Delving into the Latest Updates on Rhone-Poulenc Rorer Central Research with Synapse

概览

疾病领域	数量

免疫系统疾病	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

CysLT1(半胱氨酰白三烯受体-1)	1

关联

1

项与 Rhone-Poulenc Rorer Central Research 相关的药物

RG-7152

靶点

CysLT1

作用机制

CysLT1拮抗剂

在研机构

Rhone-Poulenc Rorer Central Research

原研机构

Sanofi

在研适应症

哮喘

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

100 项与 Rhone-Poulenc Rorer Central Research 相关的临床结果

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0 项与 Rhone-Poulenc Rorer Central Research 相关的专利（医药）

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102

项与 Rhone-Poulenc Rorer Central Research 相关的文献（医药）

2010-02-18·Journal of Pharmacy and Pharmacology3区 · 医学

The Role of an α-Amino Group on H+-dependent Transepithelial Transport of Cephalosporins in Caco-2 Cells

3区 · 医学

Article

作者: Li, Jibin ; Hidalgo, Ismael J ; Raeissi, Shamsi D

AbstractThe role of an α-amino group on interaction with the intestinal and renal peptide carriers (PEPT 1 and PEPT 2, respectively) has been the subject of much investigation. Studies have differed in their conclusions about the role of an α-amino group on carrier-mediated absorption. Most studies have used brush-border membrane vesicles or perfused intestinal segments. These techniques enable the determination of membrane uptake and luminal disappearance, respectively, but not transepithelial transport. Transepithelial transport should be more predictive of absorption because it includes basolateral efflux, which could be the rate-limiting process in drug absorption. The objective of this study was to evaluate the influence of an α-amino group on PEPT 1-mediated transepithelial transport in Caco-2 cells.The apical-to-basolateral permeability coefficients of cephalosporins with or without a free α-amino group were determined in the presence and absence of a pH gradient. Permeability coefficients obtained under these conditions were used to calculate a permeability ratio (i.e. Papp (pH 6.0)/Papp (pH 7.4)), which should indicate whether PEPT 1 is involved in transport. For cephalosporins with an α-amino group (cephalexin, cefaclor, cefadroxil, cephradine, cephaloglycin) the permeability ratios ranged between 1.77 and 2.77. In contrast, the permeability ratios for cephalosporins without an α-amino group were 1 (approx.; range = 0.74–1.26).These data suggest that the presence of an α-amino group on cephalosporins increases their PEPT 1-mediated transepithelial transport in Caco-2 monolayers.

2010-02-18·Journal of Pharmacy and Pharmacology3区 · 医学

Estimation of Oral Bioavailability in the Rat by the Accelerated Infusion Technique

3区 · 医学

Article

作者: Guo, Zuyu ; Luo, Yongyi ; Marietta, Michael P ; Hidalgo, Ismael J ; Rhodes, Gerald R ; Dobson, Glenn L

The intrinsic oral bioavailability of five drugs, paracetamol, cephalexin, aminopyrine, penicillin G, and penicillin V in rats estimated by accelerated infusion were similar or qual. comparable with those estimated by the conventional bolus dosing-AUC method.For the five drugs studied there is a good agreement between the qual. rankings of intrinsic oral bioavailability values obtained by both methods.If good exptl. designs are used it might be possible to obtain not only linear kinetic range and organ extraction ratio, but also intrinsic oral bioavailability in a single study with a relatively small number of animals.

1999-05-01·Journal of Cardiovascular Pharmacology4区 · 医学

Cardiovascular Pharmacology of the Adenosine A1/A2-Receptor Agonist AMP 579: Coronary Hemodynamic and Cardioprotective Effects in the Canine Myocardium

4区 · 医学

Article

作者: Clark, Kenneth L. ; Smits, Glenn J. ; McVey, Matthew J. ; Kitzen, Jan M. ; Cox, Bryan F. ; Perrone, Mark H.

The hemodynamic and cardioprotective properties of the novel adenosine A1/A2 receptor agonist AMP 579 (IS-[1a,2b,3b,4a(S*)]-4-[7-[[1-[(3-chloro-2-thienyl)methyl]propylamino]- 3H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxy cyclopentanecarboxamide) were studied in two canine models designed to simulate (a) mild single-vessel coronary artery disease, and (b) myocardial ischemia/reperfusion injury. In the first model, a moderate stenosis was placed on the left circumflex coronary artery (LCCA), and the effects of AMP 579 on regional myocardial blood flow were assessed. AMP 579, 10 micrograms/kg/min, i.v., for 10 min, induced coronary dilation without causing endocardial steal. In the model of ischemia/reperfusion injury (60 min LCCA occlusion/5 h reperfusion), AMP 579, 10 micrograms/kg/min, i.v., administered for 15 min before ischemia significantly decreased myocardial infarct size. Control infarct size to area at risk (IS/AAR) equaled 34 +/- 3% (n = 9); IS/AAR for AMP 579-treated dogs equaled 16 +/- 4% (n = 9). Preconditioning (5 min LCCA occlusion + 10 min reperfusion) immediately before the 60-min LCCA occlusion also resulted in a marked decrease in IS/AAR: 9 +/- 3% (n = 6). The selective A1 agonist CPA reduced infarct size when administered at 3 micrograms/kg/min, i.v., for 15 min before LCCA occlusion: IS/AAR = 11 +/- 3% (n = 5). Pretreatment of animals with the adenosine-receptor antagonist 8-SPT, 10 mg/kg, i.v., attenuated the myocardial protective effects associated with preconditioning, CPA, and AMP 579, resulting in IS/AAR values of 28 +/- 7% (n = 7), 28 +/- 4% (n = 8), and 26 +/- 3% (n = 8), respectively. The ability of 8-SPT to block the cardioprotective effects suggests that these effects were mediated through an interaction with adenosine receptors. These experimental results indicate that AMP 579 is an effective coronary vasodilator, which also can protect the heart from ischemic injury. Thus AMP 579 has the potential to be useful in cardiovascular therapeutics.

100 项与 Rhone-Poulenc Rorer Central Research 相关的药物交易

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100 项与 Rhone-Poulenc Rorer Central Research 相关的转化医学

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