SAS-1121
SAS-1121 is a norbenzomorphan-piperazine that is highly selective for the sigma 2 receptor over the sigma 1 receptor. SAS-1121 is 280-fold selective for for the sigma 2 receptor (Ki = 23.8 nM) over the sigma 1 receptor (Ki = 6659.6 nM)[1] and served as a tool compound to help identify the sigma 2 receptor as transmembrane 97 (TMEM97).[2]
References
- ^ Sahn, James J.; Hodges, Timothy R.; Chan, Jessica Z.; Martin, Stephen F. (2017-04-13). "Norbenzomorphan Scaffold: Chemical Tool for Modulating Sigma Receptor-Subtype Selectivity". ACS Medicinal Chemistry Letters. 8 (4): 455–460. doi:10.1021/acsmedchemlett.7b00066. PMC 5392765. PMID 28435536.
{{cite journal}}: CS1 maint: PMC format (link) - ^ Alon, Assaf; Schmidt, Hayden R.; Wood, Michael D.; Sahn, James J.; Martin, Stephen F.; Kruse, Andrew C. (2017-05-30). "Identification of the gene that codes for the σ2 receptor". Proceedings of the National Academy of Sciences: 201705154. doi:10.1073/pnas.1705154114. ISSN 0027-8424. PMID 28559337.
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