{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T01:21:16Z","timestamp":1760145676715,"version":"build-2065373602"},"reference-count":36,"publisher":"MDPI AG","issue":"8","license":[{"start":{"date-parts":[[2024,8,15]],"date-time":"2024-08-15T00:00:00Z","timestamp":1723680000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"French National Center for Scientific Research","award":["LOC34ERL9004","ANR-11-LABX-0015"],"award-info":[{"award-number":["LOC34ERL9004","ANR-11-LABX-0015"]}]},{"name":"French Alternative Energies and Atomic Energy Commission","award":["LOC34ERL9004","ANR-11-LABX-0015"],"award-info":[{"award-number":["LOC34ERL9004","ANR-11-LABX-0015"]}]},{"name":"French Agence Nationale de la Recherche for its financial support to the Laboratory of Excellence \u00ab Ion Channels, Science and Therapeutics \u00bb","award":["LOC34ERL9004","ANR-11-LABX-0015"],"award-info":[{"award-number":["LOC34ERL9004","ANR-11-LABX-0015"]}]},{"name":"CIFRE doctoral fellowship provided to Smartox Biotechnology (Saint-Egr\u00e8ve, France)","award":["LOC34ERL9004","ANR-11-LABX-0015"],"award-info":[{"award-number":["LOC34ERL9004","ANR-11-LABX-0015"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Toxins"],"abstract":"<jats:p>Crotalphine is an analgesic peptide identified from the venom of the South American rattlesnake Crotalus durissus terrificus. Although its antinociceptive effect is well documented, its direct mechanisms of action are still unclear. The aim of the present work was to study the action of the crotalid peptide on the NaV1.7 channel subtype, a genetically validated pain target. To this purpose, the effects of crotalphine were evaluated on the NaV1.7 component of the tetrodotoxin-sensitive Na+ current in the dorsal root ganglion neurons of adult mice, using the whole-cell patch-clamp configuration, and on cell viability, using propidium iodide fluorescence and trypan blue assays. The results show that 18.7 \u00b5M of peptide inhibited 50% of the Na+ current. The blocking effect occurred without any marked change in the current activation and inactivation kinetics, but it was more important as the membrane potential was more positive. In addition, crotalphine induced an increase in the leakage current amplitude of approximately 150% and led to a maximal 31% decrease in cell viability at a high 50 \u00b5M concentration. Taken together, these results point out, for the first time, the effectiveness of crotalphine in acting on the NaV1.7 channel subtype, which may be an additional target contributing to the peptide analgesic properties and, also, although less efficiently, on a second cell plasma membrane component, leading to cell loss.<\/jats:p>","DOI":"10.3390\/toxins16080359","type":"journal-article","created":{"date-parts":[[2024,8,15]],"date-time":"2024-08-15T03:49:36Z","timestamp":1723693776000},"page":"359","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["Rattlesnake Crotalphine Analgesic Active on Tetrodotoxin-Sensitive Na+ Current in Mouse Dorsal Root Ganglion Neurons"],"prefix":"10.3390","volume":"16","author":[{"given":"Aur\u00e9lie","family":"Antunes","sequence":"first","affiliation":[{"name":"D\u00e9partement M\u00e9dicaments et Technologies pour la Sant\u00e9 (DMTS), Institut des Sciences du Vivant Fr\u00e9d\u00e9ric Joliot, Universit\u00e9 Paris-Saclay, CEA, Service d\u2019Ing\u00e9nierie Mol\u00e9culaire pour la Sant\u00e9 (SIMoS), EMR CNRS\/CEA 9004, F-91191 Gif-sur-Yvette, France"},{"name":"Smartox Biotechnology, F-38120 Saint-Egr\u00e8ve, France"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Philippe","family":"Robin","sequence":"additional","affiliation":[{"name":"D\u00e9partement M\u00e9dicaments et Technologies pour la Sant\u00e9 (DMTS), Institut des Sciences du Vivant Fr\u00e9d\u00e9ric Joliot, Universit\u00e9 Paris-Saclay, CEA, Service d\u2019Ing\u00e9nierie Mol\u00e9culaire pour la Sant\u00e9 (SIMoS), EMR CNRS\/CEA 9004, F-91191 Gif-sur-Yvette, France"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gilles","family":"Mourier","sequence":"additional","affiliation":[{"name":"D\u00e9partement M\u00e9dicaments et Technologies pour la Sant\u00e9 (DMTS), Institut des Sciences du Vivant Fr\u00e9d\u00e9ric Joliot, Universit\u00e9 Paris-Saclay, CEA, Service d\u2019Ing\u00e9nierie Mol\u00e9culaire pour la Sant\u00e9 (SIMoS), EMR CNRS\/CEA 9004, F-91191 Gif-sur-Yvette, France"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"R\u00e9my","family":"B\u00e9roud","sequence":"additional","affiliation":[{"name":"Smartox Biotechnology, F-38120 Saint-Egr\u00e8ve, France"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2782-9615","authenticated-orcid":false,"given":"Michel","family":"De Waard","sequence":"additional","affiliation":[{"name":"Smartox Biotechnology, F-38120 Saint-Egr\u00e8ve, France"},{"name":"L\u2019Institut du Thorax, INSERM, CNRS, Universit\u00e9 de Nantes, F-44007 Nantes, France"},{"name":"LabEx \u201cIon Channels, Science and Therapeutics\u201d, F-06560 Valbonne, France"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0774-1691","authenticated-orcid":false,"given":"Denis","family":"Servent","sequence":"additional","affiliation":[{"name":"D\u00e9partement M\u00e9dicaments et Technologies pour la Sant\u00e9 (DMTS), Institut des Sciences du Vivant Fr\u00e9d\u00e9ric Joliot, Universit\u00e9 Paris-Saclay, CEA, Service d\u2019Ing\u00e9nierie Mol\u00e9culaire pour la Sant\u00e9 (SIMoS), EMR CNRS\/CEA 9004, F-91191 Gif-sur-Yvette, France"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5501-0888","authenticated-orcid":false,"given":"Evelyne","family":"Benoit","sequence":"additional","affiliation":[{"name":"D\u00e9partement M\u00e9dicaments et Technologies pour la Sant\u00e9 (DMTS), Institut des Sciences du Vivant Fr\u00e9d\u00e9ric Joliot, Universit\u00e9 Paris-Saclay, CEA, Service d\u2019Ing\u00e9nierie Mol\u00e9culaire pour la Sant\u00e9 (SIMoS), EMR CNRS\/CEA 9004, F-91191 Gif-sur-Yvette, France"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2024,8,15]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","unstructured":"Frare, B.T., Silva Resende, Y.K., Dornelas, B.C., Jorge, M.T., Souza Ricarte, V.A., Alves, L.M., and Izidoro, L.F.M. 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