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Discovery of a novel K7.2/7.3 channels agonist for the treatment of neuropathic pain.
Eur J Med Chem
December 2024
Jiangsu Key Laboratory of Marine Biological Resources and Environment, Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, China. Electronic address:
Article Synopsis
- The researchers developed and tested a series of new compounds that act as agonists for KCNQ2/3 channels, which are important for pain management.
- Among the compounds, compound 16 exhibited strong activity specifically for KCNQ2/3 channels with good effectiveness in pain models without causing liver damage.
- Additionally, compound 16 demonstrated low risk of toxicity, maintained good motor function, and had favorable pharmacokinetic properties, indicating its potential as a treatment for neuropathic pain.
Efficacy of flupirtine for postoperative pain: A systematic review and meta-analysis.
Indian J Anaesth
March 2023
Department of Obstetrics and Gynaecology, All India Institute of Medical Sciences, Mangalgiri, Andhra Pradesh, India.
Background And Aims: Flupirtine has been used for various chronic pain conditions, but its utility in the perioperative period as an analgesic is still inconclusive. This systematic review and meta-analysis aimed to assess the efficacy of flupirtine for postoperative pain.
Methods: PubMed, Embase and the Cochrane Central Register of Controlled Trials (CENTRAL) were explored for the randomised controlled trials (RCTs) which compared flupirtine with other analgesic/placebo for perioperative pain in adult patients undergoing surgery.
Flupirtine and antihistamines exert synergistic anti-nociceptive effects in mice.
Psychopharmacology (Berl)
April 2023
Jiangsu Key Laboratory of Marine Biological Resources and Environment, Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, China.
Rationale: Drug combinations are commonly used in pain management, which can produce potent analgesic effects with reduced dosage and adverse effects.
Objective: This study was designed to evaluate the anti-nociceptive effects and adverse effects of new combinations of flupirtine (a Kv7 potassium channel opener) and antihistamines (promethazine, fexofenadine) on acute and chronic pain in mice, and the possible mechanisms behind the synergistic analgesic effects were preliminarily investigated.
Methods: In acetic acid writhing test, carrageenan-induced inflammatory pain model, and paclitaxel-induced neuropathic pain model, the interaction indexes (γ) between flupirtine and antihistamines were determined by isobolographic analysis.
Comparative study of analgesia of ketorolac, tramadol, and flupirtine in the management of third molar surgery.
Natl J Maxillofac Surg
June 2022
Department of Oral and Maxillofacial Surgery, Chandra Dental College, Barabanki, Uttar Pradesh, India.
Article Synopsis
- The study focuses on postoperative pain management in patients undergoing third molar removal, identifying it as acute pain caused by surgical trauma and inflammation.
- A total of 150 patients were divided into three groups and administered different analgesics, including Flupirtine, Tramadol, and Ketorolac, after surgery.
- Results showed that Flupirtine resulted in faster pain relief and fewer side effects compared to Tramadol, suggesting its recommendation for managing postoperative pain in third molar surgeries.
The KCNQ channel inhibitor XE991 suppresses nicotinic acetylcholine receptor-mediated responses in rat intracardiac ganglion neurons.
Pharmacol Rep
August 2022
Department of Physiology, School of Allied Health Sciences, Kitasato University, 1-15-1 Kitasato, Minami-ku, Sagamihara, Kanagawa, 252-0373, Japan.
Background: XE991 (10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone) is reportedly a potent and selective Kv7 (KCNQ) channel inhibitor. This study aimed to evaluate how XE991 affects nicotinic responses in intracardiac ganglion neurons.
Methods: We studied how the KCNQ channel inhibitor XE991 could affect nicotinic responses in acutely isolated rat intracardiac ganglion neurons using a perforated patch-clamp recording configuration and Ca imaging.
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