Synthesis, in vitro and in vivo evaluation of 3β-[18F]fluorocholic acid for the detection of drug-induced cholestasis in mice [PDF]
, 2017 Introduction : Drug-induced cholestasis is a liver disorder that might be caused by interference of drugs with the hepatobiliary bile acid transporters. It is important to identify this interference early on in drug development.
De Lombaerde, Stef +7 more
core +3 more sources
Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis. [PDF]
PLoS ONE, 2014 The competitive endothelin receptor antagonists (ERA) bosentan and ambrisentan, which have long been approved for the treatment of pulmonary arterial hypertension, are characterized by very short (1 min) occupancy half-lives at the ET(A) receptor.
John Gatfield +4 more
doaj +1 more source
Riociguat for the treatment of chronic thromboembolic pulmonary hypertension. [PDF]
, 2013 BACKGROUND: Riociguat, a member of a new class of compounds (soluble guanylate cyclase stimulators), has been shown in previous clinical studies to be beneficial in the treatment of chronic thromboembolic pulmonary hypertension. METHODS: In this phase 3,
CHEST-1 Study Group, +13 more
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Sildenafil dosed concomitantly with bosentan for adult pulmonary arterial hypertension in a randomized controlled trial [PDF]
, 2017 BACKGROUND: Few controlled clinical trials exist to support oral combination therapy in pulmonary arterial hypertension (PAH). METHODS: Patients with PAH (idiopathic [IPAH] or associated with connective tissue disease [APAH-CTD]) taking bosentan (62.5 ...
Dombi, Theresa +4 more
core +1 more source
Genetic susceptibility to hepatoxicity due to bosentan treatment in pulmonary hypertension
Annals of Hepatology, 2014 Background. Hepatotoxicity is a major side effect of treatment with bosentan in patients with pulmonary hypertension (PH). Bosentan is metabolized by the cytochrome CYP2C9 and inhibits the bile salt export pump, which is encoded by ABCB11.
Hans-Jürgen Seyfarth +9 more
doaj +1 more source
Glucocorticoids for treating paediatric pulmonary hypertension: A novel use for a common medication [PDF]
, 2017 Laboratory investigations have shown the role of inflammation in the pathogenesis of pulmonary hypertension and improvement after anti-inflammatory drugs.
Aggarwal, Manish, Grady, Ronald M
core +2 more sources
The molecular genetics and cellular mechanisms underlying pulmonary arterial hypertension [PDF]
, 2012 Pulmonary arterial hypertension (PAH) is an incurable disorder clinically characterised by a sustained elevation of mean arterial pressure in the absence of systemic involvement.
Machado, Rajiv
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Spectroscopic analysis of bosentan in biological samples after a liquid-liquid microextraction [PDF]
BioImpacts, 2015 Introduction: Microextraction processes with UV-Vis measurement have been developed and validated for analysis of bosentan in biological samples. Methods: In this work, liquid–liquid microextraction procedures (DLLME & USAEME) were employed for cleanup ...
Sanaz Sajedi-Amin +7 more
doaj +1 more source
Drug Delivery, 2018 Pulmonary arterial hypertension (PAH) can be relieved by pharmacological interventions, especially the targeted drug, which is classified into endothelin receptor antagonist, phosphodiesterase 5 inhibitor, prostaglandin I2, soluble guanylate cyclase ...
Sumei Wang +3 more
doaj +1 more source
Endothelin-1 Drives Epithelial-Mesenchymal Transition In Hypertensive Nephroangiosclerosis [PDF]
, 2016 BACKGROUND: Tubulointerstitial fibrosis, the final outcome of most kidney diseases, involves activation of epithelial mesenchymal transition (EMT). Endothelin‐1 (ET‐1) activates EMT in cancer cells, but it is not known whether it drives EMT in the kidney.
Belloni, Anna S +13 more
core +1 more source