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Pharmacology

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https://www.readbyqxmd.com/read/29301138/the-effect-of-cisplatin-on-blood-ammonia-elevation-by-alanyl-glutamine-supplementation
#1
Yoko Obayashi, Kenta Kajiwara, Eiji Nakamura
BACKGROUND: Although there are many clinical studies in which the beneficial effect of glutamine formulation on mucositis induced by chemo/radiotherapy was evaluated, the results are sometimes conflicting with the report of clinical deterioration. Then, we hypothesized that chemotherapy may increase the incidence of hyperammonemia without comparable change of major parameters of hepatic/renal disorder. METHODS: To verify our hypothesis, we examined the increase in blood ammonia level with 1-h intravenous infusion of alanyl-glutamine on day 1-4 after cisplatin (CDDP) administration in rats and assessed the correlation with hepatic/renal parameters...
January 4, 2018: Pharmacology
https://www.readbyqxmd.com/read/29301136/assessment-of-the-airway-smooth-muscle-relaxant-effect-of-drotaverine
#2
Zoltán Patai, András Guttman, Endre G Mikus
BACKGROUND: Drotaverine, a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor, blocks the degradation of 3',5'-cyclic adenosine monophosphate. However, published receptor binding data showed that drotaverin also binds to the L-type voltage-operated calcium channel (L-VOCC). Based on these molecular mechanisms of action, a direct and indirect (by blocking the constrictor response) relaxant effect on airway smooth muscle can be predicted, which has not yet been assessed. SUMMARY: Accordingly, drotaverine and reference agents were tested both on the histamine-, methacholine-, or KCl-induced contraction response and on precontracted guinea pig tracheal preparations...
January 4, 2018: Pharmacology
https://www.readbyqxmd.com/read/29275416/mechanism-of-action-of-the-anti-influenza-virus-active-kampo-traditional-japanese-herbal-medicine-hochuekkito
#3
Katsuaki Dan, Keita Takanashi, Hiroko Akiyoshi, Kaori Munakata, Hideki Hasegawa, Kaoru Ogawa, Kenji Watanabe
When the Kampo medicine, Hochuekkito (Hochu), was administered to normal mice for 2 weeks, influenza virus titer was reduced. The mechanism of action of Hochu was examined using the plaque assay method. It was suggested that Hochu may either obstruct the first stage of the infection process (adsorption and entry) or may directly target viral particles. Using the plaque assay method, these 2 modes of action could not be differentiated. Virus RNA in the infected cell was verified by quantitative real-time polymerase chain reaction...
December 22, 2017: Pharmacology
https://www.readbyqxmd.com/read/29248915/using-controlled-substance-receipt-patterns-to-predict-prescription-overdose-death
#4
Christina T Holt, Kenneth L McCall, Gary Cattabriga, Chunhao Tu, Elenna K Smalley, Stephanie D Nichols
BACKGROUND: This study evaluates complete state data from controlled substance prescribing trends in the prescription monitoring program (PMP) database and their association with the risk of prescription drug overdose death. SUMMARY: Maine PMP records of individuals who died of prescription overdose deaths between 2006 and 2010 were selected (n = 690). For each subject, an age, gender, and residence matched cohort of PMP users in a 50: 1 ratio was identified (n = 34,500)...
December 14, 2017: Pharmacology
https://www.readbyqxmd.com/read/29207398/involvement-of-n-methyl-d-aspartic-acid-receptor-and-dl-%C3%AE-amino-3-hydroxy-5-methyl-4-isoxazole-propionic-acid-receptor-in-ginsenosides-rb1-and-rb3-against-oxygen-glucose-deprivation-induced-injury-in-hippocampal-slices-from-rat
#5
Shan Jiang, De-Fang Fang, Ying Chen
OBJECTIVE: Ginsenosides, Rb1 and Rb3, are the major protopanaxadiol components of ginseng saponin. In the present study, the influences of ginsenosides Rb1 and Rb3 on N-methyl-D-aspartic acid (NMDA) receptor or DL-α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor-mediated synaptic transmission after oxygen-glucose deprivation (OGD) were investigated. METHODS: NMDA receptor population spike (NMDA-PS) or AMPA receptor-mediated population spike (AMPA-PS) was recorded in the CA1 pyramidal cell layer of rat hippocampal slices by electrophysiological techniques...
