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Endothelin receptor antagonists

Clinical Pharmacology of Endothelin Receptor Antagonists Used in the Treatment of Pulmonary Arterial Hypertension

Clinical Pharmacology of Endothelin Receptor Antagonists Used in the Treatment of Pulmonary Arterial Hypertension

... secrete endothelin (ET-1) in vessels that lead to a potent and long-lasting vasoconstrictive effect in pulmonary arterial smooth muscle ...of endothelin receptor antagonists (ERA) used in the ...

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Iontophoresis of endothelin receptor antagonists in rats and men.

Iontophoresis of endothelin receptor antagonists in rats and men.

... low endothelin-dependent vascular tone in the skin of healthy rats or to the absence of iontophoretic transport into the dermis, we repeated the experiment while infusing endothelin (experiment ...of ...

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From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells

From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells

... Several endothelin receptor antagonists have been developed for the treatment of pulmonary arterial ...some endothelin receptor antagonists can be hepatotoxic and that the ...

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LIGAND-RECEPTOR INTERACTIONS

LIGAND-RECEPTOR INTERACTIONS

... While Hoh et al. (1992) may have detected hydrogen bonds with atomic force microscopy, the application of this apparatus to the study of ligand-receptor interactions was pioneered by Florin et al. (1994) and Lee ...

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Severe undernutrition increases bleeding risk on vitamin-K antagonists

Severe undernutrition increases bleeding risk on vitamin-K antagonists

... Patients with intracranial bleeding exhibited lower INR values and higher vitamin B1 levels than those with other bleeding sites.. Patients with gastrointestinal blee[r] ...

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Nonpeptide antagonists of neuropeptide receptors: tools for research and therapy.

Nonpeptide antagonists of neuropeptide receptors: tools for research and therapy.

... 1 receptor antagonists 5 ...1 receptor antagonists was designed to resemble the C-terminal region of NPY, considered an important site for the interaction with the Y 1 receptor; it ...

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Les antagonists du récepteur CB1 des cannabinoïdes : une nouvelle approche pour le traitement de la fibrose hépatique

Les antagonists du récepteur CB1 des cannabinoïdes : une nouvelle approche pour le traitement de la fibrose hépatique

... Nous avons observé que l’expres- sion des récepteurs CB1 et CB2 est fortement induite dans les zones de fibrose au cours de la cirrhose chez l’homme, notamment dans les myo- fibroblas[r] ...

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A novel role for myeloid endothelin-B receptors in hypertension

A novel role for myeloid endothelin-B receptors in hypertension

... of endothelin-1 following acute depletion of circulating monocytes and resident M/ (DTR þ DT þ ), and in controls [those with the diphtheria toxin receptor (DTR) construct but given saline, DTR þ DT - , and ...

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Endothelin-Dependent Vasoconstriction in Human Uterine Artery: Application to Preeclampsia

Endothelin-Dependent Vasoconstriction in Human Uterine Artery: Application to Preeclampsia

... competitive antagonists. Moreover, antagonists, applied individually or in combination, were unable to relax ET-1-precontracted arteries, which could be explained by the rapid internalization of ET-1/ ETR ...

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Direct Action of Endothelin-1 on Podocytes Promotes Diabetic Glomerulosclerosis

Direct Action of Endothelin-1 on Podocytes Promotes Diabetic Glomerulosclerosis

... 65. Schiwek D, Endlich N, Holzman L, Holthöfer H, Kriz W, Endlich K: Stable expression of nephrin and localization to cell-cell contacts in novel murine podocyte cell lines. Kidney Int 66: 91–101, 2004 66. Bollée G, ...

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Role of the human chymase (CMA1) in the conversion of big-endothelin-1 to endothelin-1 (1-31)

Role of the human chymase (CMA1) in the conversion of big-endothelin-1 to endothelin-1 (1-31)

... vivo. The initiation of our experiments was based on the fact that our group has demonstrated that the mMCP-4 has the capacity to cleave Big ET-1 into ET-1 (1-31) in vivo and in vitro (Houde et al., 2013). In the mouse ...

