4,549 results match your criteria Pharmacology[Journal]


In vitro Inhibitory Effects of Isofraxidin on Human Liver Cytochrome P450 Enzymes.

Pharmacology 2018 Dec 13;103(3-4):120-127. Epub 2018 Dec 13.

Isofraxidin is a Coumarin compound widely distributed in plants, such as the Umbelliferae or Chloranthaceae, and it possesses numerous pharmacological activities. However, whether isofraxidin affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. In this study, the inhibitory effects of isofraxidin on the 8 human liver CYP isoforms (i. Read More

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December 2018

Ameliorative Effect of Withaferin A on Ageing-Mediated Impairment in the Dopamine System and Its Associated Behavior of Wistar Albino Rat.

Pharmacology 2018 Dec 13;103(3-4):114-119. Epub 2018 Dec 13.

Department of Anatomy, Velammal Medical College and Hospital, Madurai,

Withaferin A (WA) was evaluated for its neuro-protective efficacy on ageing induced striatal dopamine (DA) and behavioural changes in aged rats. Wistar albino rats were divided into group I - young (3 months), Group II - aged (24 months), Group III - aged rats supplemented with WA (50 mg/kg b.w once in a day for 30 days) and Group IV - young rats supplemented with WA (50 mg/kg b. Read More

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December 2018

Effective Ibuprofen Desensitization in a Patient with Myopericarditis.

Pharmacology 2018 Dec 13;103(3-4):111-113. Epub 2018 Dec 13.

Internal Medicine, Allergy Unit, Rimini Hospital, Azienda Sanitaria Romagna, Rimini, Italy.

To date, aspirin desensitization is employed with patients with nonsteroidal anti-inflammatory drugs (NSAIDs) exacerbated respiratory diseases (NERD) or with aspirin or NSAIDs hypersensitive patients needing a stent procedure for coronary artery disease. On the other hand, few data exist regarding aspirin desensitization in other cardiological features and particularly we haven't data on different NSAIDs desensitization. Only for NERD patients we have data on ketorolac use. Read More

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December 2018

Expression of Matrix Metalloproteinase-2, Tissue Inhibitor of Matrix Metalloproteinase-2 and CD147 in the Traditional Chinese Medicine "Compound T11" for Treatment of Chronic Liver Injury.

Pharmacology 2018 Dec 13;103(3-4):128-135. Epub 2018 Dec 13.

First Clinical Medical School, Henan University of Chinese Medicine, Zhengzhou, China.

Objectives: To measure the expression of matrix metalloproteinase (MMP)-2, tissue inhibitor of matrix metalloproteinase inhibitor (TIMP)-2, and CD147 in mice with chronic liver injury induced by carbon tetrachloride after treatment with the traditional Chinese medicine (TCM) "Compound T11".

Method: Sixty male ICR mice were divided randomly into 6 groups of 10: control (C), model (M), low-dose treatment (LT; 50 mg/mL of Compound T11), medium-dose treatment (MT, 100 mg/mL), high-dose treatment (HT, 150 mg/mL), and positive drug treatment (YT, 67.5 mg/mL). Read More

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December 2018

Taxifolin Inhibits Receptor Activator of NF-κB Ligand-Induced Osteoclastogenesis of Human Bone Marrow-Derived Macrophages in vitro and Prevents Lipopolysaccharide-Induced Bone Loss in vivo.

Pharmacology 2018 Dec 6;103(1-2):101-109. Epub 2018 Dec 6.

It has been reported that taxifolin inhibit osteoclastogenesis in RAW264.7 cells. In our research, the inhibition effects of taxifolin on the osteoclastogenesis of human bone marrow-derived macrophages (BMMs) induced by receptor activator of NF-κB ligand (RANKL) as well as the protection effects in lipopolysaccharide-induced bone lysis mouse model have been demonstrated. Read More

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December 2018
4 Reads

Tauroursodeoxycholic Acid Ameliorates Lipopolysaccharide-Induced Depression Like Behavior in Mice via the Inhibition of Neuroinflammation and Oxido-Nitrosative Stress.

Pharmacology 2018 Dec 5;103(1-2):93-100. Epub 2018 Dec 5.

Department of Invasive Technology, Nantong First People's Hospital, The Second Affiliated Hospital of Nantong University, Nantong, China.

Depression is a mental disease that causes severe economic and social burdens. The mechanism for the onset of depression remains largely unknown. Recently, more and more attention is being given to the role of neuroinflammation and oxidative stress in depression. Read More

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December 2018
2 Reads

Mechanisms of Etomidate-Mediated Decrease of Spontaneous Spike Activity of Mouse Cerebellar Purkinje Cells in vivo.