December 5, 2017: Pharmacology
https://www.readbyqxmd.com/read/29190633/contractile-responses-in-spontaneously-hypertensive-rats-after-transient-middle-cerebral-artery-occlusion
#6
Anne-Sofie Grell, Maryam Mostajeran, Lars Edvinsson, Saema Ansar
Stroke is one of the leading causes of mortality and morbidity worldwide, and few therapeutic treatments have shown beneficial effect clinically. One reason for this could be the lack of risk factors incorporated into the preclinical stroke research. We have previously demonstrated phenotypic receptor changes to be one of the injurious mechanisms occurring after stroke but mostly in healthy rats. The aim of this study was to investigate if hypertension has an effect on vasoconstrictive receptor responses to endothelin 1, sarafotoxin 6c and angiotensin II after stroke by inducing transient middle cerebral artery occlusion in spontaneously hypertensive rats and Wistar-Kyoto rats using the wire-myograph...
November 30, 2017: Pharmacology
https://www.readbyqxmd.com/read/29186713/phosphatidylcholine-causes-lipolysis-and-apoptosis-in-adipocytes-through-the-tumor-necrosis-factor-alpha-dependent-pathway
#7
Tae Woo Jung, Sung Tae Kim, Jun Ho Lee, Soo In Chae, Kwang Woo Hwang, Yoon Hee Chung, Hyoung-Chun Kim, A M Abd El-Aty, Tae Jin Lee, Eon Sub Park, Ji Hoon Jeong
A phosphatidylcholine (PPC) formulation has been used to treat cellulite; however, its underlying mechanism of action remains unclear. In this study, we demonstrated that PPC induces lipolysis and apoptosis in adipocytes, and evaluated a possible tumor necrosis factor alpha (TNFα)-dependent pathway, whereby PPC exerts these effects. For in vitro study, fully differentiated 3T3-L1 cells, mouse adipocytes were treated with various concentrations of PPC and cell apoptosis and lipolysis were assayed. For in vivo experiments, mice fed on a high-fat diet for 8 weeks were injected twice to abdominal subcutaneous fat tissues of either vehicle or PPC...
November 29, 2017: Pharmacology
https://www.readbyqxmd.com/read/29141251/opioid-receptors-contribute-to-antinociceptive-effect-of-tianeptine-on-colorectal-distension-induced-visceral-pain-in-rats
#8
S Sırrı Bilge, Fatih İlkaya, Özge Darakcı, Engin Çiftcioğlu, Ayhan Bozkurt
Tianeptine is a clinically effective atypical antidepressant with distinct neurochemical properties. In this study, we aimed to investigate the contribution of opioid receptors in the antinociceptive effect of tianeptine on visceral pain in awake rats and to differentiate the subtype and the localization (central and/or peripheral) of these opioid receptors involved in this antinociception. Visceromotor response to noxious colorectal distension (CRD) was quantified with electromyographic recordings, obtained from previously implanted electrodes into the external oblique musculature of rats under anesthesia, before and after tianeptine administration...
November 15, 2017: Pharmacology
https://www.readbyqxmd.com/read/29136631/drug-induced-pseudoallergy-a-review-of-the-causes-and-mechanisms
#9
Bo Zhang, Qin Li, Chenyang Shi, Xinyue Zhang
Adverse drug reactions occur frequently and can trigger pseudoallergy, which has become a serious threat to public health. Pseudoallergy is a typical non-immune anaphylactic reaction characterized by the independence of antigen-specific immune responses. In the clinic, pseudoallergy is often elicited by the first dose of medication, and here lies its unpredictability and occasional lethal outcome. However, the mechanisms of pseudoallergy are not well understood. This review focusses on the causes and mechanisms of pseudoallergy induced by drugs...
November 15, 2017: Pharmacology
https://www.readbyqxmd.com/read/29131133/sulphonated-formononetin-induces-angiogenesis-through-vascular-endothelial-growth-factor-camp-response-element-binding-protein-early-growth-response-3-vascular-cell-adhesion-molecule-1-and-wnt-%C3%AE-catenin-signaling-pathway
#10
Zhaoju Dong, Yanan Shi, Huijuan Zhao, Ning Li, Liang Ye, Shuping Zhang, Haibo Zhu
BACKGROUND: Sodium formononetin-3'-sulphonate (Sul-F) is a derivative of the isoflavone formononetin. In this study, we investigated whether Sul-F can regulate angiogenesis and the potential mechanism in vitro. METHODS: We examined the effects of Sul-F on cell proliferation, cell invasion, and tube formation in the human umbilical vein endothelial cell line (HUVEC). To better understand the mechanism involved, we investigated effects of the following compounds: cAMP response element-binding protein (CREB) inhibitor 2-naphthol-AS-E-phosphate (KG-501), early growth response 3 (Egr-3) siRNA, vascular endothelial growth factor (VEGF) antagonist soluble VEGF receptor 1 (sFlt-1), VEGF receptor 2 blocker SU-1498, Wnt5a antagonist WIF-1 recombinant protein (WIF-1), and inhibitor of Wnt/β-catenin recombinant Dickkopf-1 protein (DKK-1)...
