- VUF10166, a Novel Compound with Differing Activities at 5-HT(3)A and 5-HT(3)AB Receptors
[作者:Thompson, AJ; Verheij, MHP; de Esch, IJP; Lummis, SCR,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:350-359 , 文章类型: Article,,卷期:2012年341-2]
- The actions of a novel, potent 5-HT(3) receptor ligand, [2-chloro(4-methylpiperazine-1-yl)quinoxaline (VUF10166)], were examined at heterologously expressed human 5-HT(3)A and 5-HT(3)AB receptors. VUF10166 displaced [(3)...
- Species Comparison and Pharmacological Characterization of Human, Monkey, Rat, and Mouse TRPA1 Channels
[作者:Bianchi, BR; Zhang, XF; Reilly, RM; Kym, PR; Yao, BB; Chen, J,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:360-368 , 文章类型: Article,,卷期:2012年341-2]
- The transient receptor potential ankyrin-1 (TRPA1) channel has emerged as an attractive target for development of analgesic and anti-inflammatory drugs. However, drug discovery efforts targeting TRPA1 have been hampered ...
- Characterization of Seizures Induced by Acute and Repeated Exposure to Tetramethylenedisulfotetramine
[作者:Zolkowska, D; Banks, CN; Dhir, A; Inceoglu, B; Sanborn, JR; McCoy, MR; Bruun, DA; Hammock, BD; Lein, PJ; Rogawski, MA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:435-446 , 文章类型: Article,,卷期:2012年341-2]
- Tetramethylenedisulfotetramine (tetramine; TETS) is a potent convulsant poison that is considered to be a chemical threat agent. To provide a basis for the investigation of antidotes for TETS-induced seizures, we charact...
- Pharmacologic Targeting of Bacterial beta-Glucuronidase Alleviates Nonsteroidal Anti-Inflammatory Drug-Induced Enteropathy in Mice
[作者:LoGuidice, A; Wallace, BD; Bendel, L; Redinbo, MR; Boelsterli, UA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:447-454 , 文章类型: Article,,卷期:2012年341-2]
- Small intestinal mucosal injury is a frequent adverse effect caused by nonsteroidal anti-inflammatory drugs (NSAIDs). The underlying mechanisms are not completely understood, but topical (luminal) effects have been impli...
- Role of Corticotropin-Releasing Factor and Corticosterone in Behavioral Sensitization to Ethanol
[作者:Pastor, R; Reed, C; Meyer, PJ; McKinnon, C; Ryabinin, AE; Phillips, TJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:455-463 , 文章类型: Article,,卷期:2012年341-2]
- Neuroadaptations underlying sensitization to drugs of abuse seem to influence compulsive drug pursuit and relapse associated with addiction. Our previous data support a role for the corticotropin-releasing factor (CRF) t...
- Pharmacokinetic Characterization of Amrubicin Cardiac Safety in an Ex Vivo Human Myocardial Strip Model. I. Amrubicin Accumulates to a Lower Level than Doxorubicin or Epirubicin
[作者:Salvatorelli, E; Menna, P; Surapaneni, S; Aukerman, SL; Chello, M; Covino, E; Sung, V; Minotti, G,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:464-473 , 文章类型: Article,,卷期:2012年341-2]
- Antitumor anthracyclines such as doxorubicin and epirubicin are known to cause cardiotoxicity that correlates with anthracycline accumulation in the heart. The anthracycline amrubicin [(7S,9S)-9-acetyl-9-amino-7-[(2-deox...
- Pharmacokinetic Characterization of Amrubicin Cardiac Safety in an Ex Vivo Human Myocardial Strip Model. II. Amrubicin Shows Metabolic Advantages over Doxorubicin and Epirubicin
[作者:Salvatorelli, E; Menna, P; Paz, OG; Surapaneni, S; Aukerman, SL; Chello, M; Covino, E; Sung, V; Minotti, G,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:474-483 , 文章类型: Article,,卷期:2012年341-2]
- Anthracycline-related cardiotoxicity correlates with cardiac anthracycline accumulation and bioactivation to secondary alcohol metabolites or reactive oxygen species (ROS), such as superoxide anion (O(2)(radical anion))a...
- Prevention of Bleomycin-Induced Lung Fibrosis in Mice by a Novel Approach of Parallel Inhibition of Cyclooxygenase and Nitric-Oxide Donation Using NCX 466, a Prototype Cyclooxygenase Inhibitor and Nitric-Oxide Donor
[作者:Pini, A; Viappiani, S; Bolla, M; Masini, E; Bani, D,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:493-499 , 文章类型: Article,,卷期:2012年341-2]
- Cyclooxygenase (COX)-inhibiting nitric oxide (NO) donors (CINODs) are designed to inhibit COX-1 and COX-2 while releasing NO. COX inhibition is responsible for anti-inflammatory and pain-relieving effects, whereas NO don...
- Ca(2+) Channel Activators Reveal Differential L-Type Ca(2+) Channel Pharmacology between Native and Stem Cell-Derived Cardiomyocytes
[作者:Kang, JS; Chen, XL; Ji, JZ; Lei, QB; Rampe, D,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:510-517 , 文章类型: Article,,卷期:2012年341-2]
- Human stem cell-derived cardiomyocytes provide new models for studying the ion channel pharmacology of human cardiac cells for both drug discovery and safety pharmacology purposes. However, detailed pharmacological chara...
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