ArticleACS medicinal chemistry letters2017
Norbenzomorphan Scaffold: Chemical Tool for Modulating Sigma Receptor-Subtype Selectivity.
Article in ACS medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
15 citing papers in PubMed, 32 citations in OpenAlex.
- Review
- Highly specific σProceedings of the National Academy of Sciences of the United States of America · 2023Article
- Highly specific σbioRxiv : the preprint server for biology · 2023Article
- σScientific reports · 2022Article
- Neuroprotective Effects of σACS chemical neuroscience · 2022Article
- Identification and characterization of MAM03055A: A novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity.European journal of pharmacology · 2021Article
- 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
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Some norbenzomorphans exhibit high affinity for sigma 1 and sigma 2 receptors, and varying the position of substituents on the aromatic ring of this scaffold has a significant effect on subtype selectivity. In particular, compounds bearing several different substituents at C7 of the norbenzomorphan ring system exhibit a general preference for the sigma 1 receptor, whereas the corresponding C8-substituted analogues preferentially bind at the sigma 2 receptor. These findings suggest that the norbenzomorphan scaffold may be a unique chemical template that can be easily tuned to prepare small molecules for use as tool compounds to study the specific biological effects arising from preferential binding at either sigma receptor subtype. In the absence of structural characterization data for the sigma 2 receptor, such compounds will be useful toward refining the pharmacophore model of its binding site.
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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.