brain disorders has opened up new directions to explore the possible role of the gut-brain axis in neurodegenerative diseases. Given the prominence of dysbiosis and colonic dysfunction in patients with Parkinson's disease (PD), we propose that toll-like receptor 4 (TLR4)-mediated intestinal dysfunction could contribute to intestinal and central inflammation in PD-related neurodegeneration.
Design: To test this hypothesis we performed studies in both human tissue and a murine model of PD. Read More
Biomed Pharmacother 2018 Dec 13;110:764-774. Epub 2018 Dec 13.
Laboratory of Molecular Pharmacology, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Pilani Campus, Rajasthan 333 031, India. Electronic address:
Besides assisting the maintenance of blood pressure and sodium homeostasis, the renin-angiotensin system (RAS) plays a pivotal role in pathogenesis of acute kidney injury (AKI). The RAS is equipped with two arms i) the pressor arm composed of Angiotensin II (Ang II)/Angiotensin converting enzyme (ACE)/Angiotensin II type 1 receptor (AT1R) also called conventional RAS, and ii) the depressor arm consisting of Angiotensin (1-7) (Ang 1-7)/Angiotensin converting enzyme 2 (ACE2)/MasR known as non-conventional RAS. Activation of conventional RAS triggers oxidative stress, inflammatory, hypertrophic, apoptotic, and pro-fibrotic signaling cascades which promote AKI. Read More
Psychiatry Res 2018 Dec 6;271:554-558. Epub 2018 Dec 6.
Department of Child and Adolescent Psychiatry and Psychology, Institute of Neurosciences, Hospital Clinic de Barcelona, C/ Villarroel 170, E-08036 Barcelona, Spain; Department of Medicine, University of Barcelona, Barcelona, Spain; The August Pi i Sunyer Biomedical Research Institute (IDIBAPS), Barcelona, Spain; Centro de Investigación Biomédica en Red de Salud Mental (CIBERSAM), Carlos III Health Institute, Spain. Electronic address:
The age of onset of some psychiatric disorders may have etiopathogenic and clinical effects and may influence outcome. Following on from previous work by our group where we showed that early onset anorexia nervosa (AN) and obsessive-compulsive disorder (OCD) shared a common genetic background, the aim of the present study is to assess genetic pleiotropy related to the serotonergic system (SLC6A4, 5HTR2A, 5HTR2C, TPH2, SLC18A1), in a common phenotype such as very-early age of onset. One hundred and sixteen adolescents diagnosed with AN and 74 adolescents diagnosed with OCD participated in the present study. Read More
Biosens Bioelectron 2018 Nov 19;126:773-784. Epub 2018 Nov 19.
Department of Nanotechnology, Faculty of Advanced Sciences and Technology, Tehran Medical Sciences , Islamic Azad University, Tehran, Iran. Electronic address:
Cancer is one of the most important causes of mortality in the world, which can be severely reduced by early detection to avoid future problems in the field of economics and mental health. Hence, electrochemical nanobiosensors as portable devices for rapid detection of cancer biomarkers, have found an important place in clinical medicine for diagnosis, managements or cancer screening. Although, these biosensors have been receiving attention in the recent years, their principles are unchanged. Read More
J Chromatogr B Analyt Technol Biomed Life Sci 2018 Dec 6;1105:10-14. Epub 2018 Dec 6.
Biomedical Microscale Analytics, Division of Systems Biomedicine and Pharmacology, Leiden Academic Center for Drug Research, Leiden University, the Netherlands. Electronic address:
Metabolomics studies using a small amount of cells may save time and money, while in some cases (e.g., profiling pathogenic cells in an early-stage tissue), only a small number of cells are accessible for analysis. Read More
Sleep Med 2018 Nov 22;54:134-141. Epub 2018 Nov 22.
Department of Epidemiology and Biostatistics, College of Public Health, Zhengzhou University, Zhengzhou, Henan, PR China. Electronic address:
Objective: To estimate the prevalence of poor sleep quality and identify related factors by gender in the Chinese rural population.
