Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues

Background and purpose: The recent development of the UT ligand palosuran (1‐[2‐(4‐benzyl‐4‐hydroxy‐piperidin‐1‐yl)‐ethyl]‐3‐(2‐methyl‐ quinolin‐4‐yl)‐urea sulphate salt) has led to the proposition that urotensin‐II (U‐II) plays a significant pathological role in acute and chronic renal injury in th...

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Veröffentlicht in:	British journal of pharmacology 2008-10, Vol.155 (3), p.374-386
Hauptverfasser:	Behm, D J, McAtee, J J, Dodson, J W, Neeb, M J, Fries, H E, Evans, C A, Hernandez, R R, Hoffman, K D, Harrison, S M, Lai, J M, Wu, C, Aiyar, N V, Ohlstein, E H, Douglas, S A
Format:	Artikel
Sprache:	eng
Schlagworte:	ACT‐058362 Animals antagonist Associated diseases and complications Biological and medical sciences Cats Cell Line Cell Membrane - drug effects Cell Membrane - metabolism CHO Cells Cricetinae Cricetulus Diabetes. Impaired glucose tolerance diabetic nephropathy Endocrine pancreas. Apud cells (diseases) Endocrinopathies Etiopathogenesis. Screening. Investigations. Target tissue resistance GPR14 G‐protein‐coupled receptor Humans Inhibitory Concentration 50 Kidneys Macaca fascicularis Male Medical sciences Mice Nephrology. Urinary tract diseases palosuran Pharmacology. Drug treatments Quinolines - administration & dosage Quinolines - pharmacology Radioligand Assay Rats Rats, Sprague-Dawley Rats, Wistar Receptors, G-Protein-Coupled - drug effects Receptors, G-Protein-Coupled - metabolism Research Papers SB‐657510 Species Specificity Urea - administration & dosage Urea - analogs & derivatives Urea - pharmacology Urinary system involvement in other diseases. Miscellaneous Urotensins - drug effects Urotensins - metabolism urotensin‐II
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