- Proprotein Convertase Substilisin/Kexin Type 9 Antagonism Reduces Low-Density Lipoprotein Cholesterol in Statin-Treated Hypercholesterolemic Nonhuman Primates
[作者:Liang, H; Chaparro-Riggers, J; Strop, P; Geng, T; Sutton, JE; Tsai, D; Bai, LF; Abdiche, Y; Dilley, J; Yu, JS; Wu, S; Chin, SM; Lee, NA; Rossi, A; Lin, JC; Rajpal, A; Pons, J; Shelton, DL,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:228-236 , 文章类型: Article,,卷期:2012年340-2]
- Proprotein convertase substilisin/kexin type 9 (PCSK9) promotes the degradation of low-density lipoprotein (LDL) receptor (LDLR) and thereby increases serum LDL-cholesterol (LDL-C). We have developed a humanized monoclon...
- Histone H3 Phosphorylation (Ser10, Ser28) and Phosphoacetylation (K9S10) Are Differentially Associated with Gene Expression in Liver of Rats Treated In Vivo with Acute Ethanol
[作者:James, TT; Aroor, AR; Lim, RW; Shukla, SD,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:237-247 , 文章类型: Article,,卷期:2012年340-2]
- The epigenetic histone modification by ethanol is emerging as one of the mechanisms for its deleterious effects in the liver. In this context, we have investigated the role of histone H3 phosphorylation at Ser10 (P-H3-Se...
- Dipeptidyl Peptidase IV Inhibitor Attenuates Kidney Injury in Streptozotocin-Induced Diabetic Rats
[作者:Liu, WJ; Xie, SH; Liu, YN; Kim, W; Jin, HY; Park, SK; Shao, YM; Park, TS,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:248-255 , 文章类型: Article,,卷期:2012年340-2]
- Dipeptidyl peptidase (DPP) IV inhibitors are probably beneficial for preventing diabetic complication and modulating glucagon-like peptide-1 receptor (GLP-1R) expression. The aim of this study was to determine whether th...
- Methamphetamine Self-Administration Causes Persistent Striatal Dopaminergic Alterations and Mitigates the Deficits Caused by a Subsequent Methamphetamine Exposure
[作者:McFadden, LM; Hadlock, GC; Allen, SC; Vieira-Brock, PL; Stout, KA; Ellis, JD; Hoonakker, AJ; Andrenyak, DM; Nielsen, SM; Wilkins, DG; Hanson, GR; Fleckenstein, AE,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:295-303 , 文章类型: Article,,卷期:2012年340-2]
- Preclinical studies have demonstrated that repeated methamphetamine (METH) injections (referred to herein as a "binge" treatment) cause persistent dopaminergic deficits. A few studies have also examined the persistent ne...
- Characterization of Two Mutations, M287L and Q266I, in the alpha 1 Glycine Receptor Subunit That Modify Sensitivity to Alcohols
[作者:Borghese, CM; Blednov, YA; Quan, Y; Iyer, SV; Xiong, W; Mihic, SJ; Zhang, L; Lovinger, DM; Trudell, JR; Homanics, GE; Harris, RA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:304-316 , 文章类型: Article,,卷期:2012年340-2]
- Glycine receptors (GlyRs) are inhibitory ligand-gated ion channels. Ethanol potentiates glycine activation of the GlyR, and putative binding sites for alcohol are located in the transmembrane (TM) domains between and wit...
- Antiserotonergic Properties of Terguride in Blood Vessels, Platelets, and Valvular Interstitial Cells
[作者:Kekewska, A; Gornemann, T; Jantschak, F; Glusa, E; Pertz, HH,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:369-376 , 文章类型: Article,,卷期:2012年340-2]
- Serotonin (5-hydroxytryptamine; 5-HT) is involved in heart valve tissue fibrosis, pulmonary arterial fibrosis, and pulmonary hypertension. We aimed at characterizing the antiserotonergic properties of the ergot alkaloid ...
- Antagonism of Protease-Activated Receptor 2 Protects against Experimental Colitis
[作者:Lohman, RJ; Cotterell, AJ; Suen, J; Liu, LG; Do, AT; Vesey, DA; Fairlie, DP,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:256-265 , 文章类型: Article,,卷期:2012年340-2]
- Many trypsin-like serine proteases such as beta-tryptase are involved in the pathogenesis of colitis and inflammatory bowel diseases. Inhibitors of individual proteases show limited efficacy in treating such conditions, ...
- Competitive Inhibition of the Luminal Efflux by Multidrug and Toxin Extrusions, but Not Basolateral Uptake by Organic Cation Transporter 2, Is the Likely Mechanism Underlying the Pharmacokinetic Drug-Drug Interactions Caused by Cimetidine in the Kidney
[作者:Ito, S; Kusuhara, H; Yokochi, M; Toyoshima, J; Inoue, K; Yuasa, H; Sugiyama, Y,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:393-403 , 文章类型: Article,,卷期:2012年340-2]
- Cimetidine, an H 2 receptor antagonist, has been used to investigate the tubular secretion of organic cations in human kidney. We report a systematic comprehensive analysis of the inhibition potency of cimetidine for the...
- The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with L-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease
[作者:Jones, CK; Bubser, M; Thompson, AD; Dickerson, JW; Turle-Lorenzo, N; Amalric, M; Blobaum, AL; Bridges, TM; Morrison, RD; Jadhav, S; Engers, DW; Italiano, K; Bode, J; Daniels, JS; Lindsley, CW; Hopkins, CR; Conn, PJ; Niswender, CM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:404-421 , 文章类型: Article,,卷期:2012年340-2]
- Parkinson's disease (PD) is a debilitating neurodegenerative disorder associated with severe motor impairments caused by the loss of dopaminergic innervation of the striatum. Previous studies have demonstrated that posit...
- Carboxylesterases 1 and 2 Hydrolyze Phospho-Nonsteroidal Anti-Inflammatory Drugs: Relevance to Their Pharmacological Activity
[作者:Wong, CC; Cheng, KW; Xie, G; Zhou, DY; Zhu, CH; Constantinides, PP; Rigas, B,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:422-432 , 文章类型: Article,,卷期:2012年340-2]
- Phospho-nonsteroidal anti-inflammatory drugs (phospho-NSAIDs) are novel NSAID derivatives with improved anticancer activity and reduced side effects in preclinical models. Here, we studied the metabolism of phospho-NSAID...
- 3-Substituted Pyrazole Analogs of the Cannabinoid Type 1 (CB(1)) Receptor Antagonist Rimonabant: Cannabinoid Agonist-Like Effects in Mice via Non-CB(1), Non-CB(2) Mechanism
[作者:Wiley, JL; Selley, DE; Wang, PL; Kottani, R; Gadthula, S; Mahadeven, A,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:433-444 , 文章类型: Article,,卷期:2012年340-2]
- The prototypic cannabinoid type 1 (CB(1)) receptor antagonist/inverse agonist, rimonabant, is comprised of a pyrazole core surrounded by a carboxyamide with terminal piperidine group (3-substituent), a 2,4-dichlorophenyl...
- The TM2 6 ' Position of GABA(A) Receptors Mediates Alcohol Inhibition
[作者:Johnson, WD; Howard, RJ; Trudell, JR; Harris, RA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:445-456 , 文章类型: Article,,卷期:2012年340-2]
- Ionotropic GABA(A) receptors (GABA(A)Rs), which mediate inhibitory neurotransmission in the central nervous system, are implicated in the behavioral effects of alcohol and alcoholism. Site-directed mutagenesis studies su...
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