Methods: Overall, 27424 subjects (10881 males and 16543 females) aged 18-79 years were enrolled from the Henan Rural Cohort Study. Sleep quality was evaluated by the standard Pittsburgh Sleep Quality Index (PSQI) and global score>5 was classified as poor sleep quality. Read More
Nurse Educ Today 2018 Dec 7;74:15-24. Epub 2018 Dec 7.
Faculty of Health and Social Development, School of Nursing, University of British Columbia, Kelowna, BC, Canada.
Objective: In this systematic review we describe best practices for teaching pharmacology to undergraduate baccalaureate nursing students based on the available evidence. Numerous teaching strategies employed in undergraduate pharmacology courses for nursing students have been summarized and compared for their impact on pharmacology knowledge retention, application of pharmacology theory to practice, and student satisfaction. Future directions for research are discussed. Read More
Gene 2018 Dec 13. Epub 2018 Dec 13.
Department of Pharmacology, Faculty of Pharmacy, Marmara University, Istanbul, Turkey.
Alzheimer's disease is a progressive neurodegenerative disorder causing common health problem with increasing age. Evidences show that the key symptoms of AD are mainly caused by cholinergic system dysfunction which has a role in cognitive disorders. Cholinergic pathways especially muscarinic receptors like M subtype also have a major role in learning, memory, cognitive functions and emotional state. Read More
Physiol Behav 2018 Dec 13. Epub 2018 Dec 13.
Iranian National Center for Addiction Studies (INCAS), Tehran University of Medical Sciences, Tehran, Iran; Department of Neuroscience, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran; Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran; Institute for Cognitive Science Studies (ICSS), Tehran, Iran; Endocrinology and Metabolism Research Institute, Tehran University of Medical Science, Tehran, Iran. Electronic address:
Working memory (WM) system, temporarily stores information and uses this information for complex cognitive tasks. WM connects memory, emotional feelings and perception. Evidence compelling that N-methyl d-aspartate receptor (NMDAR) expression relatively affect WM performance in animal models. Read More
Neurosci Lett 2018 Dec 13. Epub 2018 Dec 13.
Department of Pharmacology, Nihon University School of Dentistry, 1-8-13 Kanda-Surugadai, Chiyoda-ku, Tokyo, 101-8310, Japan; Division of Oral and Craniomaxillofacial Research, Dental Research Center, Nihon University School of Dentistry, 1-8-13 Kanda-Surugadai, Chiyoda-ku, Tokyo, 101-8310, Japan; Molecular Dynamics Imaging Unit, RIKEN Center for Life Science Technologies, 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
Temperature plays a critical role in the sensation of airflow in the nasal mucosa. Neural activities of the ethmoidal nerve, a trigeminal afferent, responding to airflow are suppressed by warm airflow, whereas cold airflow enhances the ethmoidal nerve activities, which is mimicked by application of menthol, a cold-sensitive TRPM8 receptor agonist. However, it has been an open issue how menthol modulates the spatiotemporal profiles of neural activities of somatosensory cortical neurons. Read More
Am J Pathol 2018 Dec 13. Epub 2018 Dec 13.
Institute of Hepatology London, Foundation for Liver Research, London, United Kingdom; King's College London, Faculty of Life Sciences and Medicine, London, United Kingdom. Electronic address:
Despite the growing global burden of alcoholic liver diseases, therapeutic options are limited and novel targets are urgently needed. Accumulating evidence suggests that mitochondria adapt in response to ethanol and formation of megamitochondria in the livers of patients is recognized as a hallmark of alcoholic liver diseases. The processes involved in ethanol-induced hepatic mitochondrial changes, the impact on mitochondria-shaping proteins, and the significance of megamitochondria formation remain unknown. Read More
Neuropharmacology 2018 Dec 13. Epub 2018 Dec 13.
Pharmacology and Therapeutics, NCBES Galway Neuroscience Centre, National University of Ireland, Galway, Ireland. Electronic address:
Modulation of the opioid system has re-emerged as a potential therapeutic avenue for treating depression, with efficacy of a fixed-dose combination of buprenorphine (BUP), a partial μ-opioid receptor (MOR) agonist and κ-opioid receptor (KOR) antagonist, and samidorphan (SAM), a potent MOR antagonist, as an adjuvant treatment in patients with major depressive disorder (MDD). To advance understanding of the mechanism of action underlying this combination, we examined BUP, SAM and their combination in a series of rat behavioural assays. We examined effects on locomotor activity in Sprague Dawley (SD) rats over an extended period of time in a home-cage tracking system, and behavioural despair (immobility) in the forced swim test (FST), a commonly-used test to study antidepressants, in SD and Wistar-Kyoto (WKY) rats. Read More
Pharmacol Res 2018 Dec 13. Epub 2018 Dec 13.
