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| Main Authors: | , , , , , , , , , |
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| Format: | Artículo científico |
| Language: | en |
| Published: |
Journal of natural products
2026
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| Subjects: | |
| Online Access: | https://pubmed.ncbi.nlm.nih.gov/41954290/ |
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Table of Contents:
- Antinociceptive Benzothiazine and Benzothiazole Natural Products from Marine . Marshall, Erin M Zhu, Chenxi Mayhood, Lydia Khalid, Zain Yao, Haoyi Panieri, Giuliana Cediel-Becerra, José D D Chevrette, Marc G Strother, James A Loesgen, Sandra Animals Benzothiazoles Analgesics Zebrafish Molecular Structure Biological Products Thiazines With the goal of identifying new therapeutic leads to treat pain, we screened a library of microbial chemical extracts using the Embryonic Zebrafish Irritant-evoked Hyperlocomotion (EZIH) assay, an phenotypic assay for analgesic/antinociceptive activity. We found that extracts from the bacterium substantially altered behavioral responses. Using behavior-guided fractionation to identify the active partitions, we determined that the known 1,4-benzothiazin-3-one BPSS2111-2113:C and the new benzothiazole croceithiazole A suppress behavioral responses to painful and/or nociceptive stimuli without apparent acute toxicity. Further investigation with radioligand binding assays revealed that BPSS2111-2113:C shows selective binding to both the serotonin receptor 5-HT2B and the benzodiazepine site of GABAA receptors, while croceithiazole A appears to bind the peripheral benzodiazepine receptor. These results suggest that BPSS2111-2113:C and croceithiazole A are interesting leads as analgesics, sedatives, anesthetics, or molecular probes.