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Pharmacology

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https://www.readbyqxmd.com/read/29141251/opioid-receptors-contribute-to-antinociceptive-effect-of-tianeptine-on-colorectal-distension-induced-visceral-pain-in-rats
#1
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
#2
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/29131074/tranexamic-acid-failed-to-reverse-the-anticoagulant-effect-and-bleeding-by-an-oral-direct-factor-xa-inhibitor-edoxaban
#3
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...
November 3, 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
#4
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
#5
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/29131082/aspirin-inhibits-platelet-derived-sphingosine-1-phosphate-induced-endothelial-cell-migration
#6
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...
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
#7
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/28988245/basic-in-vitro-characterization-of-the-vasodilatory-potential-of-2-aminoethyl-nitrate-fixed-dose-combinations-with-cilostazol-metoprolol-and-valsartan
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/28898893/effects-of-artesunate-on-the-expressions-of-insulin-like-growth-factor-1-osteopontin-and-c-telopeptides-of-type-ii-collagen-in-a-rat-model-of-osteoarthritis
#14
Zhe Bai, Xiao-Hui Guo, Chi Tang, Si-Tong Yue, Long Shi, Bo Qiang
OBJECTIVE: The study aims to explore the effects of artesunate on insulin-like growth factor-1 (IGF-1), Osteopontin (OPN), and C-telopeptides of type II collagen (CTX-II) in serum, synovial fluid (SF), and cartilage tissues of rats with osteoarthritis (OA). METHODS: OA models were established. Normal model, artesunate, and Viatril-S groups (20 rats respectively) were set. Enzyme-linked immunosorbent assay, IHC staining, and quantitative real-time polymerase chain reaction were conducted to calculate IGF-1, OPN, and CTX-II levels in serum, SF, and cartilage tissues of rats...
September 13, 2017: Pharmacology
https://www.readbyqxmd.com/read/28848223/mechanistic-evaluation-of-the-protective-effect-of-carnosine-on-acute-lung-injury-in-sepsis-rats
#15
Chenliang Sun, Qinfeng Wu, Xuejie Zhang, Qianru He, Hongsheng Zhao
This study analyzes the sepsis healing therapeutic potential of carnosine against experimentally sepsis-induced male albino rats. Carnosine in 2 different doses, 25 mg/kg and 50 mg/kg, were administered for 30 consecutive days. At the end of the treatment, lipid peroxidation, catalase, superoxide dismutase, glutathione peroxidase and myeloperoxidase activities were measured. Lungs weight and total protein content were determined in the bronchoalveolar fluid (BALF). Cytokines such as macrophage inhibitory factor (MIF), interleukin-8 (IL-8) and tumour necrosis factor-alpha (TNF-α) were determined in the BALF...
August 25, 2017: Pharmacology
https://www.readbyqxmd.com/read/28848215/inhibitory-effect-of-citalopram-on-the-pharmacokinetics-of-carvedilol-in-rats-and-in-vitro-models
#16
Maria Bianca Abrudan, Dana Maria Muntean, Daniela Saveta Popa, Ana-Maria Gheldiu, Maria Adriana Neag, Laurian Vlase
BACKGROUND/AIMS: The aim of this study was to investigate the drug-drug interaction between carvedilol and citalopram based on carvedilol metabolism in vitro and his pharmacokinetics (PKs) in vivo after the oral administration of the single drug and both drugs, and reveal citalopram effects on the PKs of carvedilol. METHODS: Each rat was cannulated on the femoral vein, prior to being connected to BASi Culex ABC®. Carvedilol was orally administrated in rats (3.57 mg/kg body weight [b...
August 19, 2017: Pharmacology
https://www.readbyqxmd.com/read/28848138/heat-shock-protein-27-a-novel-regulator-of-transforming-growth-factor-%C3%AE-induced-resistance-to-cisplatin-in-a549-cell
#17
Zhicheng Huang, Changliang Yang, Shuangyan Sun, Yingji Nan, Zhiguo Lang, Xiu Wang, Jihong Zhao, Ying Liu
Lung cancer is one of the major causes of cancer morbidity and mortality around the world, and the resistance to cisplatin is a critical issue to chemotherapy in lung cancer patients. Transforming growth factor β (TGF-β) signal pathway abnormality is widely observed in drug resistance during lung cancer chemotherapy. Here, we investigated the effects of heat-shock protein 27 (HSP27) in the TGF-β-induced cisplatin resistance in lung cancer cell. In this study, our results indicated that the mRNA and protein expression of HSP27 were significantly increased in human lung cancer tissues...
August 19, 2017: Pharmacology
https://www.readbyqxmd.com/read/28810242/mir-490-5p-suppresses-cell-proliferation-and-invasion-by-targeting-bub1-in-hepatocellular-carcinoma-cells
#18
Bin Xu, Tangpeng Xu, Huali Liu, Qian Min, Shidong Wang, Qibin Song
OBJECTIVE: To verify that miR-490-5p could influence hepatocellular carcinoma (HCC) cells' proliferation, invasion, cycle, and apoptosis by targeting BUB1. METHODS: Quantitative real time-PCR (QRT-PCR) was used to determine the miR-490-5p expression. Immunohistochemistry, qRT-PCR, and Western blot were employed to detect BUB1 and transforming growth factor-beta (TGFβ/Smad) signaling-related proteins expression in hepatic tissues and cells. The luciferase assay was used to confirm the targeting relationship between miR-490-5p and BUB1...
August 16, 2017: Pharmacology
https://www.readbyqxmd.com/read/28797008/resveratrol-attenuates-adriamycin-induced-focal-segmental-glomerulosclerosis-through-c3ar-c5ar-sphingosine-kinase-1-pathway
#19
Guoyong Liu, Qiang Wang, Yan Shi, Xiaofei Peng, Hong Liu, Youming Peng, Liyu He
BACKGROUND/AIM: Focal segmental glomerulosclerosis (FSGS) typically presents with nephrotic range proteinuria, which could eventually develop into end-stage renal disease. Resveratrol (RSV) is a natural polyphenol compound, which has been reported to suppress inflammatory response and renal interstitial fibrosis. This study is aimed at evaluating the renoprotective effect of RSV treatment on adriamycin-induced FSGS. METHODS: In Balb/c mice, adriamycin nephropathy was induced by adriamycin (10 mg/kg body weight, diluted in normal saline) via a tail vein on day 0...
August 11, 2017: Pharmacology
https://www.readbyqxmd.com/read/28797006/amiloride-is-effective-in-the-management-of-abiraterone-induced-mineralocorticoid-excess-syndrome-without-interfering-with-its-antineoplastic-activity
#20
Francesca Bedussi, Diego Galli, Martina Fragni, Francesca Valcamonico, Elisa Rossini, Alberto Dalla Volta, Sara Vezzoli, Elisa Roca, Vittorio Ferrari, Barbara Lazzari, Maurizio Memo, Sandra Sigala, Alfredo Berruti
BACKGROUND: The administration of abiraterone acetate (abiraterone) leads to an adrenocorticotropic hormone (ACTH)-driven increase in mineralocorticoid hormones, requiring glucocorticoid supplementation that may stimulate the growth of prostate cancer (PCa). Amiloride is a drug that selectively reduces the aldosterone-sensitive Na+/K+ exchange and could be effective in the management of mineralocorticoid excess syndrome (MCES). METHODS: The efficacy of amiloride + hydrochlorothiazide (HCT) in the clinical management of abiraterone-induced MCES was assessed in 5 consecutive patients with castration-resistant PCa (CRPC)...
August 11, 2017: Pharmacology
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