Department of Pharmacy, Xiangya Hospital, Central South University, Changsha, 410008, China; National Clinical Research Center for Geriatric Disorders (XIANGYA), Xiangya Hospital, Central South University, Changsha, 410008, Hunan, China. Electronic address:
Stress response refers to the systemic nonspecific response upon exposure to strong stimulation or chronic stress, such as severe trauma, shock, infection, burn, major surgery or improper environment, which disturb organisms and damage their physical and psychological health. However, the pathogenesis of stress induced disorder remains complicated and diverse under different stress exposure. Recently, studies have revealed a specific role of microRNAs (miRNAs) in regulating cellular function under different types of stress, suggesting a significant role in the treatment and prevention of stress-related diseases, such as stress ulcer, posttraumatic stress disorder, stress-induced cardiomyopathy and so on. Read More
Pharmacol Res 2018 Dec 13. Epub 2018 Dec 13.
Division of Experimental Cardiology, Department of Cardiology, Thoraxcenter, Erasmus University Medical Center, Rotterdam, the Netherlands.
Uridine adenosine tetraphosphate (UpA), biosynthesized by activation of vascular endothelial growth factor receptor (VEGFR) 2, was initially identified as a potent endothelium-derived vasoconstrictor in perfused rat kidney. Subsequently, the effect of UpA on vascular tone regulation was intensively investigated in arteries isolated from different vascular beds in rodents including rat pulmonary arteries, aortas, mesenteric and renal arteries as well as mouse aortas, in which UpA produces vascular contraction. In contrast, UpA produces vascular relaxation in porcine coronary small arteries and rat aortas. Read More
Bioorg Med Chem Lett 2018 Dec 10. Epub 2018 Dec 10.
Oncology Biology, Sanofi, 270 Albany Street, Cambridge MA 02139, United States.
N-substituted azaindoles were discovered as promising pan-PIM inhibitors. Lead optimization is described en route toward the identification of a clinical candidate. Modulation of physico-chemical properties allowed to solve inherent hERG and permeability liabilities. Read More
Bioorg Med Chem Lett 2018 Dec 10. Epub 2018 Dec 10.
Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States; Molecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, United States. Electronic address:
Two new cassaine-type diterpenoids, namely erythrofordins D (1) and E (2), sourced from a Cameroon collection of Erythrophleum suaveolens were isolated and assessed for anti-tumor activity. In the NCI-60 cancer cell assay, erythrofordins D (1) and E (2) were found to be cytotoxic in the low micro molar ranges with a mean GI value of 2.45 and 0. Read More
Prog Biophys Mol Biol 2018 Dec 12. Epub 2018 Dec 12.
University of Göttingen, 3rd Institute of Physics - Biophysics, 37077, Göttingen, Germany. Electronic address:
Cardiomyocyte and stroma cell cross-talk is essential for the formation of collagen-based engineered heart muscle, including engineered human myocardium (EHM). Fibroblasts are a main component of the myocardial stroma. We hypothesize that fibroblasts, by compacting the surrounding collagen network, support the self-organization of cardiomyocytes into a functional syncytium. Read More
Curr Opin Insect Sci 2018 Dec 30;30:99-106. Epub 2018 Aug 30.
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907-2089, USA.
The pressing need for new pest control products with novel modes of action has spawned interest in small molecules and peptides targeting arthropod GPCRs. Genome sequence data and tools for reverse genetics have enabled the prediction and characterization of GPCRs from many invertebrates. We review recent work to identify, characterize and de-orphanize arthropod GPCRs, with a focus on studies that reveal exciting new functional roles for these receptors, including the regulation of metabolic resistance. Read More
Prostaglandins Leukot Essent Fatty Acids 2019 Jan 29;140:42-46. Epub 2018 Nov 29.