Pharmacology 2018 Dec 5;103(1-2):82-92. Epub 2018 Dec 5.

Key Laboratory of Cellular Function and Pharmacology of Jilin Province, Yanbian University, Yanji,

Etomidate is an imidazole, nonbarbiturate hypnotic agent that is increasingly used in procedural sedation. However, the effects of etomidate on the spontaneous activity of cerebellar Purkinje cells (PCs) in living mouse have not been fully understood. In this study, we investigated the effects of etomidate on the spontaneous simple spike (SS) activity of PCs in urethane-anesthetized mice by cell-attached recording and pharmacological methods. Read More

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December 2018
2 Reads

Involvement of the cAMP-Dependent Pathway in Dextromethorphan-Induced Inhibition of Spontaneous Glutamate Transmission in the Nucleus Tractus Solitarius Neurons of Guinea Pigs.

Pharmacology 2018 Dec 5;103(1-2):76-81. Epub 2018 Dec 5.

Dextromethorphan (DEX) presynaptically decreases glutamatergic transmission in second-order neurons of the nucleus tractus solitarius (TS). To clarify the inhibitory mechanism of DEX, the present study examined the interaction of DEX with cAMP. The effects of DEX on miniature and TS-evoked excitatory postsynaptic currents (mEPSCs and eEPSCs) were recorded under activation of the cAMP-dependent pathway using the brainstem slices. Read More

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December 2018
1 Read

ErbB4 Receptors in the Medial Habenula Regulate Contextual Fear Memory.

Pharmacology 2018 Dec 4;103(1-2):68-75. Epub 2018 Dec 4.

Department of Pathophysiology, Zunyi Medical College, Zunyi, China.

The Medial Habenular (MHb) and the Lateral Habenular nuclei are 2 main parts of the habenular complex (Hb). Recent studies showed that MHb plays an important role in memory, and in the expression of ErbB4. However, the expression of MHb ErbB4 receptor and its role in fear memory is not well understood. Read More

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December 2018
4 Reads

Mechanisms of Hydrogen Sulfide against the Progression of Severe Alzheimer's Disease in Transgenic Mice at Different Ages.

Pharmacology 2018 Nov 16;103(1-2):50-60. Epub 2018 Nov 16.

Department of Biomedical, Metabolic and Neural Sciences, Section of Pharmacology and Molecular Medicine, University of Modena and Reggio Emilia, Modena,

Backgroud: Alzheimer disease is an age-related severe neurodegenerative pathology. The level of the third endogenous gas, hydrogen sulfide (H2S), is decreased in the brain of Alzheimer's disease (AD) patients compared with the brain of the age-matched normal individuals; also, plasma H2S levels are negatively correlated with the severity of AD. Recently, we have demonstrated that systemic H2S injections are neuroprotective in an early phase of preclinical AD. Read More

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November 2018
4 Reads

Propranolol Suppresses Cobalt Chloride-Induced Hypoxic Proliferation in Human Umbilical Vein Endothelial Cells in vitro.

Pharmacology 2018 Nov 16;103(1-2):61-67. Epub 2018 Nov 16.

Background/aims: To investigate the effect of propranolol on cobalt chloride (CoCl2)-induced hypoxic proliferation in human umbilical vein endothelial cells (HUVECs).

Methods: CoCl2 was administrated to HUVECs to mimic hypoxic proliferation in infantile hemangioma. The proliferation of HUVECs was detected by Cell Counting Kit-8. Read More

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November 2018
3 Reads
1.581 Impact Factor

Multiple-Dose Pharmacokinetics, Pharmacodynamics, and Safety of the Urotensin-II Receptor Antagonist Palosuran in Healthy Male Subjects.

Pharmacology 2018 1;102(5-6):339-346. Epub 2018 Nov 1.

Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland.

Purpose: To investigate the multiple-dose pharmacokinetics (PK), pharmacodynamics (PD), and tolerability of palosuran, a selective, potent antagonist of the human UT receptor.

Methods: This was a double-blind, randomized, placebo-controlled study. Three dose levels were investigated for PKs, PDs, and safety in sequential groups of 8 subjects each. Read More

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November 2018
5 Reads

Tetanic Facilitation of Neuromuscular Transmission by Adenosine A2A and Muscarinic M1 Receptors is Dependent on the Uptake of Choline via High-Affinity Transporters.

Pharmacology 2018 Oct 31;103(1-2):38-49. Epub 2018 Oct 31.

Department of Pharmacology and Therapeutic, State University of Maringá, Maringá, Brazil.

