Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use.

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

1973 • 12,522 citations

SOME QUANTITATIVE USES OF DRUG ANTAGONISTS

1959 • 3,948 citations

Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.

1994 • 650 citations

Evidence for endothelin-1-mediated vasoconstriction in severe chronic heart failure

1995 • 575 citations

Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties

1981 • 557 citations

Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels.

1994 • 521 citations

Reversal of postischemic acute renal failure with a selective endothelinA receptor antagonist in the rat.

1994 • 198 citations

Pathophysiological role of endothelin in acute renal failure

1990 • 173 citations

Role of endothelin in the maintenance of blood pressure in conscious rats with chronic heart failure. Acute effects of the endothelin receptor antagonist Ro 47-0203 (bosentan).

1994 • 165 citations

Effect of different endothelin receptor antagonists and of the novel non‐peptide antagonist Ro 46‐2005 on endothelin levels in rat plasma

1993 • 122 citations

In Vitro Biological Profile of a Highly Potent Novel Endothelin (ET) Antagonist BQ-123 Selective for the ETA Receptor

1992 • 116 citations

Activation of endothelin ET_A receptors masks the constrictor role of endothelin ET_B receptors in rat isolated small mesenteric arteries

1997 • 105 citations

Specific binding of endothelin on human vascular smooth muscle cells in culture.

1989 • 103 citations

Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

1996 • 102 citations

Necessity of dual blockade of endothelin ET_A and ET_B receptor subtypes for antagonism of endothelin‐1‐induced contraction in human bronchi

1996 • 87 citations

Specific receptors for endothelin on membranes from human placenta. Characterization and use in a binding assay

1989 • 82 citations

Downregulation of endothelin receptors by autocrine production of endothelin-1

1993 • 69 citations

Role of endothelin in acute renal failure due to rhabdomyolysis in rats.

1995 • 67 citations

Effects of a new endothelin antagonist, TAK-044, on post-ischemic acute renal failure in rats

1994 • 64 citations

Are There Different ETB Receptors Mediating Constriction and Relaxation?

1995 • 62 citations

Role of endogenous endothelin in normal hemodynamic status of anesthetized dogs

1995 • 52 citations

ET _A and ET _B Receptors Mediate Contraction to Endothelin-1 in Renal Artery of Aging SHR

1995 • 51 citations

Improvement of Postischemic Acute Renal Failure with the Novel Orally Active Endothelin-A Receptor Antagonist LU 135252 in the Rat

1998 • 50 citations

Endothelin in renal pathophysiology: From experimental to therapeutic application

1996 • 49 citations

In Vivo Pharmacology of Ro 46-2005, The First Synthetic Nonpeptide Endothelin Receptor Antagonist: Implications for Endothelin Physiology

1993 • 46 citations

In vitro characterisation of Ro 46‐8443, the first non‐peptide antagonist selective for the endothelin ET_B receptor

1996 • 43 citations

BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist.

1995 • 41 citations

Radioimmunological Determination of Endothelin Peptides in Human Plasma: A Methodological Approach

1994 • 39 citations

Isolation, characterisation, growth and culture of endothelial cells from the rat aorta

1986 • 30 citations

Role of Endothelin in a Rabbit Model of Acute Myocardial Infarction: Effects of Receptor Antagonists

1996 • 30 citations

Endothelin in ischemic acute renal failure

1997 • 29 citations

Potential contribution of endothelin to renal abnormalities in glycerol-induced acute renal failure in rats.

1998 • 25 citations

Radioimmunoassay evidence that the pressor effect of big endothelindash1 is due to local conversion to endothelindash1

1995 • 20 citations

Endothelin-1 in heart failure: a new therapeutic target?

1996 • 13 citations