- Pharmacological Chaperones Restore Function to MC4R Mutants Responsible for Severe Early-Onset Obesity
[作者:Rene, P; Le Gouill, C; Pogozheva, ID; Lee, G; Mosberg, HI; Farooqi, IS; Valenzano, KJ; Bouvier, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:520-532 , 文章类型: Article,,卷期:2010年335-3]
- Heterozygous null mutations in the melanocortin-4 receptor (MC4R) cause early-onset obesity in humans, indicating that metabolic homeostasis is sensitive to quantitative variation in MC4R function. Most of the obesity-ca...
- Magnetic Resonance Imaging Detection and Time Course of Cerebral Microhemorrhages during Passive Immunotherapy in Living Amyloid Precursor Protein Transgenic Mice
[作者:Luo, F; Rustay, NR; Seifert, T; Roesner, B; Hradil, V; Hillen, H; Ebert, U; Severin, JM; Cox, BF; Llano, DA; Day, M; Fox, GB,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:580-588 , 文章类型: Article,,卷期:2010年335-3]
- In recent years immunotherapy-based approaches for treating Alzheimer's disease have become the subject of intensive research. However, an important mechanistic-related safety concern is exacerbation of the risk of micro...
- Prevention of Bleomycin-Induced Pulmonary Fibrosis by a Novel Antifibrotic Peptide with Relaxin-Like Activity
[作者:Pini, A; Shemesh, R; Samuel, CS; Bathgate, RAD; Zauberman, A; Hermesh, C; Wool, A; Bani, D; Rotman, G,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:589-599 , 文章类型: Article,,卷期:2010年335-3]
- Pulmonary fibrosis is a progressive and lethal lung disease characterized by accumulation of extracellular matrix and loss of pulmonary function. No cure exists for this pathologic condition, and current treatments often...
- Endogenous Luminal Surface Adenosine Signaling Regulates Duodenal Bicarbonate Secretion in Rats
[作者:Ham, M; Mizumori, M; Watanabe, C; Wang, JH; Inoue, T; Nakano, T; Guth, PH; Engel, E; Kaunitz, JD; Akiba, Y,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:607-613 , 文章类型: Article,,卷期:2010年335-3]
- Luminal ATP increases duodenal bicarbonate secretion (DBS) via brush border P2Y receptors. Because ATP is sequentially dephosphorylated to adenosine (ADO) and the brush border highly expresses adenosine deaminase (ADA), ...
- A Transmembrane Amino Acid in the GABA(A) Receptor beta(2) Subunit Critical for the Actions of Alcohols and Anesthetics
[作者:McCracken, ML; Borghese, CM; Trudell, JR; Harris, RA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:600-606 , 文章类型: Article,,卷期:2010年335-3]
- Alcohols and inhaled anesthetics enhance the function of GABA(A) receptors containing alpha, beta, and gamma subunits. Molecular analysis has focused on the role of the alpha subunits; however, there is evidence that the...
- Bronchodilator Activity of (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino] carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407), a Potent, Long-Acting, and Selective Muscarinic M3 Receptor Antagonist
[作者:Villetti, G; Pastore, F; Bergamaschi, M; Bassani, F; Bolzoni, PT; Battipaglia, L; Amari, G; Rizzi, A; Delcanale, M; Volta, R; Cenacchi, V; Cacciani, F; Zaniboni, M; Berti, F; Rossoni, G; Harrison, S; Petrillo, P; Santoro, E; Scudellaro, R; Mannini, F; Geppetti, PA; Razzetti, R; Patacchini, R; Civelli, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:622-635 , 文章类型: Article,,卷期:2010年335-3]
- The novel quaternary ammonium salt (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl) methyl] amino] carbonyl]oxy]-1-[2-oxo-2-(2-thienyl) ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407) showed subnanomolar affiniti...
- A Novel Family of Negative and Positive Allosteric Modulators of NMDA Receptors
[作者:Costa, BM; Irvine, MW; Fang, GY; Eaves, RJ; Mayo-Martin, MB; Skifter, DA; Jane, DE; Monaghan, DT,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:614-621 , 文章类型: Article,,卷期:2010年335-3]
- The N-methyl-D-aspartate (NMDA) receptor family regulates various central nervous system functions, such as synaptic plasticity. However, hypo-or hyperactivation of NMDA receptors is critically involved in many neurologi...
