This is a progress report on a National Institute of Justice (NIJ) grant project whose goal is to provide spectroscopic and pharmacological information relevant to law enforcement on two related series of synthetic opioids, AH-7921 and U-47700, along with a variety of analogues based on their core structures.
Progress is reported on the following three project methods: 1) the use of combinatorial approaches with commercially available starting material to create both report and novel analogs within each of the series; 2) the generation of a stable clonal OPRM1 expressing cell line and determination of rank order of potencies for signaling; and 3) the analytical characterization of analogs. The pharmacological studies, using an invitro functional assay for human OPRM1 receptor, provide a foundation from which effects in humans can be anticipated. These results provide key insights on the structure-activity relations (SAR) of the U- and AH-series analogues and information on their possibility of being abusable opioids. Raw GC/MS files for the analogs were provided to Jason Bordson (DEA Chicago) and are being reviewed by NIST for inclusion in the next version of the SWGDRUG database. Monographs that contain all the spectra for each of the analogs are being developed and will be submitted to SWGDRUG to be housed on its website and available to forensic researchers. The project is exploring other ways of making the data available to the forensic community.
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