- JNJ-20788560 [9-(8-Azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic Acid Diethylamide], a Selective Delta Opioid Receptor Agonist, Is a Potent and Efficacious Antihyperalgesic Agent That Does Not Produce Respiratory Depression, Pharmacologic Tolerance, or Physical Dependence
[作者:Codd, EE; Carson, JR; Colburn, RW; Stone, DJ; Van Besien, CR; Zhang, SP; Wade, PR; Gallantine, EL; Meert, TF; Molino, L; Pullan, S; Razler, CM; Dax, SL; Flores, CM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:241-251 , 文章类型: Article,,卷期:2009年329-1]
mu-Opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple origins, but their side effects, such as constipation, respiratory depression, and abuse liability, adversely affect patients....
- Transport of Lamivudine [(-)-beta-L-2 ',3 '-Dideoxy-3 '-thiacytidine] and High-Affinity Interaction of Nucleoside Reverse Transcriptase Inhibitors with Human Organic Cation Transporters 1, 2, and 3
[作者:Minuesa, G; Volk, C; Molina-Arcas, M; Gorboulev, V; Erkizia, I; Arndt, P; Clotet, B; Pastor-Anglada, M; Koepsell, H; Martinez-Picado, J,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:252-261 , 文章类型: Article,,卷期:2009年329-1]
Nucleoside reverse transcriptase inhibitors (NRTIs) need to enter cells to act against the HIV-1. Human organic cation transporters (hOCT1-3) are expressed and active in CD4+ T cells, the main target of HIV-1, and hav...
- Functional Genetic Variation in the Basal Promoter of the Organic Cation/Carnitine Transporters OCTN1 (SLC22A4) and OCTN2 (SLC22A5)
[作者:Tahara, H; Yee, SW; Urban, TJ; Hesselson, S; Castro, RA; Kawamoto, M; Stryke, D; Johns, SJ; Ferrin, TE; Kwok, PY; Giacomini, KM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:262-271 , 文章类型: Article,,卷期:2009年329-1]
The organic cation/ergothioneine transporter OCTN1 (SLC22A4) and the high-affinity carnitine transporter OCTN2 (SLC22A5), play an important role in the disposition of xenobiotics and endogenous compounds. Here, we ana...
- Characterization of the A(2B) Adenosine Receptor from Mouse, Rabbit, and Dog
[作者:Auchampach, JA; Kreckler, LM; Wan, TC; Maas, JE; van der Hoeven, D; Gizewski, E; Narayanan, J; Maas, GE,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:2-13 , 文章类型: Article,,卷期:2009年329-1]
We have cloned and pharmacologically characterized the A(2B) adenosine receptor (AR) from the dog, rabbit, and mouse. The full coding regions of the dog and mouse A(2B)AR were obtained by reverse transcriptase-polymer...
- Rewarding Morphine-Induced Synaptic Function of delta-Opioid Receptors on Central Glutamate Synapses
[作者:Bie, BH; Zhu, W; Pan, ZZZ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:290-296 , 文章类型: Article,,卷期:2009年329-1]
The rewarding effect of opioids, the driving force for compulsive behaviors of opioid abuse and addiction, is primarily mediated by the mu-opioid receptor. However, the role of the delta-opioid receptor (DOR) in opioi...
- Rapid Identification of the Hepatic Cytochrome P450 2C19 Activity Using a Novel and Noninvasive [C-13]Pantoprazole Breath Test
[作者:Desta, Z; Modak, A; Nguyen, PD; Lemler, SM; Kurogi, Y; Li, L; Flockhart, DA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:297-305 , 文章类型: Article,,卷期:2009年329-1]
We tested the hypothesis that the stable isotope [C-13]pantoprazole is O-demethylated by cytochrome P450 CYP2C19 and that the (CO2)-C-13 produced and exhaled in breath as a result can serve as a safe, rapid, and nonin...
- The Microtubule-Targeting Agents, PBOX-6 [Pyrrolobenzoxazepine 7-[(dimethylcarbamoyl) oxy]-6-(2-naphthyl) pyrrolo-[2,1-d] (1,5)-benzoxazepine] and Paclitaxel, Induce Nucleocytoplasmic Redistribution of the Peptidyl-Prolyl Isomerases, Cyclophilin A and Pin1, in Malignant Hematopoietic Cells
[作者:Bane, FT; Bannon, JH; Pennington, SR; Campaini, G; Williams, DC; Zisterer, DM; Mc Gee, MM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:38-47 , 文章类型: Article,,卷期:2009年329-1]
Microtubule assembly and disassembly is required for the maintenance of cell structure, mobility, and division. However, the cellular and biochemical implications of microtubule disruption are not fully understood. Us...
- Synergy between Enzyme Inhibitors of Fatty Acid Amide Hydrolase and Cyclooxygenase in Visceral Nociception
[作者:Naidu, PS; Booker, L; Cravatt, BF; Lichtman, AH,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:48-56 , 文章类型: Article,,卷期:2009年329-1]
The present study investigated whether inhibition of fatty acid amide hydrolase (FAAH), the enzyme responsible for anandamide catabolism, produces antinociception in the acetic acidinduced abdominal stretching model o...
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