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Phorbol dibutyrate enhances local anaesthetic action
S Austin1, J McGivern, C N Scholfield
1School of Biomedical Science, Queen's University, Belfast.
British Journal of Pharmacology
|January 1, 1991
Summary
Phorbol ester enhances the effects of local anesthetics like lignocaine and procaine on olfactory cortex responses. This potentiation suggests protein kinase C activation modifies anesthetic action, though the exact mechanism remains unclear.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Local anesthetics, such as lignocaine and procaine, are known to depress synaptic transmission.
- Phorbol esters are activators of protein kinase C, an enzyme involved in various cellular signaling pathways.
Purpose of the Study:
- To investigate the effect of phorbol esters on the depressant action of local anesthetics on synaptic responses in the rat olfactory cortex.
- To explore the potential involvement of protein kinase C in modulating the efficacy of local anesthetics.
Main Methods:
- Synaptically-evoked field responses were recorded from rat olfactory cortex slices.
- The effects of varying concentrations of lignocaine and procaine on these responses were assessed.
- The influence of beta-phorbol 12,13-dibutyrate and beta-phorbol 13-monobutyrate on anesthetic potency was evaluated.
Main Results:
- Lignocaine and procaine produced dose-dependent depressions of synaptic responses.
- Beta-phorbol 12,13-dibutyrate significantly increased the potency of both lignocaine and procaine.
- Beta-phorbol 13-monobutyrate had no effect on anesthetic potency, and phorbol dibutyrate did not affect presynaptic Na+ and K+ currents.
Conclusions:
- Activation of protein kinase C by phorbol dibutyrate potentiates the depressant effects of lignocaine and procaine on olfactory cortex synaptic transmission.
- The mechanism of potentiation is likely related to protein kinase C signaling, distinct from direct effects on ion channels or transmitter release.