Background/aims: In this study, we evaluated the functional impact of facilitatory presynaptic adenosine A2A and muscarinic M1 receptors in the recovery of neuromuscular tetanic depression caused by the blockage of high-affinity choline transporter (HChT) by hemicholinium-3 (HC-3), a condition that mimics a myasthenia-like condition.

Methods: Rat diaphragm preparations were indirectly stimulated via the phrenic nerve trunk with 50-Hz frequency trains, each consisting of 500-750 supramaximal intensity pulses. The tension at the beginning (A) and at the end (B) of the tetanus was recorded and the ratio (R) B/A calculated. Read More

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October 2018
3 Reads

Comparative Pharmacokinetic Study of Mangiferin in Normal and Alloxan-Induced Diabetic Rats after Oral and Intravenous Administration by UPLC-MS/MS.

Pharmacology 2018 Oct 25;103(1-2):30-37. Epub 2018 Oct 25.

Laboratory Animal Center, Chongqing Medical University, Chongqing, China.

Backgrounds: Diabetes mellitus (DM)-induced morphological and/or functional complications may alter the pharmacokinetic profiles of mangiferin. This study aims to compare pharmacokinetic profiles of mangiferin in normal and alloxan-induced diabetic rats after oral and intravenous administration.

Methods: Mangiferin was administered orally (10 mg/kg) and intravenously (2 mg/kg) to normal and alloxan-induced diabetic Sprague-Dawley (SD) rats (n = 8). Read More

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October 2018
5 Reads

Malondialdehyde Assay in the Evaluation of Aspirin Antiplatelet Effects.

Pharmacology 2018 Oct 24;103(1-2):23-29. Epub 2018 Oct 24.

Institute for Pharmacology and Clinical Pharmacology, Heinrich Heine University, Düsseldorf, Germany.

Aspirin is essential in secondary prevention of patients after myocardial infarction and with coronary artery disease. However, impaired pharmacodynamic response to aspirin is frequent (high on-treatment platelet reactivity [HTPR]). This leads to an enhanced prevalence of cardiovascular events and to an impaired clinical outcome. Read More

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October 2018
5 Reads

Prevention of Stent Thrombosis in Rats by a Direct Oral Factor Xa Inhibitor Edoxaban.

Pharmacology 2018 Oct 19;103(1-2):17-22. Epub 2018 Oct 19.

Rare Disease Laboratories, Daiichi Sankyo Co., Ltd., Tokyo, Japan.

Background/aims: Stent thrombosis is a serious complication after percutaneous coronary intervention and femoropopliteal endovascular intervention. The aim of this study was to determine the antithrombotic effects of a direct factor Xa inhibitor edoxaban alone or in combination with antiplatelet agents in a rat model of stent thrombosis.

Methods: Stainless steel stents (4 stents per rat) were placed in an extracorporeal arteriovenous shunt. Read More

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October 2018
8 Reads

In vitro and in vivo GABAA Receptor Interaction of the Propanidid Metabolite 4-(2-[Diethylamino]-2-Oxoethoxy)-3-Methoxy-Benzeneacetic Acid.

Pharmacology 2018 Oct 17;103(1-2):10-16. Epub 2018 Oct 17.

KL Maddy Equine Analytical Chemistry Laboratory, University of California Davis, Davis, California, USA.

Background: Propanidid is a γ-aminobutyric acid type A (GABAA) receptor agonist general anesthetic and its primary metabolite is 4-(2-[diethylamino]-2-oxoethoxy)-3-methoxy-benzeneacetic acid (DOMBA). Despite having a high water solubility at physiologic pH that might predict low-affinity GABAA receptor interactions, DOMBA is reported to have no effect on GABAA receptor currents, possibly because the DOMBA concentrations studied were simply insufficient to modulate GABAA receptors. Our objectives were to measure the propanidid and DOMBA concentration responses on -GABAA receptors and to measure the behavioral responses of DOMBA in mice at concentrations that affect GABAA receptor currents in vitro. Read More

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October 2018

Involvement of MicroRNA-133a in the Protective Effect of Hydrogen Sulfide against Ischemia/Reperfusion-Induced Endoplasmic Reticulum Stress and Cardiomyocyte Apoptosis.

Pharmacology 2018 Oct 16;103(1-2):1-9. Epub 2018 Oct 16.

Department of Cardiology, Bethune International Peace Hospital, Shijiazhuang, China.

Aim: Myocardial ischemia/reperfusion (I/R) injury is a severe trauma that cells undergo and is associated with cardiomyocyte apoptosis. Recently, miRNAs have been demonstrated to play an important role in cardiovascular biology and disease. However, whether the miR-133a and ER stress play a role in hydrogen sulfide (H2S) protection of cardiomyocytes against I/R-induced apoptosis remains unclear. Read More

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October 2018
3 Reads
1.580 Impact Factor

Antiallodynic Effects of Intrathecal Areca Nut for Spinal Nerve-Ligated and Chemotherapy-Induced Neuropathic Pain in Rats.

