Synthesis and evaluation of novel, selective, functionalized γ-butyrolactones as sigma-2 ligands

Synthesis and evaluation of novel, selective, functionalized γ-butyrolactones as sigma-2 ligands

The sigma-2 (σ 2 ) receptor was discovered nearly 40 years ago and was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein)). Aberrant σ 2 activity has been linked to diseases and conditions such as schizophrenia, Alzheimer’s disease, neuro...

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Veröffentlicht in:Medicinal chemistry research 2022-02, Vol.31 (2), p.337-349
Hauptverfasser: Blass, Benjamin E., Gao, Rong, Blattner, Kevin M., Gordon, John C., Pippin, Douglas A., Canney, Daniel J.
Format: Artikel
Sprache:eng
Schlagworte:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Inorganic Chemistry
Medicinal Chemistry
Original Research
Pharmacology/Toxicology
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Zusammenfassung:The sigma-2 (σ 2 ) receptor was discovered nearly 40 years ago and was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein)). Aberrant σ 2 activity has been linked to diseases and conditions such as schizophrenia, Alzheimer’s disease, neuropathic pain, traumatic brain injury, and cancer. The utility of σ 2 as a therapeutic target is currently under investigation in numerous laboratories. Herein, we report on the synthesis and evaluation of a series of novel, functionalized γ-butyrolactones that are potent σ 2 receptor ligands.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-021-02831-5