- Calpain Inhibitor Protects Cells against Light-Induced Retinal Degeneration
[作者:Imai, S; Shimazawa, M; Nakanishi, T; Tsuruma, K; Hara, H,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:645-652 , 文章类型: Article,,卷期:2010年335-3]
- Calpains are activated by excessive light exposure and related to retinal degeneration. We investigated the protective effects of ((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2,3-di-oxopropyl)amino)carbonyl)-3-methylbutyl...
- Identification and Characterization of Novel NMDA Receptor Antagonists Selective for NR2A-over NR2B-Containing Receptors
[作者:Bettini, E; Sava, A; Griffante, C; Carignani, C; Buson, A; Capelli, AM; Negri, M; Andreetta, F; Senar-Sancho, SA; Guiral, L; Cardullo, F,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:636-644 , 文章类型: Article,,卷期:2010年335-3]
- NR1/NR2A is a subtype of N-methyl-D-aspartate receptors (NMDARs), which are glutamate and glycine-gated Ca2+ permeable channels highly expressed in the central nervous system. A high-throughput screening (HTS) campaign u...
- Effects of a Positive Allosteric Modulator of Group II Metabotropic Glutamate Receptors, LY487379, on Cognitive Flexibility and Impulsive-Like Responding in Rats
[作者:Nikiforuk, A; Popik, P; Drescher, KU; van Gaalen, M; Relo, AL; Mezler, M; Marek, G; Schoemaker, H; Gross, G; Bespalov, A,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:665-673 , 文章类型: Article,,卷期:2010年335-3]
- Orthosteric group II metabotropic glutamate receptor (mGluR) agonists are regarded as novel, effective medications for all major symptom domains of schizophrenia, including cognitive disturbances. mGluR2s also can be aff...
- Dexmedetomidine Induces Both Relaxations and Contractions, via Different alpha(2)-Adrenoceptor Subtypes, in the Isolated Mesenteric Artery and Aorta of the Rat
[作者:Wong, ESW; Man, RYK; Vanhoutte, PM; Ng, KFJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:659-664 , 文章类型: Article,,卷期:2010年335-3]
- Dexmedetomidine is an alpha(2)-adrenoceptor agonist and anesthetic. The present study was designed to characterize the receptor subtypes and the downstream mechanisms of the vascular effects of dexmedetomidine in small (...
- Comparison of Prostaglandin E-2 Receptor Subtype 4 Agonist and Sulfasalazine in Mouse Colitis Prevention and Treatment
[作者:Jiang, GL; Bin Im, W; Donde, Y; Wheeler, LA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:546-552 , 文章类型: Article,,卷期:2010年335-3]
- Prodrugs of 5-aminosalicylic acid (5-ASA), such as sulfasalazine, have been the mainstay for the treatment and maintenance of inflammatory bowel disease (IBD) for decades, which is attributable to their antiadaptive immu...
- Stimulation of alpha 7 Nicotinic Acetylcholine Receptor by Nicotine Increases Suppressive Capacity of Naturally Occurring CD4(+)CD25(+) Regulatory T Cells in Mice In Vitro
[作者:Wang, DW; Zhou, RB; Yao, YM; Zhu, XM; Yin, YM; Zhao, GJ; Dong, N; Sheng, ZY,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:553-561 , 文章类型: Article,,卷期:2010年335-3]
- alpha 7 Nicotinic acetylcholine receptor (alpha 7 nAChR) has been found in several non-neuronal cells and is described as an important regulator of cellular function. Naturally occurring CD4(+)CD25(+) regulatory T cells ...
- Differential Activation of Pregnane X Receptor and Constitutive Androstane Receptor by Buprenorphine in Primary Human Hepatocytes and HepG2 Cells
[作者:Li, LH; Hassan, HE; Tolson, AH; Ferguson, SS; Eddington, ND; Wang, HB,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:562-571 , 文章类型: Article,,卷期:2010年335-3]
- Buprenorphine is a partial mu-opioid receptor agonist used for the treatment of opioid dependence that has several advantages over methadone. The principal route of buprenorphine disposition has been well established; ho...
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