title: Synthesis of the first sulfur-35-labeled hERG radioligand.
abstract: The synthesis of the first high specific activity S-35-labeled hERG radioligand, [(35)S]MK-0499, for use in HTS assays of drug candidates for hERG interaction is described. The radioligand is prepared by [(35)S]sulfonylation of a high diastereomeric excess (de) aniline precursor prepared from unlabeled MK-0499.
authors.affiliation: Department of Drug Metabolism, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. conrad_raab@merck.com
authors.forename: Conrad E
authors.initials: CE
authors.lastname: Raab
authors.forename: John W
authors.initials: JW
authors.lastname: Butcher
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Connolly
authors.forename: Jerzy
authors.initials: J
authors.lastname: Karczewski
authors.forename: Nathan X
authors.initials: NX
authors.lastname: Yu
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Staskiewicz
authors.forename: Nigel
authors.initials: N
authors.lastname: Liverton
authors.forename: Dennis C
authors.initials: DC
authors.lastname: Dean
authors.forename: David G
authors.initials: DG
authors.lastname: Melillo
mesh_terms: D001578:Benzopyrans / Q000737:chemistry* / Q000494:pharmacology*; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology; D013462:Sulfur Radioisotopes / Q000737:chemistry
chemical_list: D001578:Benzopyrans; D051638:Ether-A-Go-Go Potassium Channels; D010880:Piperidines; D026902:Potassium Channel Blockers; D019275:Radiopharmaceuticals; D013462:Sulfur Radioisotopes; C087257:L 706000