Pharmacology 2018 10;102(5-6):332-338. Epub 2018 Oct 10.

Department of Anesthesiology and Pain Medicine, Chonnam National University Medical School, Gwangju, Republic of

This study examined the effects of intrathecal areca nut on spinal nerve-ligated and chemotherapy-induced neuropathic pain (NP), and investigated the relevance of spinal 5-hydroxytryptamine (5-HT) and α2-adrenergic receptors to those effects. For drug administration, intrathecal catheters were inserted into the subarachnoid space of male Sprague-Dawley rats. NP was induced either by spinal nerve ligation (left spinal nerves L5 and L6) or by chemotherapeutic injection (intraperitoneal cisplatin, 2 mg/kg/day, once daily for 4 days). Read More

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October 2018
2 Reads

Structure-Activity Relationship of the GPR55 Antagonist, CID16020046.

Pharmacology 2018 8;102(5-6):324-331. Epub 2018 Oct 8.

Background/aims: CID16020046 blocks the effect of the lipid lysophosphatidylinositol (LPI) at its receptor, GPR55. CID16020046 and another antagonist, ML193, have been used to investigate GPR55-mediated effects of LPI on cells, tissues, and in vivo. Here we describe the structure-activity relationship of CID16020046. Read More

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October 2018
2 Reads

The Anticancer Effect of Huaier Extract in Renal Cancer 786-O Cells.

Pharmacology 2018 8;102(5-6):316-323. Epub 2018 Oct 8.

Department of Urology, Qilu Hospital of Shandong University, Jinan,

Background: Trametes robiniophila Murr (Huaier) has been used as an adjuvant therapy of tumor in traditional Chinese medicine for many years, but the underlying mechanisms are largely unknown. In the present study, we tested the inhibitory effect of Huaier extract on renal cancer 786-O cells and explored the possible mechanisms.

Methods: 786-O cells were treated by gradient concentrations of Huaier extract, cell viability, invasion, migration and apoptosis were assessed by cell counting kit 8, cell scratch, transwell, and flow cytometry assay in vitro. Read More

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October 2018
9 Reads

Ropivacaine Protects against Memory Impairment and Hippocampal Damage in a Rat Neurodegeneration Model.

Pharmacology 2018 26;102(5-6):307-315. Epub 2018 Sep 26.

Graduate Institute of Basic Medicine, New Taipei City,

Background: Ropivacaine, a long-acting amide local anesthetic agent, has been demonstrated to inhibit glutamatergic transmission. Glutamate neurotoxicity plays a pivotal role in the pathogenesis of brain disorders. The purpose of this study is to investigate the neuroprotective effect of ropivacaine against brain damage induced by kainic acid (KA), an analogue of glutamate. Read More

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September 2018

Nitrosonifedipine, a Photodegradation Product of Nifedipine, Suppresses Pharmacologically Induced Aortic Aneurysm Formation.

Pharmacology 2018 25;102(5-6):287-299. Epub 2018 Sep 25.

Department of Pharmacy, Tokushima University Hospital, Tokushima,

Background/aims: We have reported that nitrosonifedipine (NO-NIF), a photodegradation product of nifedipine, has strong antioxidant and endothelial protective effects, and can suppress several cardiovascular diseases in animal models. The objective of the present study was to investigate the effects of NO-NIF on aortic aneurysm formation.

Methods: The mice were infused with β-aminopropionitrile for 2 weeks and angiotensin II for 6 weeks to induce aortic aneurysm formation. Read More

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September 2018

Chronic Stress May Not Be a Factor in the Behavioral Response to Chronic Lithium in ICR Mice.

Pharmacology 2018 25;102(5-6):281-286. Epub 2018 Sep 25.

School of Behavioral Sciences, Tel Aviv-Yaffo Academic College, Tel-Aviv,

Background: Lithium (Li) is the prototypic mood-stabilizing drug, but the individual response to Li is highly heterogeneous. Some evidence suggest interactions between Li and stress, and it is possible to hypothesize that lithium's effects are modified by stress conditions. The current study examines the interaction between 2 chronic stressors, constant light (CL) and restrain and the behavioral responses to chronic Li in female and male mice. Read More

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September 2018
1 Read

Attenuation of Remifentanil-Induced Hyperalgesia by Betulinic Acid Associates with Inhibiting Oxidative Stress and Inflammation in Spinal Dorsal Horn.

