ArticleChemMedChem2016
Norbenzomorphan Framework as a Novel Scaffold for Generating Sigma 2 Receptor/PGRMC1 Subtype-Selective Ligands.
Article in ChemMedChem, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 26 citations in OpenAlex.
- "Cut-and-Sew" Reactions of β-Lactams via C-C Bond Activation.Journal of the American Chemical Society · 2025Article
- Neuroprotective Effects of σACS chemical neuroscience · 2022Article
- Virtual Screening for Ligand Discovery at the σACS medicinal chemistry letters · 2020Article
- Development of Tetrahydroindazole-Based Potent and Selective Sigma-2 Receptor Ligands.ChemMedChem · 2019Article
- Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.Bioorganic & medicinal chemistry · 2019Article
- Neuroprotective Efficacy of a Sigma 2 Receptor/TMEM97 Modulator (DKR-1677) after Traumatic Brain Injury.ACS chemical neuroscience · 2019Article
- Small molecule modulators of σ2R/Tmem97 reduce alcohol withdrawal-induced behaviors.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Article
- High-Content Microfluidic Screening Platform Used To Identify σ2R/Tmem97 Binding Ligands that Reduce Age-Dependent Neurodegeneration in C. elegans SC_APP Model.ACS chemical neuroscience · 2018Article
- Natural Products and Their Mimics as Targets of Opportunity for Discovery.The Journal of organic chemistry · 2017Article
- Sigma 2 Receptor/Tmem97 Agonists Produce Long Lasting Antineuropathic Pain Effects in Mice.ACS chemical neuroscience · 2017Article
- Identification of the gene that codes for the σProceedings of the National Academy of Sciences of the United States of America · 2017Article
- Norbenzomorphan Scaffold: Chemical Tool for Modulating Sigma Receptor-Subtype Selectivity.ACS medicinal chemistry letters · 2017Article
- Small molecule modulator of sigma 2 receptor is neuroprotective and reduces cognitive deficits and neuroinflammation in experimental models of Alzheimer's disease.Journal of neurochemistry · 2017Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
A novel structural class with high affinity and subtype selectivity for the sigma 2 receptor has been discovered. Preliminary structure-affinity relationship data are presented showing that 8-substituted 1,3,4,5-tetrahydro-1,5-methanobenzazepine (norbenzomorphan) derivatives elicit modest to high selectivity for the sigma 2 over the sigma 1 receptor subtype. Indeed, piperazine analogue 8-(4-(3-ethoxy-3-oxopropyl)piperazin-1-yl)-1,3,4,5-tetrahydro-1,5-methanobenzazepine-2-carboxylate (SAS-1121) is 574-fold selective for the sigma 2 over the sigma 1 receptor, thereby establishing it as one of the more subtype-selective sigma 2 binding ligands reported to date. Emerging evidence has implicated the sigma 2 receptor in multiple health disorders, so the drug-like characteristics of many of the selective sigma 2 receptor ligands disclosed herein, coupled with their structural similarity to frameworks found in known drugs, suggest that norbenzomorphan analogues may be promising candidates for further development into drug leads.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.