Nutrition Department, Faculty of Medicine, University of Chile, Santiago, Chile.
Supplementation with omega-3 fatty acids or thyroid hormone (T) exhibit negative effects on inflammatory reactions in experimental animals. The aim of this work was to assess the hypothesis that docosahexaenoic acid (DHA) plus T co-administration enhances liver resolvin (Rv) levels as inflammation resolution mediators. Combined DHA (daily doses of 300 mg/kg for 3 consecutive days)-T (0. Read More
Carbohydr Polym 2019 Feb 17;206:653-663. Epub 2018 Nov 17.
Biomedical Engineering Institute, Jinan University, Guangzhou 510632, PR China. Electronic address:
The rapid emergence of antibiotic-resistant Gram-negative bacteria (GNB) is becoming a global healthcare concern, and it urgently needs novel strategies to match the clinical challenge. In this work, we conjugated chitosan (CS) with LED 209, a highly selective inhibitor of QseC of GNB, to create the novel selective antimicrobial agent CS/LED. The data of FT-IR, NMR and elemental analysis for CS/LED conjugates proved the successful conjugation of CS with LED 209. Read More
Mol Cancer 2018 Dec 15;17(1):174. Epub 2018 Dec 15.
The Institute of Cell Metabolism, Shanghai Key Laboratory of Pancreatic Disease, Shanghai General Hospital, Shanghai Jiaotong University, School of Medicine, Shanghai, 200080, China.
Background: Chromatin modification at mitosis is closely related to transcriptional reactivation in the subsequent cell cycle. We reasoned this process is deregulated by oncogenic signals, which would contribute to mitotic stress resistance in pancreatic cancer. Here, we show DMAP1/Bub3 complex mediates mitotic stress-induced cellular apoptosis, while this effect is counteracted by c-Src in pancreatic cancer cells. Read More
Biomed Pharmacother 2018 Dec 12;110:667-676. Epub 2018 Dec 12.
Department of Pharmacology and Clinical Pharmacy, College of Medicine and Health Sciences, Sultan Qaboos University, P.O. Box 35, Al Khod, 123, Oman.
We assessed the effect of treatment with the dipeptidyl peptidase-4 inhibitor, sitagliptin, on adenine-induced chronic kidney disease (CKD). Six equal groups of rats were given either normal food or food mixed with adenine (0.25% w/w for five weeks) to induce CKD. Read More
Neurobiol Aging 2018 Nov 16;75:62-70. Epub 2018 Nov 16.
Department of Neuropsychiatry, Seoul National University Hospital, Seoul, Republic of Korea; Institute of Human Behavioral Medicine, Medical Research Center, Seoul National University, Seoul, Republic of Korea; Department of Psychiatry, Seoul National University College of Medicine, Seoul, Republic of Korea. Electronic address:
This study aimed to investigate the relationship of hypertension with beta-amyloid (Aβ) and neurodegeneration biomarkers of Alzheimer's disease (AD) and the modulating effect of apolipoprotein E-ε4 (APOE4). In total, 259 cognitively normal (CN) and 79 AD dementia older adults received clinical assessments including the evaluation for the presence of hypertension, [C]-Pittsburgh-compound-B-positron emission tomography, magnetic resonance imaging, and APOE genotyping. We used a clinical stage-specific approach, separately focusing on CN and AD dementia stages. Read More
J Pharm Biomed Anal 2018 Dec 10;165:198-206. Epub 2018 Dec 10.
Bioanalytical Sciences, Bristol-Myers Squibb, Princeton, NJ, 08543, USA.
Stable isotope labeled (SIL) compounds have been commonly used as internal standards (IS) to ensure the accuracy and quality of liquid chromatography-mass spectrometry (LC-MS) bioanalytical assays. Recently, the application of SIL drugs and LC-MS assays to microdose absolute bioavailability (BA) studies has gained increasing attention. This approach can provide significant cost and time saving, and higher data quality compared to the accelerator mass spectrometry (AMS)-based method, since it avoids the use of radioactive drug, high-cost AMS instrumentation and complex measurement processes. Read More
Psychiatry Res 2018 Dec 6;271:516-525. Epub 2018 Dec 6.
