- Selexipag: A Selective Prostacyclin Receptor Agonist that Does Not Affect Rat Gastric Function
[作者:Morrison, K; Ernst, R; Hess, P; Studer, R; Clozel, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:249-255 , 文章类型: Article,,卷期:2010年335-1]
- Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}- N-(methylsulfonyl) acetamide] is an orally available prostacyclin (PGI(2)) receptor (IP receptor) agonist that is chemically distinct from PGI(2) and i...
- Agonist-Specific Compartmentation of cGMP Action in Myometrium
[作者:Buxton, ILO; Milton, D; Barnett, SD; Tichenor, SD,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:256-263 , 文章类型: Article,,卷期:2010年335-1]
- Nitric oxide relaxes myometrium in a cGMP-independent manner. Although cGMP activates its cognate kinase, this is not required for the inhibitory effect of nitric oxide. Thus, nitric oxide-mediated cGMP elevation does no...
- Transcriptional Regulation of Renal Cytoprotective Genes by Nrf2 and Its Potential Use as a Therapeutic Target to Mitigate Cisplatin-Induced Nephrotoxicity
[作者:Aleksunes, LM; Goedken, MJ; Rockwell, CE; Thomale, J; Manautou, JE; Klaassen, CD,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:2-12 , 文章类型: Article,,卷期:2010年335-1]
- The use of the chemotherapeutic drug cisplatin is limited in part by nephrotoxicity. Cisplatin causes renal DNA adducts and oxidative stress in rodents. The transcription factor Nrf2 (nuclear factor E2-related factor 2) ...
- Diminished Activity-Dependent Brain-Derived Neurotrophic Factor Expression Underlies Cortical Neuron Microcircuit Hypoconnectivity Resulting from Exposure to Mutant Huntingtin Fragments
[作者:Gambazzi, L; Gokce, O; Seredenina, T; Katsyuba, E; Runne, H; Markram, H; Giugliano, M; Luthi-Carter, R,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:13-22 , 文章类型: Article,,卷期:2010年335-1]
- Although previous studies of Huntington's disease (HD) have addressed many potential mechanisms of striatal neuron dysfunction and death, it is also known, based on clinical findings, that cortical function is dramatical...
- E6201, a Novel Kinase Inhibitor of Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase Kinase-1 and Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase Kinase Kinase-1: In Vivo Effects on Cutaneous Inflammatory Responses by Topical Administration
[作者:Muramoto, K; Goto, M; Inoue, Y; Ishii, N; Chiba, K; Kuboi, Y; Omae, T; Wang, YJ; Gusovsky, F; Shirota, H,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:23-31 , 文章类型: Article,,卷期:2010年335-1]
- E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8,9,16-trihydroxy-3,4-dimethyl-3,4,9,10-tetrahydro-1H-2-benzoxacyclotetradecine1,7(8H)-dione)] is a novel anti-inflammatory agent that has potent inhibitory effects on the prod...
- Therapeutic Role of Rifaximin in Inflammatory Bowel Disease: Clinical Implication of Human Pregnane X Receptor Activation
[作者:Cheng, J; Shah, YM; Ma, XC; Pang, XY; Tanaka, T; Kodama, T; Krausz, KW; Gonzalez, FJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:32-41 , 文章类型: Article,,卷期:2010年335-1]
- Human pregnane X receptor (PXR) has been implicated in the pathogenesis of inflammatory bowel disease (IBD). Rifaximin, a human PXR activator, is in clinical trials for treatment of IBD and has demonstrated efficacy in C...
- Genetic Polymorphisms in Organic Cation Transporter 1 (OCT1) in Chinese and Japanese Populations Exhibit Altered Function
[作者:Chen, LG; Takizawa, M; Chen, E; Schlessinger, A; Segenthelar, J; Choi, JH; Sali, A; Kubo, M; Nakamura, S; Iwamoto, Y; Iwasaki, N; Giacomini, KM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:42-50 , 文章类型: Article,,卷期:2010年335-1]
- Organic cation transporter 1 (OCT1; SLC22A1) seems to play a role in the efficacy and disposition of the widely used antidiabetic drug metformin. Genetic variants in OCT1 have been identified largely in European populati...