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Fluorescent agonists and antagonists for vasopressin/oxytocin g protein-coupled receptors: usefulness in ligand screening assays and receptor studies.

Fluorescent agonists and antagonists for vasopressin/oxytocin g protein-coupled receptors: usefulness in ligand screening assays and receptor studies.

... V2 receptor in the principal cells of rabbit collecting ducts ...V2 receptor in the basal plasma membrane of the LLC-PK1 porcine epithelial cells by microphotolysis (photobleaching) ...V2 receptor ...

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N-methyl d-aspartate receptor antagonists ketamine and MK-801 induce wake-related aberrant gamma oscillations in the rat neocortex.

N-methyl d-aspartate receptor antagonists ketamine and MK-801 induce wake-related aberrant gamma oscillations in the rat neocortex.

... Is ketamine- or MK-801-induced increased  synchrony specific for the blockage of NMDAr? Non-competitive NMDAr antagonists also bind at least at sigma (18) and dopaminergic (13) receptors. Our data show that ...

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Endothelin-1 in osteoarthritic chondrocytes triggers nitric oxide production and upregulates collagenase production

Endothelin-1 in osteoarthritic chondrocytes triggers nitric oxide production and upregulates collagenase production

... of endothelin-1 (ET-1) on nitric oxide (NO) release and inducible nitric oxide synthase (iNOS) expression by human osteoarthritis (OA) chondrocytes Effect of endothelin-1 (ET-1) on nitric oxide (NO) release ...

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Intracrine endothelin signaling evokes IP3-dependent increases in nucleoplasmic Ca2+ in adult cardiac myocytes

Intracrine endothelin signaling evokes IP3-dependent increases in nucleoplasmic Ca2+ in adult cardiac myocytes

... Intracrine signalling refers to a process whereby a ligand, originating within a target cell or taken up from the extracellular milieu, acts upon an intracellular receptor (reviewed in [9-11, 62-67]). The origin ...

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Estrogen Receptor Related Receptor Alpha (ERRα) in Skeletal Tissues

Estrogen Receptor Related Receptor Alpha (ERRα) in Skeletal Tissues

... 11. Luegmayr E, Glantschnig H, Wesolowski G, Gentile M, Fisher J, Rodan G, et al. Osteoclast formation, survival and morphology are highly dependent on exogenous cholesterol/lipoproteins. Cell death Differ. 2004 ...

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Endothelin-1 in osteoarthritic chondrocytes triggers nitric oxide production and upregulates collagenase production.

Endothelin-1 in osteoarthritic chondrocytes triggers nitric oxide production and upregulates collagenase production.

... by endothelin-1 (ET-1) in human osteoarthritis (OA) chondrocytes Phosphorylation of p38 mitogen-activated protein (MAP) kinase, Akt, p44/42 and stress-activated protein kinase/Jun-N-terminal kinase (SAP/JNK) by ...

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Regulation of cardiac nitric oxide signaling by nuclear β-adrenergic and endothelin receptors

Regulation of cardiac nitric oxide signaling by nuclear β-adrenergic and endothelin receptors

... and endothelin receptors can regulate nitric oxide (NO) ...B endothelin receptors (ETB) are present in cardiac nuclear membranes and regulate ...and endothelin increased NO production in isolated ...

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The nuclear receptor liver receptor homolog-1 is an estrogen receptor target gene.

The nuclear receptor liver receptor homolog-1 is an estrogen receptor target gene.

... developmental defects, such as impaired node formation and gastrulation (Pare et al., 2004). During adulthood, LRH-1 plays important roles in cholesterol and lipid homeostasis by controlling the expression of genes ...

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Small Molecule CCR4 Antagonists Protect Mice from Aspergillus Infection and Allergy

Small Molecule CCR4 Antagonists Protect Mice from Aspergillus Infection and Allergy

... 3.4. The CCR4 Antagonist SP50 Protects a Murine Model of Cystic Fibrosis from Aspergillosis Based on previous results, we resorted to a murine model of CF challenged with A. fumigatus and first evaluated the expression ...

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