Pharmacology 2018 25;102(5-6):300-306. Epub 2018 Sep 25.

Department of Anesthesiology and Pain Clinic, The First Affiliated Hospital of Jiaxing University, Jiaxing,

Remifentanil-induced hyperalgesia (RIH) is known to be associated with oxidative stress and inflammation. Betulinic acid (BA) was reported to reduce visceral pain owing to its anti-oxidative and anti-inflammatory potential. Here, we -explored whether BA can attenuate RIH through inhibiting oxidative stress and inflammation in spinal dorsal horn. Read More

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September 2018
4 Reads

MPT0B169 and MPT0B002, New Tubulin Inhibitors, Induce Growth Inhibition, G2/M Cell Cycle Arrest, and Apoptosis in Human Colorectal Cancer Cells.

Pharmacology 2018 18;102(5-6):262-271. Epub 2018 Sep 18.

Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, Taipei,

We previously synthesized new tubulin inhibitors, MPT0B169 and MPT0B002, which induced growth inhibition and apoptosis in leukemia cells. However, their effects on solid tumor cells have not been determined. In this study, we investigated the effects of MPT0B169 and MPT0B002 on glioblastoma, breast, lung, and colorectal cancer (CRC) cell lines. Read More

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September 2018

Melatonin Induces Osteoblastic Differentiation of Mesenchymal Stem Cells and Promotes Fracture Healing in a Rat Model of Femoral Fracture via Neuropeptide Y/Neuropeptide Y Receptor Y1 Signaling.

Pharmacology 2018 18;102(5-6):272-280. Epub 2018 Sep 18.

Graduate Training Base of Jinzhou Medical University, 463rd Hospital of PLA, Shenyang,

The function of melatonin (MLT) in promoting fracture healing has been demonstrated in previous studies. However, the molecular mechanism underlying therapeutic effects of MLT is not entirely clear. In this study, mesenchymal stem cells (MSCs) were isolated from rat bone marrow and identified by flow cytometry. Read More

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September 2018
1 Read

Sodium Houttuyfonate Inhibits Voltage-Gated Peak Sodium Current and Anemonia Sulcata Toxin II-Increased Late Sodium Current in Rabbit Ventricular Myocytes.

Pharmacology 2018 23;102(5-6):253-261. Epub 2018 Aug 23.

Cardio-Electrophysiological Research Laboratory, Medical College, Wuhan University of Science and Technology, Wuhan,

Aim: Sodium houttuyfonate (SH), a chemical compound originating from Houttuynia cordata, has been reported to have anti-inflammatory, antibacterial, and antifungal effects, as well as cardioprotective effects. In this study, we investigated the effects of SH on cardiac electrophysiology, because to the best of our knowledge, this issue has not been previously investigated.

Methods: We used the whole-cell patch-clamp technique to explore the effects of SH on peak sodium current (INa. Read More

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August 2018
9 Reads

A Novel, Nonpeptidic, Orally Active Bivalent Inhibitor of Human β-Tryptase.

Pharmacology 2018 22;102(5-6):233-243. Epub 2018 Aug 22.

Department of Microbiology and Immunology, Joan and Sanford I. Weill Medical College of Cornell University, New York, New York, USA.

β-Tryptase is released from mast cells upon degranulation in response to allergic and inflammatory stimuli. Human tryptase is a homotetrameric serine protease with 4 identical active sites directed toward a central pore. These active sites present an optimized scenario for the rational design of bivalent inhibitors, which bridge 2 adjacent active sites. Read More

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August 2018
8 Reads

Biochemical Properties of TAK-828F, a Potent and Selective Retinoid-Related Orphan Receptor Gamma t Inverse Agonist.

Pharmacology 2018 22;102(5-6):244-252. Epub 2018 Aug 22.

Biomolecular Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd., Fujisawa, Japan.

Background/aims: Retinoid-related orphan receptor gamma t (RORγt) is a master regulator of T helper 17 cells that plays a pivotal role in the production of inflammatory cytokines including interleukin (IL)-17. Therefore, RORγt has attracted much attention as a target receptor for the treatment of inflammatory diseases including rheumatoid arthritis, multiple sclerosis, inflammatory bowel diseases, and psoriasis. This study aims to characterize TAK-828F, a potent and selective RORγt inverse agonist. Read More

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August 2018
7 Reads

Inhibition of Nicotine Dependence by Curcuminoid Is Associated with Reduced Acetylcholinesterase Activity in the Mouse Brain.

Pharmacology 2018 10;102(3-4):223-232. Epub 2018 Aug 10.

Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.

