AI Article Synopsis
- Some norbenzomorphans have a strong attraction to sigma 1 and sigma 2 receptors, and changing substituents on their aromatic ring can affect which receptor subtype they prefer.
- Compounds with different substituents at C7 tend to favor the sigma 1 receptor, while those at C8 are more likely to bind to the sigma 2 receptor.
- This variability in binding suggests that the norbenzomorphan structure could be a valuable tool for creating small molecules that help researchers study the specific effects of targeting these sigma receptors, especially since the sigma 2 receptor's structure is not well understood yet.
Article 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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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5392765 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.7b00066 | DOI Listing |
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