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PF-04691502, a Potent and Selective Oral Inhibitor of PI3K and mTOR Kinases with Antitumor Activity
Deregulation of the phosphoinositide 3-kinase (PI3K) signaling pathway such as by PTEN loss or PIK3CA mutation occurs frequently in human cancer and contributes to resistance to antitumor therapies.Expand
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Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
The affinity of eletriptan ((R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]-1H-indole) for a range of 5-HT receptors was compared to values obtained for other 5-HT1B/1D receptorExpand
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Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain.
In vivo microdialysis was used to assess the central serotonergic effects and extracellular brain levels of the 5-HT(1B/1D) receptor agonists eletriptan, zolmitriptan and sumatriptan in rats afterExpand
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Effects of Chronic PPAR-Agonist Treatment on Cardiac Structure and Function, Blood Pressure, and Kidney in Healthy Sprague-Dawley Rats
PPAR-γ agonists have been associated with heart failure (HF) in diabetic patients. These incidences have been reported mostly in patient populations who were at high risk for HF or had pre-existingExpand
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Time course of AQP-2 and ENaC regulation in the kidney in response to PPAR agonists associated with marked edema in rats.
Peroxisome-proliferator-activated receptor (PPAR-gamma) agonists improve insulin sensitivity, but are associated with edema. Increased distal tubule sodium and water reabsorption through theExpand
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Characterisation of the contractile activity of eletriptan at the canine vascular 5-HT1B receptor.
The functional activity of eletriptan ((R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]- 1 H-indole) at the contractile serotonin (5-hydroxytryptamine; 5-HT) '1B-like' receptor inExpand
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Sunitinib, a receptor tyrosine kinase inhibitor, increases blood pressure in rats without associated changes in cardiac structure and function.
BACKGROUND Sunitinib, a multi-tyrosine kinase inhibitor has demonstrated clinical activity in advanced renal cell carcinoma and imatinib-resistant/intolerant gastrointestinal stromal tumor. It hasExpand
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Reconciling Human Rights and the Public Interest: Conceptual Problems and Doctrinal Uncertainty in the Jurisprudence of the European Court of Human Rights
The incorporation of the European Convention on Human Rights (ECHR) by the Human Rights Act 1998 raises many interesting questions concerning how deeply it will penetrate the United Kingdom'sExpand
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Brexit and Scotland
In the 2016 Brexit referendum, Scotland voted decisively to Remain in the EU, while a UK-wide majority voted to Leave. This article discusses responses to the constitutional significance of aExpand
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Community Benefit Through Community Ownership of Renewable Generation in Scotland: Power to the People?
Community ownership is being promoted by the Scottish Government as a means of delivering economic benefits to communities in which renewable electricity developments are situated. This paper arguesExpand
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