Nicotine is a stimulatory component in tobacco that activates the central nervous system reward pathway and causes nicotine dependence. We found that the anti-inflammatory agent, curcuminoid, prevents nicotine dependence and relapse, as assessed by the conditioned placed preference test. Curcuminoid (1, 3. Read More

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November 2018

A pan-NADPH Oxidase Inhibitor Ameliorates Kidney Injury in Type 1 Diabetic Rats.

Pharmacology 2018 10;102(3-4):180-189. Epub 2018 Aug 10.

Graduate School of Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul, Republic of Korea.

Background: NADPH oxidases (Nox) is a major enzyme system contributing to oxidative stress, which plays an important role in the pathogenesis of diabetic kidney disease (DKD). We have shown an elevation of renal Nox1, Nox2, and Nox4 in diabetic mice. APX-115, a pan-Nox inhibitor, attenuated the progression of DKD in mice. Read More

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November 2018
19 Reads

MicroRNA-124 Prevents H2O2-Induced Apoptosis and Oxidative Stress in Human Lens Epithelial Cells via Inhibition of the NF-κB Signaling Pathway.

Authors:
Xiu-Li Gu

Pharmacology 2018 10;102(3-4):213-222. Epub 2018 Aug 10.

Aim: To investigate the regulation of microRNA-124 -(miRNA-124) on NF-κB pathway from H2O2-induced apoptosis and oxidative stress in human lens epithelial cells (hLEC).

Methods: The MTT (3-[4, 5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay was used to detect hLEC -viability. HLECs were divided into Blank, H2O2, mimics (miRNA-124 mimics) + H2O2, NC+ H2O2, pyrrolidine dithiocarbamate (PDTC; NF-κB signaling pathway inhibitor) + H2O2, and inhibitors (miRNA-124 inhibitors) + PDTC + H2O2 groups. Read More

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November 2018

γ-Acetylcholine Receptor Mediating Dynamic Changes of Resistance to Rocuronium in the Denervated Skeletal Muscle.

Pharmacology 2018 10;102(3-4):190-195. Epub 2018 Aug 10.

Department of Anesthesiology, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.

Background/aims: Denervation resulted in resistance to non-depolarizing muscle relaxants (NDMRs), the magnitude of which changed after denervation in the skeletal muscle. The aim of this study was to investigate whether changed potencies of rocuronium were due to altered γ-acetylcholine receptor (γ-AChR) expression after skeletal muscle denervation.

Methods: Innervated and denervated muscle cells were used in this study. Read More

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November 2018
1 Read

11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor Development by Lentiviral Screening Based on Computational Modeling.

Pharmacology 2018 10;102(3-4):169-179. Epub 2018 Aug 10.

In this study, rat and human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have been cloned by lentiviral transduction and expressed by CHO-K1 cells. The results showed that recombinant plasmids contained R11bhsd1 or H11bhsd1 have been constructed, which is consistent with the gene bank respectively. A clone cell was selected with G418 and cultivated to express 11β-HSD1. Read More

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November 2018
12 Reads

Icariin Improves Sepsis-Induced Mortality and Acute Kidney Injury.

Pharmacology 2018 10;102(3-4):196-205. Epub 2018 Aug 10.

Department of Kidney Transplantation, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.

Objectives: Icariin (ICA) is a bioactive flavonoid with renal protective actions. This study investigated the effects of ICA on renal injury, inflammation, oxidative damage, apoptosis, and survival in a mouse model of cecal ligation and perforation (CLP)-induced sepsis.

Methods: Sepsis was induced by CLP. Read More

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November 2018
7 Reads
1.580 Impact Factor

Once-a-Day Trazodone in the Treatment of Depression in Routine Clinical Practice.

Pharmacology 2018 10;102(3-4):206-212. Epub 2018 Aug 10.

Department of Psychology, Faculty of Arts, Masaryk University, Brno, Czech Republic.

Objective: The aim of the study was to evaluate the efficacy, tolerability, and safety of once-a day trazodone tablets (Trittico Prolong® 300 mg) in patients with moderate to severe depression in routine clinical practice.

Methods: Men and women ≥18 years old with Montgomery-Åsberg Depression Rating Scale (MADRS) scores > 21 and Clinical Global Impression - Severity (CGI/S) ≥4 were included in this post-authorization, non-interventional, observational prospective safety study, conducted in 8 psychiatric centers in the Czech -Republic. The acute treatment phase lasted 5 weeks: 1 week of titration and 4 weeks of full-dose treatment. Read More

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November 2018
11 Reads

Unexpected Growth-Promoting Effect of Oxaliplatin in Excision Repair Cross-Complementation Group 1 Transfected Human Colon Cancer Cells.

