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dc.contributor.advisorMeisheri, Kaushik D.
dc.contributor.authorRop, Eric C.
dc.date.accessioned2012-02-13T16:49:17Z
dc.date.available2012-02-13T16:49:17Z
dc.date.issued1995
dc.identifier.urihttp://hdl.handle.net/10920/24962
dc.descriptionvi, 49 p.en_US
dc.description.abstractU-37883A, a novel blocker of ATP-sensitive K+ channels, produces a unique, nonkaliuretic, natriuretic diuresis in vivo by directly affecting the kidney. Specific binding of the renal U-37883A receptor was characterized by testing the abilities of several classes of chemically diverse compounds to compete for 3H-U-37883 binding in dog renal cortex membranes. Classes of K ATP modulators tested for their ability to competitively bind at the renal U-37883A receptor included U-37883A guanidine analogs, the sulfonylurea and K ATP' blocker glyburide, cyanoguanidine K ATP blockers and openers, other structurally diverse K ATP openers, and several imidazoline compounds. Several U-37883A guanidine analogs competitively displaced 3H-U37883 binding at 10 µM. Of all other structurally diverse classes of K ATP modulators tested, only the imidazoline compounds phentolamine and antazoline showed significant (95 .2 and 73 .0% respectively) displacement of 3H-U37883 at 10 µM . The general correlation of a compound's activity in the renal 3H-U37883 binding assay and in the in vitro K ATP channel blockade assay, demonstrated the similarity of the U-37883A receptors in these two tissues. However, some compounds were found to be either kidney selective (U56521E) or vascular selective (U-38313E). Thus, this study shows that the U-37883A receptor specifically mediates the K ATP channel blocking activity of several U-37883A guanidine analogs and imidazolines, and that the U-37883A receptors in the kidney and the vasculature are very similar, but can be differentiated.en_US
dc.description.sponsorshipCardiovascular Diseases Research. Upjohn Company. Kalamazoo, Michigan.
dc.format.mimetypeapplication/pdf
dc.language.isoen_USen_US
dc.relation.ispartofKalamazoo College Health Sciences Senior Individualized Projects Collection
dc.relation.ispartofseriesSenior Individualized Projects. Health Sciences;
dc.rightsU.S. copyright laws protect this material. Commercial use or distribution of this material is not permitted without prior written permission of the copyright holder. All rights reserved.
dc.titleReceptor Binding Characterization in Dog Renal Cortex Membranes of (3H) U-37883, a Novel ATP-Sensitive K+ Channel Blocker and In Vivo Diuretic/Natriureticen_US
dc.typeThesisen_US
KCollege.Access.ContactIf you are not a current Kalamazoo College student, faculty, or staff member, email dspace@kzoo.edu to request access to this thesis.


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