Synthesis of the first sulfur-35-labeled hERG radioligand.
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.
Raab
Conrad E
CE
Department of Drug Metabolism, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. conrad_raab@merck.com
Butcher
John W
JW
Connolly
Thomas M
TM
Karczewski
Jerzy
J
Yu
Nathan X
NX
Staskiewicz
Steven J
SJ
Liverton
Nigel
N
Dean
Dennis C
DC
Melillo
David G
DG
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
D001578:Benzopyrans; D051638:Ether-A-Go-Go Potassium Channels; D010880:Piperidines; D026902:Potassium Channel Blockers; D019275:Radiopharmaceuticals; D013462:Sulfur Radioisotopes; C087257:L 706000