Pharmacology 2018 26;102(3-4):161-168. Epub 2018 Jul 26.

Univ Lyon, Université Claude Bernard Lyon 1, INSERM 1052, CNRS 5286, Centre Léon Bérard, Centre de Recherche en Cancérologie de Lyon, Lyon, France.

The nucleotide excision repair protein excision repair cross-complementation group 1 (ERCC1) has been repeatedly shown to be involved in the sensitivity of cancer cells to platinum derivatives. In order to better understand this process, we transfected HCT-116 cells with a plasmid encoding ERCC1 and studied their in vitro and in vivo behaviour. No main differences were observed for sensitivity to platinum drugs, DNA repair capacity and clonogenicity in vitro. Read More

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November 2018
5 Reads

Pharmacokinetic Study on Protocatechuic Aldehyde and Hydroxysafflor Yellow A of Danhong Injection in Rats with Hyperlipidemia.

Pharmacology 2018 25;102(3-4):154-160. Epub 2018 Jul 25.

Background: Protocatechuic aldehyde (PAL) and hydroxysafflor yellow A (HSYA) are 2 effective ingredients of Danhong Injection, which is extensively used for the clinical treatment of cardio-cerebrovascular diseases. This study aims to investigate the pharmacokinetic differences between single and combined medication of PAL and HSYA and analyze the interaction of the above effective components in hyperlipidemia rats.

Methods: Thirty male SD rats were randomly divided into the control group (n = 6) and the model group (n = 24). Read More

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November 2018
3 Reads

Quercetin Shows the Pharmacological Activity to Simultaneously Downregulate the Inflammatory and Fibrotic Responses to Tissue Injury in Association with its Ability to Target Multi-Kinases.

Pharmacology 2018 17;102(3-4):142-153. Epub 2018 Jul 17.

Chemical Kinomics Center, Korea Institute of Science and Technology, Seoul, Republic of Korea.

Aim: Previous studies have suggested that quercetin is effective for treating diverse chronic disorders including organ fibrosis and airway and cardiovascular disorders. To access the pharmacological background for its broad efficacy, we examined the ability of quercetin to modulate the inflammatory and fibrotic responses associated with organ injury that commonly underlie the pathogenesis of those disorders.

Methods: A cutaneous wound model on rabbit ear was used for in vivo study. Read More

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November 2018
4 Reads

Cyanidin Protects SH-SY5Y Human Neuroblastoma Cells from 1-Methyl-4-Phenylpyridinium-Induced Neurotoxicity.

Pharmacology 2018 6;102(3-4):126-132. Epub 2018 Jul 6.

School of Pharmacy, Wenzhou Medical Medical University, Wenzhou, China.

Cyanidin is an anthocyanidin extracted from a variety of fruits and vegetables. Cyanidin showed benefits against diabetes, cancer, and atherosclerosis. However, the potential neuroprotective effects of cyanidin against Parkinson's disease (PD) have not been examined. Read More

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November 2018
6 Reads

Quantification of Hydrochlorothiazide and Ramipril/Ramiprilate in Blood Serum and Cerebrospinal Fluid: A Pharmacokinetic Assessment of Central Nervous System Adverse Effects.

Pharmacology 2018 6;102(3-4):133-137. Epub 2018 Jul 6.

Institute for Biomedical and Pharmaceutical Research, Nuremberg, Germany.

Background: A drug must reach the central nervous system (CNS) in order to directly cause CNS adverse effects (AEs). Our current study addressed the pharmacokinetic (PK) background of the assumption that CNS concentrations of hydrochlorothiazide (HCT) and ramiprilate may directly cause CNS AEs such as headache and drowsiness.

Methods: In neurological patients, paired serum and cerebrospinal fluid (CSF) samples were withdrawn simultaneously. Read More

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November 2018

Ranolazine Prevents Levosimendan-Induced Atrial Fibrillation.

Pharmacology 2018 6;102(3-4):138-141. Epub 2018 Jul 6.

Department of Cardiology II (Electrophysiology), University Hospital Münster, Münster, Germany.

Objectives: Levosimendan is a calcium sensitizer that is used as positive inotropic drug in acute decompensated heart failure. An increased incidence of atrial fibrillation after levosimendan-treatment was observed in clinical and experimental studies. Due to the limited range of antiarrhythmic drugs, the aim of the present study was to assess potential antiarrhythmic effects of ranolazine in levosimendan-pretreated isolated rabbit hearts. Read More

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November 2018
2 Reads

SLCO1B1 c.521T>C Genotyping in the Austrian Population Using 2 Commercial Real-Time Polymerase Chain Reaction Assays: An Implementation Study.

