Metabotropic glutamate receptor 1 (mGluR1) has been a prime target for drug discovery due to its heavy involvement in various brain disorders. Recent studies suggested that mGluR1 is associated with chronic pain and can serve as a promising target for the treatment of neuropathic pain. In an effort to develop a novel mGluR1 antagonist, we designed and synthesized a library of compounds with tetrahydrothieno[2,3-c]pyridine scaffold. Among these compounds, compound 9b and 10b showed excellent antagonistic activity in vitro and demonstrated pain-suppressing activity in animal models of pain. Both compounds were orally active, and compound 9b exhibited a favorable pharmacokinetic profile in rats. We believe that these compounds can provide a promising lead compound that is suitable for the potential treatment of neuropathic pain.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.ejmech.2015.04.060 | DOI Listing |
Eur J Pain
February 2025
Center for Mathematics, Computation and Cognition, Federal University of ABC, São Bernardo do Campo, SP, Brazil.
Background And Objective: Non-invasive neuromodulation techniques (NIN), such as transcranial Direct Current Stimulation (tDCS) and repetitive Transcranial Magnetic Stimulation (rTMS), have been extensively researched for their potential to alleviate pain by reversing neuroplastic changes associated with neuropathic pain (NP), a prevalent and complex condition. However, treating NP remains challenging due to the numerous variables involved, such as different techniques, dosages and aetiologies. It is necessary to provide insights for clinicians and public healthcare managers to support clinical decision-making.
View Article and Find Full Text PDFFront Neurol
January 2025
Department of Pain Medicine, China-Japan Friendship Hospital, Beijing, China.
Purpose: Postherpetic neuralgia (PHN) is a type of refractory neuropathic pain that causes significant suffering, disability, economic loss, and medical burden. In this study, we aim to evaluate the efficacy and safety of interferon (IFN)-α1b injection into the intervertebral foramen of patients with PHN.
Patients And Methods: This is a study protocol for a randomized, double-blind placebo-controlled multicenter clinical trial.
Pain Manag
January 2025
Division of Pain Medicine, Department of Anesthesiology, Perioperative, and Pain Medicine, Stanford University, Stanford, CA, USA.
Aim: We aimed to evaluate real-world outcomes of peripheral nerve stimulation (PNS) used to treat chronic neuropathic pain (CNP) at a tertiary pain management center.
Methods: Thirty adults who underwent PNS for CNP between June 2015 and September 2021 completed pain and psychosocial assessments in the 6 months before, and 2-3 years after PNS treatment. Pain intensity was measured using the NIH Patient Reported Outcomes Measurement Information System (PROMIS) Pain Intensity Short From (3A).
FASEB J
January 2025
Department of Physiology, Yonsei University College of Medicine, Seoul, Republic of Korea.
Neuropathic pain, caused by nerve damage, greatly affects quality of life. Recent research proposes modulating brain activity, particularly through electrical stimulation of the insular cortex (IC), as a treatment option. This study aimed to understand how IC stimulation (ICS) affects pain modulation.
View Article and Find Full Text PDFFront Pharmacol
January 2025
Pharmacology and Therapeutics, School of Medicine, University of Galway, Galway, Ireland.
Paclitaxel (PTX) is a commonly used chemotherapeutic drug, however, one of its major adverse effects is chronic neuropathic pain, with the incidence being higher in women than in men. The neurobiological mechanisms behind this sex difference are still largely unclear, and the endocannabinoid system, which exhibits sexual dimorphism and plays a key role in pain regulation, is a promising area for further studies. The present study aimed to characterise pain-, cognition-, anxiety-, and depression-related behaviours in male and female rats following PTX administration, and associated alterations in the endocannabinoid system.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!