- Distinct Interactions of Human beta(1)- and beta(2)-Adrenoceptors with Isoproterenol, Epinephrine, Norepinephrine, and Dopamine
[作者:Weitl, N; Seifert, R,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:760-769 , 文章类型: Article,,卷期:2008年327-3]
Fluorescence studies with purified human beta(2)-adrenoceptor (beta(2)AR) revealed that the endogenous catecholamines, (-)-epinephrine (EPI), (-)-norepinephrine (NE), and dopamine (DOP), stabilize distinct active rece...
- Involvement of ST1B Subfamily of Cytosolic Sulfotransferase in Kynurenine Metabolism to Form Natriuretic Xanthurenic Acid Sulfate
[作者:Senggunprai, L; Yoshinari, K; Shimada, M; Yamazoe, Y,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:789-798 , 文章类型: Article,,卷期:2008年327-3]
Natriuretic substances are a group of molecules affecting sodium homeostasis in the body. Recently, two new molecules having natriuresis effects, xanthurenic acid 8-O-beta-D-glucoside and xanthurenic acid 8-O-sulfate ...
- Identification and Characterization of Novel Small-Molecule Protease-Activated Receptor 2 Agonists
[作者:Gardell, LR; Ma, JN; Seitzberg, JG; Knapp, AE; Schiffer, HH; Tabatabaei, A; Davis, CN; Owens, M; Clemons, B; Wong, KK; Lund, B; Nash, NR; Gao, Y; Lameh, J; Schmelzer, K; Olsson, R; Burstein, ES,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:799-808 , 文章类型: Article,,卷期:2008年327-3]
We report the first small-molecule protease-activated receptor (PAR) 2 agonists, AC-55541 [N-[[1-(3-bromo-phenyl)-eth-(E)-ylidene-hydrazinocarbonyl]-(4-oxo-3,4-dihydro-phthalazin-1-yl)-methyl]-benzamide] and AC-264613...
- Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity
[作者:Hill, RJ; Dabbagh, K; Phippard, D; Li, C; Suttmann, RT; Welch, M; Papp, E; Song, KW; Chang, KC; Leaffer, D; Kim, YN; Roberts, RT; Zabka, TS; Aud, D; Dal Porto, J; Manning, AM; Peng, SL; Goldstein, DM; Wong, BR,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:610-619 , 文章类型: Article,,卷期:2008年327-3]
P38 alpha is a protein kinase that regulates the expression of inflammatory cytokines, suggesting a role in the pathogenesis of diseases such as rheumatoid arthritis (RA) or systemic lupus erythematosus. Here, we desc...
- S32826, A Nanomolar Inhibitor of Autotaxin: Discovery, Synthesis and Applications as a Pharmacological Tool
[作者:Ferry, G; Moulharat, N; Pradere, JP; Desos, P; Try, A; Genton, A; Giganti, A; Beucher-Gaudin, M; Lonchampt, M; Bertrand, M; Saulnier-Blache, JS; Tucker, GC; Cordi, A; Boutin, JA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:809-819 , 文章类型: Article,,卷期:2008年327-3]
Autotaxin catalyzes the transformation of lyso-phosphatidylcholine in lyso-phosphatidic acid (LPA). LPA is a phospholipid possessing a large panel of activity, in particular as a motility factor or as a growth signal,...
- Inactivation of the Maternal Fragile X Gene Results in Sensitization of GABA(B) Receptor Function in the Offspring
[作者:Zupan, B; Toth, M,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:820-826 , 文章类型: Article,,卷期:2008年327-3]
Fragile X syndrome is an X-linked disorder caused by the inactivation of the FMR1 gene, with symptoms ranging from impaired cognitive functions to seizures, anxiety, sensory abnormalities, and hyperactivity. Although ...
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