School of Nursing, Jilin University, Changchun, China; Department of Pharmacology, college of Basic Medical sciences, Jilin University, Changchun, China. Electronic address:
This study aims to systematically evaluate the efficacy of Pet robot intervention (PRI) for people with dementia. Two waves of electronic searches of the PubMed, EMBASE, Web of Science, Cochrane library, IEEE Digital Library and PsycINFO databases were conducted. In total, eight articles from six randomized controlled trials (RCTs) met the eligibility criteria and were included in this systematic review. Read More
Eur J Pharm Sci 2018 Dec 12. Epub 2018 Dec 12.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Mohali, Punjab 160 062, India. Electronic address:
Breast cancer is the most commonly diagnosed cancer and the leading cause of cancer death in females as per the global cancer project (GLOBOCAN 2018) estimates of breast cancer incidence and mortality produced by the International Agency for Research on Cancer (IARC). In 2018, there will be 2,088,849 new cases of breast cancer and 626,679 cases of deaths due to breast cancer in 5 regions (Americas, Africa, Europe, Asia and Oceania) at 20 sites of the world. Epidemiologic studies on diet and cancer have guided the search for some nutraceuticals acting as anti-cancer agents. Read More
Exp Gerontol 2018 Dec 12. Epub 2018 Dec 12.
Institute of Medical Biology, Chinese Academy of Medical Sciences, Kunming 650118, China; Medical Primate Research Center & Neuroscience Center, Chinese Academy of Medical Sciences, Beijing 100005, China; Yunnan Key Laboratory of Vaccine Research Development on Severe Infectious Diseases, Kunming 650118, China. Electronic address:
The Chinese tree shrew (TS) has many unique advantages that make it suitable for use as an experimental animal model for human disease including moderate body size, low cost of feeding, short reproductive cycle and lifespan, and close phylogenetic relationship to primates. Our previous studies have shown that TS treated with the mitochondrial inhibitor MPTP displayed classic Parkinsonian symptoms. Additionally, the structure of TS alpha-synuclein (α-syn) is highly homologous to that found in humans. Read More
Microb Pathog 2018 Dec 12. Epub 2018 Dec 12.
Department of Kriyasharir Institute of Medical Sciences, Banaras Hindu University, Varanasi, Uttar Pradesh, 221005, India.
Reinwardtia indica (Lineceae) is a medicinal plant cultivated in the Himalayan region. It is effectively used in folk medicines for the treatment of various health complications. In the present study, the shade dried leaves and stem were extracted in three different solvents such as ethyl acetate, ethanol, and hydro-alcoholic. Read More
Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.
The Netherlands Cancer Institute, Division of Pharmacology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands. Electronic address:
Quizartinib, a second-generation FLT3 inhibitor, is in clinical development for the treatment of acute myeloid leukemia. We studied its pharmacokinetic interactions with the multidrug efflux transporters ABCB1 and ABCG2 and the multidrug metabolizing enzyme CYP3A, using in vitro transport assays and knockout and transgenic mouse models. Quizartinib was transported by human ABCB1 in vitro, and by mouse (m)Abcb1 and mAbcg2 in vivo. Read More
J Ethnopharmacol 2018 Dec 12. Epub 2018 Dec 12.
Laboratory of Oncological Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, 646000, Sichuan, PR China; Key Laboratory of Gastrointestinal Pharmacology of Chinese Materia Medica of the State Administration of Traditional Chinese Medicine, Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Xi'an 710032, Shaanxi, PR China. Electronic address:
Ethnopharmacological Relevance: The development of a multidrug-resistant (MDR) phenotype is a main obstacle to the successful treatment of breast cancer. Saponins of several herbs are considered as promising candidates for drug resistance treatment. We extracted Paris saponin VII (PS VII) from Trillium tschonoskii Maxim. Read More
Pharmacol Res 2018 Dec 12. Epub 2018 Dec 12.
Department of Medicine, Section of Pharmacology, University of Perugia, Italy.
