Subcutaneous application of local anesthetic drug lidocaine and cardiac antiarrhythmic n-propyl-ajmaline produced the reversible use-dependent inhibition of feline polymodal mechano-heat C-fiber cutaneous sensory units (CMH-units) excited by moderate noxious mechanical stimulus. The discharge rate as well as the number of evoked spikes of polymodal sensory units treated with the drugs decreased below the values observed under noxious chemical excitation of CMH-units. The repeated mechano-stimulation with 5 to 30 sec interval between stimuli produced complete though a reversible block of the treated units. Quaternary amine n-propyl-ajmaline induced use-dependent inhibition of CMH-units in lower concentrations than tertiary amine lidocaine. The use-dependent inhibition of CMH-units is discussed in connection with nociception and local analgesia.
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J Headache Pain
February 2025
Brain Science & Engineering Institute, Kyungpook National University, 2177 Dalgubeol-daero, Jung-gu, Daegu, 41940, Republic of Korea.
Background: Although peripheral administration of pregnenolone sulfate (PS) has been reported to produce pronociceptive effects, the mechanisms by which PS modulates the excitability of nociceptive neurons are poorly understood. Here, we report on the excitatory role of PS in peripheral nociceptive neurons, focusing on its effects on tetrodotoxin-resistant (TTX-R) Na channels.
Methods: TTX-R Na current (I) mediated by Na1.
J Microbiol Biotechnol
November 2024
Department of Biotechnology and Department of Integrative Food, Bioscience and Biotechnology (BK21 FOUR), Chonnam National University, Gwangju 61186, Republic of Korea.
This study investigates the modulatory effects of nicergoline, a major bioactive compound derived from ergot fungus, on the 5-hydroxytryptamine 3A (5-HT3A) receptor. Utilizing a two-electrode voltage-clamp technique, we evaluated the impact of nicergoline on the 5-HT-induced inward current (I) in 5-HT3A receptors. Our findings reveal that nicergoline inhibits I in a reversible and concentration-dependent manner.
View Article and Find Full Text PDFKorean J Physiol Pharmacol
December 2024
Department of Pharmacology, College of Medicine, The Catholic University of Korea, Seoul 06591, Korea.
Olanzapine, an atypical antipsychotic, is widely used in the treatment of schizophrenia and bipolar disorder due to its modulation of dopamine and serotonin receptor systems. While its primary action involves antagonism of dopamine D2 and serotonin 5-HT (5-hydroxytryptamine)A receptors, recent evidence suggests that olanzapine also inhibits 5-HT receptors, which are ligand-gated ion channels involved in synaptic transmission in central and peripheral nervous systems. The present study aimed to investigate the action of olanzapine on 5-HT receptor-mediated currents using whole-cell voltage-clamp recordings in NCB-20 neuroblastoma cells.
View Article and Find Full Text PDFJ Clin Invest
December 2024
Department of Pharmacology and Therapeutics, College of Medicine and.
Korean J Physiol Pharmacol
November 2024
Department of Pharmacology, College of Medicine, The Catholic University of Korea, Seoul 06591, Korea.
Haloperidol is a typical antipsychotic drug effective in alleviating positive symptoms of schizophrenia by blocking dopamine receptor 2 (DR2). However, it is also known to produce neuropsychiatric effects by acting on various targets other than DR. In this study, we investigated effect of haloperidol on function of 5-hydroxytryptamine (5-HT) receptor, a ligand-gated ion channel belonging to the serotonin receptor family using the whole-cell voltage clamp technique and NCB20 neuroblastoma cells.
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