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Phentolamine selectively blocks C-fiber conduction in different species, including humans

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Electrophysiological analysis reveals phentolamine selectively reduces C-fiber conduction, suggesting its potential in pain modulation.

Phentolamine reduces compound action potential amplitudes in C-fibers more than in A-fibers, indicating a selective impact on nociceptive pathways.
A concentration of 100 µM phentolamine inhibited action potentials in cutaneous C-fibers while not affecting A-fibers, showing its specificity.
Using patch-clamp experiments, phentolamine was shown to block voltage-gated sodium channels, with Na V 1.8 being the most sensitive.
These findings highlight phentolamine's potential for exploring C-fiber function and developing selective pain relief agents.

Engler et al. (2025) studied this question.

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