October 31, 2017: Pharmacology
https://www.readbyqxmd.com/read/29131129/effect-of-diazepam-on-24-hour-blood-pressure-and-heart-rate-in-healthy-young-volunteers
#11
Alfredo Costa, Daniele Bosone, Annalisa Zoppi, Angela D Apos Angelo, Natascia Ghiotto, Elena Guaschino, Matteo Cotta Ramusino, Roberto Fogari
AIM: To assess the effects of evening chronic administration of diazepam on 24-h blood pressure (BP) and heart rate (HR) in healthy young adults. METHODS: This randomized double blind, cross-over study evaluated the effects of diazepam 5 mg or placebo, both ingested in the evening, on 24-h ambulatory BP and HR in healthy subjects aged 21-30. RESULTS: A total of 30 subjects were included in the analysis. At the end of 4-week diazepam intake, an increase in 24-h HR mean values was found (+5...
October 31, 2017: Pharmacology
https://www.readbyqxmd.com/read/29065407/hypoxic-stress-upregulates-the-expression-of-slc38a1-in-brown-adipocytes-via-hypoxia-inducible-factor-1%C3%AE
#12
Tetsuhiro Horie, Kazuya Fukasawa, Takashi Iezaki, Gyujin Park, Yuki Onishi, Kakeru Ozaki, Takashi Kanayama, Manami Hiraiwa, Yuka Kitaguchi, Katsuyuki Kaneda, Eiichi Hinoi
The availability of amino acid in the brown adipose tissue (BAT) has been shown to be altered under various conditions; however, little is known about the possible expression and pivotal role of amino acid transporters in BAT under physiological and pathological conditions. The present study comprehensively investigated whether amino acid transporters are regulated by obesogenic conditions in BAT in vivo. Moreover, we investigated the mechanism underlying the regulation of the expression of amino acid transporters by various stressors in brown adipocytes in vitro...
October 25, 2017: Pharmacology
https://www.readbyqxmd.com/read/29131082/aspirin-inhibits-platelet-derived-sphingosine-1-phosphate-induced-endothelial-cell-migration
#13
Amin Polzin, Betül Knoop, Andreas Böhm, Lisa Dannenberg, Mark Zurek, Tobias Zeus, Malte Kelm, Bodo Levkau, Bernhard H Rauch
BACKGROUND: Aspirin plays a crucial role in the prevention of cardiovascular diseases. We previously described that aspirin has effects beyond inhibition of platelet aggregation, as it inhibited thrombin-mediated release of sphingosine-1-phosphate (S1P) from human platelets. S1P is a bioactive lipid with important functions on inflammation and apoptosis. In endothelial cells (EC), S1P is a key regulator of cell migration. In this study, we aimed to analyze the effects of aspirin on platelet-induced EC migration...
2018: Pharmacology
https://www.readbyqxmd.com/read/29131074/tranexamic-acid-failed-to-reverse-the-anticoagulant-effect-and-bleeding-by-an-oral-direct-factor-xa-inhibitor-edoxaban
#14
Yuko Honda, Taketoshi Furugohri, Yoshiyuki Morishima
BACKGROUND/AIMS: Agents to reverse the anticoagulant effect of edoxaban, an oral direct factor Xa inhibitor, would be desirable in emergency situations. The aim of this study is to determine the effect of tranexamic acid, an antifibrinolytic agent, on the anticoagulant activity and bleeding by edoxaban in rats. METHODS: A supratherapeutic dose of edoxaban (3 mg/kg) was intravenously administered to rats. Three minutes after dosing, tranexamic acid (100 mg/kg) was given intravenously...
2018: Pharmacology
https://www.readbyqxmd.com/read/28988245/basic-in-vitro-characterization-of-the-vasodilatory-potential-of-2-aminoethyl-nitrate-fixed-dose-combinations-with-cilostazol-metoprolol-and-valsartan
#15
Matthias Oelze, Philipp Welschof, Maike Knorr, Lan P Tran, Elisabeth Ullmann, Paul Stamm, Swenja Kröller-Schön, Thomas Jansen, Maximilian Kopp, Eberhard Schulz, Tommaso Gori, Karl Burgin, Armin Scherhag, Dirk Sartor, Thomas Münzel, Andreas Daiber
BACKGROUND/AIMS: 2-aminoethyl nitrate (CLC-1011) is a member of the class of organic nitrates that cause vasodilation by the generation of nitric oxide (•NO). These drugs are mainly used for the treatment of angina pectoris and ischemic heart disease. The aim of this study was to characterize the vasodilatory potency of this organic nitrate alone and in combination with clinically established cardiovascular drugs. METHODS: Vasodilation by CLC-1011 was tested by isometric tension studies, either alone or combined with cilostazol, valsartan, and metoprolol...