Pharmacology 2018 28;102(1-2):88-90. Epub 2018 Jun 28.

Institute of Clinical Chemistry and Laboratory Medicine, General Hospital Steyr, Steyr, Austria.

Statin-induced myopathy is reported to be significantly associated with the SCLO1B1 c.521T>C polymorphism. To date, SLCO1B1 c. Read More

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November 2018

Puerarin Attenuates Osteoarthritis via Upregulating AMP-Activated Protein Kinase/Proliferator-Activated Receptor-γ Coactivator-1 Signaling Pathway in Osteoarthritis Rats.

Pharmacology 2018 29;102(3-4):117-125. Epub 2018 Jun 29.

Department of Orthopaedic Surgery, Shanghai Jiao Tong University Affiliated Sixth People's Hospital, Shanghai, China.

Background/aims: Osteoarthritis is the most common degenerative joint disease and causes major pain and disability in adults. It has been reported that mitochondrial dysfunction in chondrocytes was associated with osteoarthritis. Puerarin has multiple effects including restoring mitochondrial function. Read More

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November 2018
9 Reads

Bardoxolone Methyl Suppresses Hepatitis B Virus Large Surface Protein Variant W4P-Related Carcinogenesis and Hepatocellular Carcinoma Cell Proliferation Via the Inhibition of Signal Transducer and Activator of Transcription 3 Signaling.

Pharmacology 2018 28;102(1-2):105-113. Epub 2018 Jun 28.

Department of Fundamental Pharmaceutical Science, Graduate School, Kyung Hee University, Seoul, Republic of Korea.

Bardoxolone methyl (CDDO-me) is a synthetic triterpenoid that has been shown to suppress various cancers and inflammation. It has been implicated for the suppression of signal transducer and activator of transcription 3 (STAT3)-mediated signaling, which plays crucial roles in the development and progression of hepatocellular carcinoma (HCC). Previously, we showed that hepatitis B virus (HBV) large surface protein (LHB) variant W4P promotes carcinogenesis and tumor progression through STAT3 activation. Read More

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November 2018
11 Reads

Effects of Folpet, Captan, and Captafol on Human Aromatase in JEG-3 Cells.

Pharmacology 2018 28;102(1-2):81-87. Epub 2018 Jun 28.

Center of Scientific Research, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.

Background: Estradiol, produced by aromatase (CYP19A1), is very important for reproduction. Folpet, captan, and captafol belong to the phthalimide class of fungicides. They are used to protect the leaves of plants or fruits. Read More

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November 2018
7 Reads
1.580 Impact Factor

17-(Allylamino)-17-Demethoxygeldanamycin Enhances Etoposide-Induced Cytotoxicity via the Downregulation of Xeroderma Pigmentosum Complementation Group C Expression in Human Lung Squamous Cell Carcinoma Cells.

Pharmacology 2018 28;102(1-2):91-104. Epub 2018 Jun 28.

Department of Biochemical Science and Technology, National Chiayi University, Chiayi, Taiwan.

Etoposide (VP16) is a topoisomerase II inhibitor and has been used for the treatment of non-small cell lung cancer (NSCLC). Xeroderma pigmentosum complementation group C (XPC) protein is a DNA damage recognition factor in nucleotide excision repair and involved in regulating NSCLC cell proliferation and viability. Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone that is responsible for the stabilization and maturation of many oncogenic proteins. Read More

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November 2018
8 Reads

Effective Desensitization to Tocilizumab in Delayed Hypersensitivity Reaction.

Pharmacology 2018 28;102(1-2):114-116. Epub 2018 Jun 28.

Internal Medicine, Allergy Unit, Rimini Hospital, Azienda sanitaria Romagna, Rimini, Italy.

We present tocilizumab desensitization of a 47-year-old woman affected by rheumatoid arthritis with full body delayed erythematous urticarial reaction. Skin test for tocilizumab gave cutaneous reaction after 6 h at 20 mg/mL. The schedule of desensitization was then adapted for non-immediate reaction. Read More

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November 2018
1 Read

Melatonin Loading Chitosan-Tripolyphosphate Nanoparticles: Application in Attenuating Etoposide-Induced Genotoxicity in HepG2 Cells.

Pharmacology 2018 25;102(1-2):74-80. Epub 2018 Jun 25.

Etoposide is one of the most effective chemotherapeutic agents used in the treatment of various types of cancers. However, as a Topoisomerase II inhibitor, during clinical use, several side effects may occur. In addition, in several in vivo and in vitro studies, etoposide has been shown to have a range of genotoxic effects including single and double strand breaks. Read More

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November 2018
1 Read
1 Citation
1.581 Impact Factor