Phentolamine selectively blocks C-fiber conduction in different species, including humans
Suppressing AP conduction and inhibiting VGSCs, phentolamine exhibits features reminiscent of local anesthetics, but with a stronger effect on C-fibers, which may be attributed to its stronger action on tetrodotoxin-resistant VGSCs. However, due to its markedly higher affinity for α-adrenergic receptors compared with VGSCs, systemic administration of phentolamine is limited by its adrenergic side effects. These findings suggest that phentolamine could be useful for exploring C-fiber function and provide a basis for the development of more selective and potent antinociceptive agents.
Authors
- Maike Franziska Dohrn (ORCID: https://orcid.org/0000-0002-5320-9807)
- Jannis Körner (ORCID: https://orcid.org/0000-0002-8537-1606)
- Natja Haag (ORCID: https://orcid.org/0000-0002-2482-5969)
- Andelain Erickson (ORCID: https://orcid.org/0000-0001-8134-7919)
- Idil Toklucu (ORCID: https://orcid.org/0009-0005-4403-3028)
- Karl Meßlinger (ORCID: https://orcid.org/0000-0002-8099-3860)
- Stanislav Koulchitsky (ORCID: https://orcid.org/0000-0001-9504-6404)
- Roberto DeCol
- Raya Bott
- Siegfried Engler
- Tal Hoffmann (ORCID: https://orcid.org/0000-0002-8893-3520)
- Angelika Lampert (ORCID: https://orcid.org/0000-0001-6319-6272)
- Justus P. Beier (ORCID: https://orcid.org/0000-0002-0179-1962)
- Ralf Hausmann (ORCID: https://orcid.org/0000-0002-0130-110X)
- Robert Brunkhorst
- Barbara Namer
Institutions
- Friedrich-Alexander-Universität Erlangen-Nürnberg (DE)
- University of Würzburg (DE)
- Augenklinik Universitätsklinikum Würzburg (DE)
- Universitätsklinikum Aachen (DE)
- Universitätsklinikum Würzburg (DE)
- RWTH Aachen University (DE)
Publication Details
- Journal
- Regional Anesthesia & Pain Medicine
- Published
- 2025-09-21
- DOI
- https://doi.org/10.1136/rapm-2025-106791
- Citations
- 1
- Primary Topic
- Pain Mechanisms and Treatments
- Type
- article
- Field-Weighted Citation Impact
- 1.16