Determination of a highly selective mixed-affinity sigma receptor ligand, in rat plasma by ultra performance liquid chromatography mass spectrometry and its application to a pharmacokinetic study

► A selective, rapid and sensitive UPLC/MS method was developed and validated to quantitate a highly selective mixed-affinity sigma receptor ligand. ► The validated analytical method resulted in a run time of 4 min. The calibration curve exhibited excellent linearity over a concentration range of 5-4000 ng/mL (LLOQ, 5 ng/mL). The intra- and inter-day precision values were below 15% and accuracy ranged from −6.5% to 5.0%. ► The validated method was successfully applied to an intravenous pharmacokinetic study of CM156 in rats.