title: Measurement of the class III antidysrhythmic drug, UK-68,798, in plasma by radioimmunoassay.
abstract: A sensitive radioimmunoassay (RIA) for the specific determination of 1-(4-methanesulphonamidophenoxy)-2-[N-(4-methanesulphonamido -phenethyl)-N- methylamino]ethane (UK-68,798), a novel class III antidysrhythmic agent, in human plasma is described. Specific antisera were raised in sheep using desmesyl-UK-68,798-succinate-ovalbumin conjugate as the antigenic hapten carrier protein. The antisera produced exhibited high specificity for UK-68,798 compared with known metabolites from animals, other antidysrhythmic agents and co-administered drugs. Good correlation was found in a comparison of the RIA method with a high-performance liquid chromatography (HPLC) method (r = 0.997) and a 10-fold lower limit of determination was observed for the RIA method compared with the HPLC method (0.05 and 0.5 ng ml-1, respectively). The RIA method was applied to the analysis of UK-68,798 in plasma obtained from human volunteers receiving the compound.
authors.affiliation: Department of Drug Metabolism, Pfizer Central Research, Kent, UK.
authors.forename: D K
authors.initials: DK
authors.lastname: Walker
authors.forename: G W
authors.initials: GW
authors.lastname: Aherne
authors.forename: J E
authors.initials: JE
authors.lastname: Arrowsmith
authors.forename: P E
authors.initials: PE
authors.lastname: Cross
authors.forename: B
authors.initials: B
authors.lastname: Kaye
authors.forename: D A
authors.initials: DA
authors.lastname: Smith
authors.forename: D A
authors.initials: DA
authors.lastname: Stopher
authors.forename: W
authors.initials: W
authors.lastname: Wild
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000097:blood*; D000918:Antibody Specificity; D001322:Autoanalysis; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D006241:Haptens / Q000032:analysis / Q000138:chemical synthesis; D010627:Phenethylamines / Q000097:blood* / Q000138:chemical synthesis / Q000276:immunology; D011863:Radioimmunoassay; D051381:Rats; D012756:Sheep / Q000276:immunology; D013449:Sulfonamides / Q000097:blood* / Q000138:chemical synthesis / Q000276:immunology
chemical_list: D000889:Anti-Arrhythmia Agents; D006241:Haptens; D010627:Phenethylamines; D013449:Sulfonamides; C063533:dofetilide