- Cellular Pharmacokinetic/Pharmacodynamic Relationship of Platinum Cytostatics in Head and Neck Squamous Cell Carcinoma Evaluated by Liquid Chromatography Coupled to Tandem Mass Spectrometry
[作者:Theile, D; Detering, JC; Herold-Mende, C; Dyckhoff, G; Haefeli, WE; Weiss, J; Burhenne, J,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:51-58 , 文章类型: Article,,卷期:2012年341-1]
- Cisplatin (diaminodichloroplatinum) is the favored platinum (Pt) drug for the treatment of head and neck squamous cell carcinoma (HNSCC). However, Pt drug alternatives such as carboplatin (diaminoplatinum-cyclobutan-1,1-...
- Anti-Inflammatory Mechanism of Compound K in Activated Microglia and Its Neuroprotective Effect on Experimental Stroke in Mice
[作者:Park, JS; Shin, JA; Jung, JS; Hyun, JW; Le, TKV; Kim, DH; Park, EM; Kim, HS,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:59-67 , 文章类型: Article,,卷期:2012年341-1]
- Microglial activation plays a pivotal role in the pathogenesis of various neurologic disorders, such as cerebral ischemia, Alzheimer's disease, and Parkinson's disease. Thus, controlling microglial activation is a promis...
- Selective Glucocorticoid Receptor Agonists for the Treatment of Inflammatory Bowel Disease: Studies in Mice with Acute Trinitrobenzene Sulfonic Acid Colitis
[作者:Reuter, KC; Grunwitz, CR; Kaminski, BM; Steinhilber, D; Radeke, HH; Stein, J,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:68-80 , 文章类型: Article,,卷期:2012年341-1]
- Despite being a mainstay of inflammatory bowel disease (IBD) therapy, glucocorticoids (GCs) still carry significant risks with respect to unwanted side effects. Alternative drugs with a more favorable risk/benefit ratio ...
- A Novel Small Molecule, (E)-5-(2,4-di-tert-butyl-6-((2,4-dioxothiazolidin-5-ylidene)methyl)phenyl)-5 '-methyl-7,7 '-dimethoxy-4,4 '-bibenzo[d][1,3]dioxole-5,5 '-dicarboxylate (7k), Alleviates the Development of D-Galactosamine/Lipopolysaccharide-Induced Acute Liver Failure by Inhibiting Macrophage Infiltration and Regulating Cytokine Expression
[作者:Deng, CY; Liu, J; Wang, GC; Ma, L; Xie, CF; Wang, XW; Li, XX; Chen, LJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:146-155 , 文章类型: Article,,卷期:2012年341-1]
- Acute liver failure (ALF) is a relatively rare liver disorder that leads to the massive death of hepatocytes. Our previous study reported that a novel small-molecule agent, (E)-5-(2,4-di-tert-butyl-6-((2,4-dioxothiazolid...
- Microinjection of Glycine into the Ventral Tegmental Area Selectively Decreases Ethanol Consumption
[作者:Li, J; Nie, H; Bian, WL; Dave, V; Janak, PH; Ye, JH,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:196-204 , 文章类型: Article,,卷期:2012年341-1]
- The mechanisms of ethanol addiction are not completely understood. The mesolimbic dopaminergic system is involved in many drug-related behaviors, including ethanol self-administration. The dopaminergic neurons in this sy...
- Role of Transient Receptor Potential Ankyrin 1 in Gastric Accommodation in Conscious Guinea Pigs
[作者:Koseki, J; Oshima, T; Kondo, T; Tomita, T; Fukui, H; Watari, J; Hattori, T; Kase, Y; Miwa, H,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:205-212 , 文章类型: Article,,卷期:2012年341-1]
- We report the establishment of a new model for measuring gastric tone and liquid meal-induced accommodation in conscious guinea pigs and the role played by transient receptor potential ankyrin 1 (TRPA1). An indwelling po...
- Relationship between Dose, Drug Levels, and D2 Receptor Occupancy for the Atypical Antipsychotics Risperidone and Paliperidone
[作者:Muly, EC; Votaw, JR; Ritchie, J; Howell, LL,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:81-89 , 文章类型: Article,,卷期:2012年341-1]
- Blockade of D2 family dopamine receptors (D2Rs) is a fundamental property of antipsychotics, and the degree of striatal D2R occupancy has been related to antipsychotic and motor effects of these drugs. Recent studies sug...
- A Humanized Glycoprotein VI (GPVI) Mouse Model to Assess the Antithrombotic Efficacies of Anti-GPVI Agents
[作者:Mangin, PH; Tang, CJ; Bourdon, C; Loyau, S; Freund, M; Hechler, B; Gachet, C; Jandrot-Perrus, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:156-163 , 文章类型: Article,,卷期:2012年341-1]
- Glycoprotein VI (GPVI) has been proposed as a promising antiplatelet target, because its blockade prevents experimental thrombosis without impairing hemostasis. The objective of this study was to develop a preclinical to...
- An Oxycodone Conjugate Vaccine Elicits Drug-Specific Antibodies that Reduce Oxycodone Distribution to Brain and Hot-Plate Analgesia
[作者:Pravetoni, M; Le Naour, M; Harmon, TM; Tucker, AM; Portoghese, PS; Pentel, PR,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:225-232 , 文章类型: Article,,卷期:2012年341-1]
- Opioid conjugate vaccines have shown promise in attenuating the behavioral effects of heroin or morphine in animals. The goal of this study was to extend this approach to oxycodone (OXY), a commonly abused prescription o...
- Effects of Celecoxib on Prostanoid Biosynthesis and Circulating Angiogenesis Proteins in Familial Adenomatous Polyposis
[作者:Dovizio, M; Tacconelli, S; Ricciotti, E; Bruno, A; Maier, TJ; Anzellotti, P; Di Francesco, L; Sala, P; Signoroni, S; Bertario, L; Dixon, DA; Lawson, JA; Steinhilber, D; FitzGerald, GA; Patrignani, P,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:242-250 , 文章类型: Article,,卷期:2012年341-1]
- Vascular cyclooxygenase (COX)-2-dependent prostacyclin (PGI(2)) may affect angiogenesis by preventing endothelial activation and platelet release of angiogenic factors present in platelet alpha-granules. Thus, a profound...
- Studies of the Biogenic Amine Transporters. 14. Identification of Low-Efficacy "Partial" Substrates for the Biogenic Amine Transporters
[作者:Rothman, RB; Partilla, JS; Baumann, MH; Lightfoot-Siordia, C; Blough, BE,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:251-262 , 文章类型: Article,,卷期:2012年341-1]
- Several compounds have been identified that display low-efficacy, "partial substrate" activity. Here, we tested the hypothesis that the mechanism of this effect is a slower rate of induced neurotransmitter efflux than th...
- Xanomeline Modulation of the Blood Oxygenation Level-Dependent Signal in Awake Rats: Development of Pharmacological Magnetic Resonance Imaging as a Translatable Pharmacodynamic Biomarker for Central Activity and Dose Selection
[作者:Baker, S; Chin, CL; Basso, AM; Fox, GB; Marek, GJ; Day, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:263-273 , 文章类型: Article,,卷期:2012年341-1]
- In vivo translational imaging techniques, such as positron emission tomography and single-photon emission-computed tomography, are the only ways to adequately determine that a drug engages its target. Unfortunately, ther...
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