Cannabinoids are known to possess anti-inflammatory and immunomodulatory properties, but the mechanisms involved are not fully understood. CB2 is the cannabinoid receptor that is expressed primarily on hematopoietic cells and mediates the immunoregulatory functions of cannabinoids. In order to study the effect of JTE907, a selective/inverse agonist of CB2 with anti-inflammatory properties, on the differentiation of T cell subtypes, we used an in vitro system of Th lineage-specific differentiation of naïve CD4 T lymphocytes isolated from the mouse spleen. Read More
J Pharmacol Toxicol Methods 2018 Dec 12. Epub 2018 Dec 12.
Office of Translational Science, Office of Clinical Pharmacology, Division of Applied Regulatory Science, U.S. Food and Drug Administration, Center for Drug Evaluation and Research, White Oak Federal Research Center, 10903 New Hampshire Ave, Silver Spring, MD 20993, USA. Electronic address:
Topical ophthalmic drugs are the most commonly used dosage form to treat diseases of the anterior segment of the eye. Although this dosage form has the advantages of ease of application, small volume dose, and rapid action and is largely devoid of systemic adverse effects, the bioavailability is low due to pre-corneal anatomical barriers and the nature of the drug formulation itself. Some complex generic formulations (suspensions, ointments, gels) for topical ophthalmic products face impediments to rapid regulatory approval because of the complex nature of the formulations and difficulties in determining bioequivalence with the innovator product. Read More
Toxicology 2018 Dec 12. Epub 2018 Dec 12.
Laboratory of Pharmacology and Pathophysiology, Faculty of Pharmacy, Kindai University (formerly known as Kinki University), Higashi-Osaka, 577-8802, Japan. Electronic address:
Bortezomib, a first-line agent for treatment of multiple myeloma, exhibits anticancer activity through proteasome inhibition. However, bortezomib-induced peripheral neuropathy (BIPN) is one of the most serious side effects. Since decreased proteasomal degradation of Ca3. Read More
Life Sci 2018 Dec 12. Epub 2018 Dec 12.
Department of Pharmacology, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India. Electronic address:
Cyclophosphamide (CP) is an important anticancer drug which belongs to the class of alkylating agent. Cyclophosphamide is mostly used in bone marrow transplantation, rheumatoid arthritis, lupus erythematosus, multiple sclerosis, neuroblastoma and other types of cancer. Dose-related cardiotoxicity is a limiting factor for its use. Read More
Behav Brain Res 2018 Dec 12. Epub 2018 Dec 12.
Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA, 23298, USA. Electronic address:
The objective of the present study is to investigate the role of α4, α5, α6 or β2 nAChR subunits in the antidepressant-like effect of bupropion. Adult male mice were treated with subcutaneous acute doses of bupropion (3 and 10 mg/kg) 30 min before the forced swim test (FST) in α4, α5, α6, or β2 nAChR subunit knockout (KO) and wild-type (WT) mice. In addition, the effects of β2* antagonist dihydro-β-erythroidine (DHβE, 3 mg/kg) on antidepressant-like effects of bupropion in C57BL/6 J mice were assessed. Read More
Behav Brain Res 2018 Dec 12. Epub 2018 Dec 12.
The Brain and Muscle Energy Group, Electron Microscopy Laboratory, Department of Oral Biology, University of Oslo, NO-0316, Oslo, Norway; Synaptic Neurochemistry and Amino Acid Transporters Labs, Division of Anatomy, Department of Molecular Medicine, Institute of Basic Medical Sciences (IMB) and Healthy Brain Ageing Centre (SERTA), University of Oslo, NO-0317, Oslo, Norway; Center for Healthy Aging, Department of Neuroscience and Pharmacology, Faculty of Health Sciences, University of Copenhagen, DK-2200 Copenhagen N, Denmark.
Glutamatergic α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) carry the bulk of excitatory synaptic transmission. Their modulation plays key roles in synaptic plasticity, which underlies hippocampal learning and memory. A dysfunctional glutamatergic system may negatively affect learning abilities and underlie symptoms of attention-deficit/hyperactivity disorder (ADHD). Read More
Neuropharmacology 2018 Dec 12. Epub 2018 Dec 12.
