Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons.
Previous studies have shown that local anesthetics block voltage-dependent Na+ channels and nicotinic acetylcholine receptors. The present study investigated the effect of the local anesthetic, procaine on another ligand-gated ion channel, the 5-HT3 receptor, in rat nodose ganglion neurons. Procaine (0.01-100 microM) inhibited the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. The inhibition was fully reversible, concentration-dependent but not sensitive to changes in membrane potential. Concentration-response curves indicated that procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM. These observations suggest that one of the actions of procaine in nervous system is on 5-HT3 receptors.
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Laboratory of Molecular and Cellular Neurobiology, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892, USA.
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D000818:Animals; D007473:Ion Channels / Q000737:chemistry / Q000187:drug effects*; D008297:Male; D009474:Neurons / Q000187:drug effects*; D009620:Nodose Ganglion / Q000166:cytology / Q000187:drug effects*; D018408:Patch-Clamp Techniques; D011343:Procaine / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011985:Receptors, Serotonin / Q000737:chemistry / Q000187:drug effects*
D007473:Ion Channels; D011985:Receptors, Serotonin; D011343:Procaine