The effects of local anesthetics (LAs) on G protein-mediated responses of voltage-dependent K+ (I(K)) and Ca++ currents in rat anterior pituitary tumor (GH3) cells were analyzed by using a whole-cell voltage clamp. Extracellular lidocaine inhibited I(K) with an IC50 of 1.9 mM, comparable to 2.6 mM for I(Ba) but 10 times higher than the IC50 for I(Na) (0.17 mM). Low concentrations of lidocaine (30-100 microM), which had no direct effect on basal I(K), attenuated both the stimulatory and inhibitory modulation of K+ channels by thyrotropin-releasing hormone (TRH). Both modulations had an IC50 approximately 40 microM independent of [TRH]. Intracellular QX314 (100 microM), a quaternary, charged form of lidocaine, also significantly attenuated the TRH effects; however, external QX314 and the neutral LA benzocaine (100 microM) did not. Lidocaine (
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1124/mol.55.1.150 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The Utilization of Ultrasound-Guided Regional Nerve Blocks in Anesthetic Management for Fracture Surgery.
J Pain Res
January 2025
Department of General Surgery, The 955th Hospital of Chinese People's Liberation Army, Tibet, 854000, People's Republic of China.
Fracture surgeries are frequently accompanied by severe pain, necessitating efficacious pain management strategies to enhance postoperative recovery. Nerve block techniques, which are critical in mitigating pain, involve the targeted administration of local anesthetics to disrupt nerve signal transmission, thereby achieving significant analgesia. Traditionally, these techniques rely on anatomical landmarks and the clinician's expertise, which can introduce variability and potential risks.
View Article and Find Full Text PDFThe influence of Dexmedetomidine as an additive to local anesthetics in dental procedures: A systematic review.
Med Oral Patol Oral Cir Bucal
January 2025
Department of Oral and Maxillofacial Surgery Dental School, University of Pernambuco Arnóbio Marques St., 310 Zip code 50100-130, Recife, PE, Brazil
Background: This review aimed to assess if the use of dexmedetomidine as an additive to local anesthetics promotes greater safety and efficacy than local anesthetics alone in dental procedures.
Material And Methods: the systematic review was structured according to the PICO strategy and adhered to the Preferred Reporting Items for Systematic Reviews and Meta-analyses (PRISMA) checklist. Studies were included based on the eligibility criteria, and data from the included studies were collected by one author.
An Injectable Oil-Based Depot Formulation of -Acyloxymethyl Prodrug of Ropivacaine for Long-Acting Local Analgesia: Formulation Development and In Vitro/In Vivo Evaluation.
Pharmaceutics
December 2024
School of Pharmacy, Nantong University, 9 Seyuan Road, Nantong 226019, China.
The development of novel long-acting injectables for local anesthetics is necessary to effectively manage the acute postoperative pain. The aim of this study was to prepare an injectable oil-based formulation of ropivacaine (ROP) prodrug (ropivacaine stearoxil, ROP-ST) and to investigate the pharmacokinetics and pharmacodynamics after injectable administration. A novel -acyloxymethyl prodrug of ROP, i.
View Article and Find Full Text PDFLidocaine Enhanced Antitumor Efficacy and Relieved Chemotherapy-Induced Hyperalgesia in Mice with Metastatic Gastric Cancer.
Int J Mol Sci
January 2025
Department of Anaesthesiology, West China Hospital, Sichuan University, Chengdu 610041, China.
With the widespread use of lidocaine for pain control in cancer therapy, its antitumor activity has attracted considerable attention in recent years. This paper provides a simple strategy of combining lidocaine with chemotherapy drugs for cancer therapy, aiming to relieve chemotherapy-induced pain and achieve stronger antitumor efficacy. However, there is still a lack of substantial pre-clinical evidence for the efficacy and related mechanisms of such combinations, obstructing their potential clinical application.
View Article and Find Full Text PDFTopical anesthetics methods used to reduce needle pain/discomfort prior to local anesthesia in children and adolescents: a scoping review.
Evid Based Dent
January 2025
São Leopoldo Mandic College, Campinas, Brazil.
Objectives: The aim of this study was to review the most effective topical anesthetic methods for reducing pain/discomfort prior to dental local anesthetic needle puncture for dental procedures in children and adolescents.
Methods: A scoping review was conducted. Individual search strategies were developed for each of the bibliographic databases (Cochrane, Embase, LILACS, LIVIVO, Pubmed, Scopus, PsyINFO, Web of Science), and in the gray literature (Google Scholar, Open Gray), comprehensively, without restrictions on language, publication data, or level of socioeconomic development of the country in which the study was conducted.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!