SAS-1121

SAS-1121 is an organic molecule which binds to a specific protein, the sigma-2 receptor, found in cell membranes. It is highly selective for this over the related sigma-1 receptor. The sigma-2 receptor is significant in cancer and some neurological illnesses.

These two receptors are cell surface receptors: proteins in a cell membrane which pass a signal to the cell when some external molecule binds to them.

SAS-1121 is 280-fold selective for the sigma 2 receptor (K_i = 23.8 nM) ^[jargon] over the sigma 1 receptor (K_i = 6659.6 nM),^[jargon]^[1] and served as a tool compound to help identify the sigma 2 receptor as transmembrane 97 (TMEM97).^[2]

SAS-1121 is classed as a norbenzomorphan-piperazine.

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.
^ 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. 114 (27): 7160–7165. doi:10.1073/pnas.1705154114. ISSN 0027-8424. PMC 5502638. PMID 28559337.

[1] 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.

[2] 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. 114 (27): 7160–7165. doi:10.1073/pnas.1705154114. ISSN 0027-8424. PMC 5502638. PMID 28559337.

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