October 7, 2017: Pharmacology
https://www.readbyqxmd.com/read/28988243/efficacy-in-treating-lung-metastasis-of-invasive-breast-cancer-with-functional-vincristine-plus-dasatinib-liposomes
#16
Fan Zeng, Rui-Jun Ju, Lei Liu, Hong-Jun Xie, Li-Min Mu, Wan-Liang Lu
BACKGROUND: The metastasis of breast cancer is the leading cause of death, while lung metastasis is a major clinical phenomenon in patients with invasive breast cancer. The current treatment option comprising surgery, radiation, and standard chemotherapy cannot achieve a satisfactory effect on the treatment of lung metastasis of breast cancer. In this study, we report the potential of preventing lung metastasis of invasive breast cancer using the newly developed functional vincristine plus dasatinib liposomes...
October 7, 2017: Pharmacology
https://www.readbyqxmd.com/read/28965119/thiadiazolidinone-8-ameliorates-inflammation-associated-with-experimental-colitis-in-mice
#17
Vanessa Mateus, João Rocha, Paula Alves, Hélder Mota-Filipe, Bruno Sepodes, Rui Pinto
Thiadiazolidinone-8 (TDZD-8) is an effective thiadiazolidinone derivate that is able to suppress the expression of inflammatory cytokines; it also presents tissue protective actions by glycogen synthase kinase (GSK)-3β inhibition, promoting thus an anti-inflammatory effect. Since inflammatory bowel disease is a chronic disease with reduced quality of life, where currently available therapies are only able to induce or maintain the patient in remission, it is crucial to investigate new pharmacological approaches...
September 30, 2017: Pharmacology
https://www.readbyqxmd.com/read/28930747/quantification-of-bisoprolol-and-metoprolol-in-simultaneous-human-serum-and-cerebrospinal-fluid-samples
#18
Ali Sigaroudi, Martina Kinzig, Oliver Wahl, Christoph Stelzer, Michael Schroeter, Uwe Fuhr, Ulrike Holzgrabe, Fritz Sörgel
BACKGROUND: Bisoprolol and metoprolol are moderately lipophilic, beta(1)-selective betablockers reported to cause adverse effects in the central nervous system (CNS), such as sleep disturbance, suggesting that both drugs may reach relevant concentrations in the brain. CNS beta(2)-receptor blockade has been suspected to be related to such effects. The higher molecular size of bisoprolol (325 Dalton) and the higher beta(1)-selectivity compared to metoprolol (267 Dalton) would suggest a lower rate of CNS effects...
September 21, 2017: Pharmacology
https://www.readbyqxmd.com/read/28926842/pharmacotherapy-with-thymoquinone-improved-pancreatic-%C3%AE-cell-integrity-and-functional-activity-enhanced-islets-revascularization-and-alleviated-metabolic-and-hepato-renal-disturbances-in-streptozotocin-induced-diabetes-in-rats
#19
Adel Galal El-Shemi, Osama Adnan Kensara, Aiman Alsaegh, Mohammed Hasan Mukhtar
AIMS: This study is aimed at evaluating the antidiabetic effects of thymoquinone (TQ) on streptozotocin (STZ)-induced diabetes in rats, and exploring the possible underlying mechanisms. METHODS: Diabetes was induced in adult male Wistar rats by intraperitoneal injection of freshly prepared STZ (65 mg/kg). After disease induction, 42 rats were equally assigned to: controls, STZ-diabetic group, and STZ-diabetic group treated with oral TQ (35 mg/kg/day) for 5 weeks...
September 20, 2017: Pharmacology
https://www.readbyqxmd.com/read/28926841/beneficial-combination-of-lacosamide-with-retigabine-in-experimental-animals-an-isobolographic-analysis
#20
Jarogniew J Luszczki, Mirosław Zagaja, Barbara Miziak, Maria W Kondrat-Wrobel, Katarzyna Zaluska, Paula Wroblewska-Luczka, Piotr Adamczuk, Stanislaw J Czuczwar, Magdalena Florek-Luszczki
BACKGROUND/AIM: To isobolographically determine the types of interactions that occur between retigabine and lacosamide (LCM; two third-generation antiepileptic drugs) with respect to their anticonvulsant activity and acute adverse effects (sedation) in the maximal electroshock-induced seizures (MES) and chimney test (motor performance) in adult male Swiss mice. METHODS: Type I isobolographic analysis for nonparallel dose-response effects for the combination of retigabine with LCM (at the fixed-ratio of 1:1) in both the MES and chimney test in mice was performed...
September 20, 2017: Pharmacology
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