- Characterization of CCX282-B, an Orally Bioavailable Antagonist of the CCR9 Chemokine Receptor, for Treatment of Inflammatory Bowel Disease
[作者:Walters, MJ; Wang, Y; Lai, N; Baumgart, T; Zhao, BN; Dairaghi, DJ; Bekker, P; Ertl, LS; Penfold, MET; Jaen, JC; Keshav, S; Wendt, E; Pennell, A; Ungashe, S; Wei, Z; Wright, JJK; Schall, TJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:61-69 , 文章类型: Article,,卷期:2010年335-1]
- The chemokine system represents a diverse group of G protein-coupled receptors responsible for orchestrating cell recruitment under both homeostatic and inflammatory conditions. Chemokine receptor 9 (CCR9) is a chemokine...
- Ezetimibe Ameliorates Cardiovascular Complications and Hepatic Steatosis in Obese and Type 2 Diabetic db/db Mice
[作者:Fukuda, M; Nakamura, T; Kataoka, K; Nako, H; Tokutomi, Y; Dong, YF; Yasuda, O; Ogawa, H; Kim-Mitsuyama, S,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:70-75 , 文章类型: Article,,卷期:2010年335-1]
- Type 2 diabetes plays a major role in the development of cardiovascular diseases. The present study was undertaken to investigate the effect of ezetimibe, a potent cholesterol absorption inhibitor, on cardiovascular inju...
- Interaction between Sensory C-fibers and Cardiac Mast Cells in Ischemia/Reperfusion: Activation of a Local Renin-Angiotensin System Culminating in Severe Arrhythmic Dysfunction
[作者:Morrey, C; Brazin, J; Seyedi, N; Corti, F; Silver, RB; Levi, R,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:76-84 , 文章类型: Article,,卷期:2010年335-1]
- Renin, the rate-limiting enzyme in the activation of the renin-angiotensin system (RAS), is synthesized and stored in cardiac mast cells. In ischemia/reperfusion, cardiac sensory nerves release neuropeptides such as subs...
- Heme Oxygenase-1 Deficiency Leads to Alteration of Soluble Guanylate Cyclase Redox Regulation
[作者:Jones, AW; Durante, W; Korthuis, RJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:85-91 , 文章类型: Article,,卷期:2010年335-1]
- Heme oxygenase-1 knockout, H(mox)1(-/-), mice exhibit exacerbated vascular lesions after ischemia-reperfusion and mechanical injury. Surprisingly, we found no studies that reported contractile responses and sensitivity t...
- Pharmacological Effects of Cannabinoids on the Caco-2 Cell Culture Model of Intestinal Permeability
[作者:Alhamoruni, A; Lee, AC; Wright, KL; Larvin, M; O'Sullivan, SE,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:92-102 , 文章类型: Article,,卷期:2010年335-1]
- Activation of cannabinoid receptors decreases emesis, inflammation, gastric acid secretion, and intestinal motility. However, the effects of cannabinoids on intestinal permeability have not yet been established. The aim ...
- A Selective Cannabinoid-1 Receptor Antagonist, PF-95453, Reduces Body Weight and Body Fat to a Greater Extent than Pair-Fed Controls in Obese Monkeys
[作者:Wagner, JD; Zhang, L; Kavanagh, K; Ward, GM; Chin, JE; Hadcock, JR; Auerbach, BJ; Harwood, HJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:103-113 , 文章类型: Article,,卷期:2010年335-1]
- Cannabinoid-1 (CB1) receptor antagonists exhibit pharmacological properties favorable to treatment of obesity, caused by both centrally mediated effects on appetite and peripherally mediated effects on energy metabolism....
- Curcumin Stimulates Reactive Oxygen Species Production and Potentiates Apoptosis Induction by the Antitumor Drugs Arsenic Trioxide and Lonidamine in Human Myeloid Leukemia Cell Lines
[作者:Sanchez, Y; Simon, GP; Calvino, E; de Blas, E; Aller, P,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:114-123 , 文章类型: Article,,卷期:2010年335-1]
- Arsenic trioxide (ATO, Trisenox) is an important antileukemic drug, but its efficacy is frequently low when used as a single agent. Here, we demonstrate that the apoptotic action of ATO is greatly increased when combined...
- Dopamine Uptake Inhibitors but Not Dopamine Releasers Induce Greater Increases in Motor Behavior and Extracellular Dopamine in Adolescent Rats Than in Adult Male Rats
[作者:Walker, QD; Morris, SE; Arrant, AE; Nagel, JM; Parylak, S; Zhou, GY; Caster, JM; Kuhn, CM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:124-132 , 文章类型: Article,,卷期:2010年335-1]
- Most life-long drug addiction begins during adolescence. Important structural and functional changes in brain occur during adolescence and developmental differences in forebrain dopamine systems could mediate a biologic ...
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