- Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis
[作者:Bedard, PW; Clerin, V; Sushkova, N; Tchernychev, B; Antrilli, T; Resmini, C; Keith, JC; Hennan, JK; Kaila, N; DeBernardo, S; Janz, K; Wang, Q; Crandall, DL; Schaub, RG; Shaw, GD; Carter, LL,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:497-506 , 文章类型: Article,,卷期:2008年324-2]
P-selectin plays a significant and well documented role in vascular disease by mediating leukocyte and platelet rolling and adhesion. This study characterizes the in vitro activity, pharmacokinetic properties, and the...
- Contractile and vasorelaxant effects of hydrogen sulfide and its biosynthesis in the human internal mammary artery
[作者:Webb, GD; Lim, LH; Oh, VMS; Yeo, SB; Cheong, YP; Ali, MY; El Oakley, R; Lee, CN; Wong, PS; Caleb, MG; Salto-Tellez, M; Bhatia, M; Chan, ESY; Taylor, EA; Moore, PK,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:876-882 , 文章类型: Article,,卷期:2008年324-2]
This study aimed to test these hypotheses: cystathionine gamma-lyase (CSE) is expressed in a human artery, it generates hydrogen sulfide (H2S), and H2S relaxes a human artery. H2S is produced endogenously in rat arter...
- Gene expression analysis in rats treated with experimental acetyl-coenzyme A carboxylase inhibitors suggests interactions with the peroxisome proliferator-activated receptor alpha pathway
[作者:Waring, JF; Yang, Y; Healan-Greenberg, CH; Adler, AL; Dickinson, R; McNally, T; Wang, XJ; Weitzberg, M; Xu, XD; Lisowski, A; Warder, SE; Gu, YG; Zinker, BA; Blomme, EA; Camp, HS,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:507-516 , 文章类型: Article,,卷期:2008年324-2]
Acetyl CoA carboxylase (ACC) 2, which catalyzes the carboxylation of acetyl-CoA to form malonyl-CoA, has been identified as a potential target for type 2 diabetes and obesity. Small-molecule inhibitors of ACC2 would b...
- The guinea pig as a preclinical model for demonstrating the efficacy and safety of statins
[作者:Madsen, CS; Janovitz, E; Zhang, R; Nguyen-Tran, V; Ryan, CS; Yin, XH; Monshizadegan, H; Chang, M; D'Arienzo, C; Scheer, S; Setters, R; Search, D; Chen, X; Zhuang, SB; Kunselman, L; Peters, A; Harrity, T; Apedo, A; Huang, C; Cuff, CA; Kowala, MC; Blanar, MA; Sun, CQ; Robl, JA; Stein, PD,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:576-586 , 文章类型: Article,,卷期:2008年324-2]
Statins, because of their excellent efficacy and manageable safety profile, represent a key component in the current armamentarium for the treatment of hypercholesterolemia. Nonetheless, myopathy remains a safety conc...
- S33138[N-[4-[2-[(3aS, 9bR)-8-cyano-1,3a, 4,9b-tetrahydro[1]-benzopyrano[3,4-c] pyrrol-2(3H)-yl)-ethyl]phenylacetamide], a preferential dopamine D-3 versus D-2 receptor antagonist and potential antipsychotic agent: I. Receptor-binding profile and functional actions at G-protein-coupled receptors
[作者:Millan, MJ; La Cour, CM; Novi, F; Maggio, R; Audinot, V; Newman-Tancredi, A; Cussac, D; Pasteau, V; Boutin, JA; Dubuffet, T; Lavielle, G,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:587-599 , 文章类型: Article,,卷期:2008年324-2]
The novel, potential antipsychotic, S33138 (N-[4-[2-[(3aS, 9bR)-8-cyano-1,3a, 4,9b-tetrahydro[1]benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenylacetamide), displayed similar to 25-fold higher affinity at human (h) dopa...
- S33138[N-[4-[2-[(3aS, 9bR)-8-cyano-1, 3a, 4, 9b-tetrahydro[1]benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenylacetamide], a preferential dopamine D-3 versus D-2 receptor antagonist and potential antipsychotic agent. II. A neurochemical, electrophysiological and behavioral characterization in vivo
[作者:Millan, MJ; Svenningsson, P; Ashby, CR; Hill, M; Egeland, M; Dekeyne, A; Brocco, M; Di Cara, B; Lejeune, F; Thomasson, N; Munoz, C; Mocaer, E; Crossman, A; Cistarelli, L; Girardon, S; Iob, L; Veiga, S; Gobert, A,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:600-611 , 文章类型: Article,,卷期:2008年324-2]
The novel benzopyranopyrrolidine, S33138 [N-[4-[2-[(3aS, 9bR)-8-cyano-1, 3a, 4,9b-tetrahydro[1]benzopyrano[3,4-c]pyrrol-2(3H)-yl)ethyl]phenylacetamide], is a preferential antagonist of cloned human D-3 versus D-2L and...
- Single-vesicle catecholamine release has greater quantal content and faster kinetics in chromaffin cells from hypertensive, as compared with normotensive, rats
[作者:Miranda-Ferreira, R; de Pascual, R; de Diego, AMG; Caricati, A; Gandia, L; Jurkiewicz, A; Garcia, AG,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:685-693 , 文章类型: Article,,卷期:2008年324-2]
In a previous study performed in the intact adrenal gland (Lim et al., 2002), stimulation with acetylcholine (ACh) or high K+ concentrations (K+) produced greater catecholamine release in spontaneously hypertensive ra...
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