The endothelins(ET) are a family of potent vasoactive peptides first isolated from the supernatant of cultured porcine aorta cells. Currently, three members of the endothelin family, namely ET-1, 2 and 3, are known. Elevated levels of ET-1 have been found in patients with myocardial infarction, vasospastic angina, cardiogenic and septic shock, sub-arachnoid hemorrhage and renal failure[3]. Endothelins are formed from the corresponding big endothelins through the action of endothelin converting enzymes. They exert their actions via specific membrane recepters. Two endothelin receptor subtypes have been isolated and cloned[3]. The sulfanilamide antibacterial agent sulfisoxazole is found to be a good endothelin receptor antagonist (IC50's of 0.60 µM and 22 µM for the ETA and ETB receptors, respectively) [3]. ET-1 causes a dose dependent accumulation of phosphoinositide metabolites in TE 671 cells and in the transfected COS 7 cells in the presence of lithium. Addition of sulfisoxazole results in a parallel shift to the right of the ET-1 dose response curve in the TE 671 cells indicating that sulfisoxazole acts as a functional antagonist of ET-1 in this system[3]. Experimental studies in rats have recently proved that the use of the antagonist protects the retina against ischemic damage in processes like glaucoma, reducing electro-retinogram alterations and normalizing changes in the acetylcolintransferase levels, synthethase nitric oxide, Thy-1(a specific marker of retina ganglionary cells) and FGF-2 (trophic factor produced by glial cells in stress conditions), typical of ischemia conditions[4].
United States, Kentucky
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University of Louisville
Recruiting
Louisville, Kentucky, United States, 40202
Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu
Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu
Sub-Investigator: Forest Arnold, DO
Sub-Investigator: Timothy Wiemkwn, PhD
Sub-Investigator: Robert Kelley, PhD
Sub-Investigator: James Summersgill, PhD
Sub-Investigator: Ruth Carrico, PhD
Sub-Investigator: Julie Harting, PharmD
Sub-Investigator: Paula Peyrani, MD
Principal Investigator: David Seligson, MD
Sub-Investigator: Craig Roberts, MD
Principal Investigator: Julio Ramirez, MD 收起 <<
United States, Kentucky
... 展开 >>
University of Louisville
Recruiting
Louisville, Kentucky, United States, 40202
Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu
Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu
Sub-Investigator: Forest Arnold, DO
Sub-Investigator: Timothy Wiemkwn, PhD
Sub-Investigator: Robert Kelley, PhD
Sub-Investigator: James Summersgill, PhD
Sub-Investigator: Ruth Carrico, PhD
Sub-Investigator: Julie Harting, PharmD
Sub-Investigator: Paula Peyrani, MD
Principal Investigator: David Seligson, MD
Sub-Investigator: Craig Roberts, MD
Principal Investigator: Julio Ramirez, MD 收起 <<
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