title: Distinct epitopes on amiloride.
abstract: Most Na(+)-selective transport proteins are inhibited by the drug amiloride. Studies using amiloride analogues suggest that specific regions of amiloride might participate in binding to receptors on these transport proteins. To determine whether certain domains of this drug are recognized as distinct epitopes, amiloride was coupled to albumin through either its C-5 NH2-group on the pyrazine ring or through a terminal NH2-group of the guanidino moiety, and antibodies were raised against these amiloride-albumin conjugates. Studies of antibody binding to amiloride analogues identified the 3,5-diaminopyrazinyl, the guanidinocarbonyl, and the C-6 halo moieties as distinct epitopes, although the antibodies required the presence of both the 3,5-diaminopyrazinyl as well as the guanidinocarbonyl moiety for binding.
authors: Department of Medicine, University of Pennsylvania, Philadelphia 19104.
authors: T R
authors: TR
authors: Kleyman
authors: J P
authors: JP
authors: Kraehenbuhl
authors: B C
authors: BC
authors: Rossier
authors: E J
authors: EJ
authors: Cragoe
authors: D G
authors: DG
authors: Warnock
mesh_terms: D000584:Amiloride / Q000031:analogs & derivatives* / Q000276:immunology*; D000818:Animals; D000906:Antibodies; D000911:Antibodies, Monoclonal; D000936:Antigen-Antibody Complex / Q000032:analysis; D004797:Enzyme-Linked Immunosorbent Assay; D000939:Epitopes / Q000032:analysis*; D015394:Molecular Structure; D011817:Rabbits / Q000276:immunology; D012709:Serum Albumin; D013329:Structure-Activity Relationship
chemical_list: D000906:Antibodies; D000911:Antibodies, Monoclonal; D000936:Antigen-Antibody Complex; D000939:Epitopes; D012709:Serum Albumin; D000584:Amiloride