Department of Psychiatry, Psychotherapy and Psychosomatics, Faculty of Medicine, RWTH Aachen University, 52074, Aachen, Germany; JARA Institute Brain Structure Function Relationship Institute for Neuroscience and Medicine (INM 10), Forschungszentrum Jülich, 52425 Jülich, Germany.
Current models of aggression suggest that in addition to personality traits and environmental factors, biological vulnerability associated with genetics substantially impacts aggressive behavior. In a functional imaging study, we investigated the influence of the single nucleotide polymorphism of the mu 1 subtype opioid receptor gene (OPRM1), implicated in sociability, on correlates of trait and state aggression to delineate the function of these influences in aggression. A key aim was further to differentiate different aspects of aggressive reactions - namely, the reaction to provocation and the decision to punish an opponent. Read More
Eur J Pharmacol 2018 Dec 12. Epub 2018 Dec 12.
Department of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, VA, USA. Electronic address:
Mu-opioid receptor agonists are clinically effective analgesics, but also produce undesirable effects that limit their clinical utility. The nociceptin opioid peptide (NOP) receptor system also modulates nociception, and NOP agonists might be useful adjuncts to enhance the analgesic effects or attenuate the undesirable effects of mu-opioid agonists. The present study determined behavioral interactions between the NOP agonist (-)-Ro 64-6198 and mu-opioid ligands that vary in mu-opioid receptor efficacy (17-cyclopropylmethyl-3,14β-dihyroxy-4,5α-epoxy-6α-[(3 ́-isoquinolyl)acetamindo]morphinan (NAQ) < buprenorphine < nalbuphine < morphine = oxycodone < methadone) in male rhesus monkeys. Read More
Eur J Pharmacol 2018 Dec 12. Epub 2018 Dec 12.
Institute of Pharmacology and Toxicology, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China, 310058. Electronic address:
Osteosarcoma is the most common primary malignant bone tumour, but the survival rate of patients has plateaued since the mid-1980s. Adriamycin is an integral component of the current first-line chemotherapies used for osteosarcoma, but dose-dependent severe side effects often limit its clinical application. Here, we propose a potential combination regimen in which adriamycin plus 2-bromopalmitate, a palmitoylation inhibitor, exhibited powerful therapeutic effects on osteosarcoma. Read More
Eur J Pharmacol 2018 Dec 12. Epub 2018 Dec 12.
Centre National de la Recherche Scientifique and University of Strasbourg, Institut des Neurosciences Cellulaires et Intégratives, 67000 Strasbourg, France. Electronic address:
Inflammatory processes are critical promoting factors of chronic pain states, mostly by inducing peripheral and central sensitization of the nociceptive system. These processes are associated with a massive increase in glutamatergic transmission, sometimes facilitated by spinal disinhibition. In this study, we used etifoxine, a non-benzodiazepine anxiolytic known to amplify inhibition mediated by gamma-aminobutyric acid type A (GABA) receptors in pain processing regions, either directly (through allosteric modulation) or indirectly (through the synthesis of endogenous neurosteroids). Read More
Angew Chem Int Ed Engl 2018 Dec 15. Epub 2018 Dec 15.
Concepts leading to single enantiomers of chiral molecules are of crucial importance for many applications, including pharmacology and biotechnology. Recently, mesoporous metal phases encoded with chiral information have been developed. We propose here to fine-tune the enantioaffinity of such structures by imposing an electric potential, which can influence the electrostatic interactions between the chiral metal and the target enantiomer. Read More
Arthritis Rheumatol 2018 Dec 15. Epub 2018 Dec 15.
Division of Rheumatology, Ospedale Pediatrico Bambino Gesù, IRCCS, Rome, Italy.
Objectives: Our aim was to evaluate expression of type I interferon (IFNα/β)- and type II IFN (IFNγ)-inducible genes in muscle biopsies of JDM patients and to correlate their expression levels with histological and clinical features.
Methods: Expression levels of IFN-inducible genes and pro-inflammatory cytokines were assessed by quantitative PCR in muscle biopsies of JDM patients (n = 39), Duchenne muscular dystrophy (DMD) patients (n = 24) and healthy controls (HCs) (n = 4). Histological and immunofluorescence studies were performed on muscle biopsy sections. Read More