We have shown that members of a new series of tricyclic pyridophthalazine diones, defined as glycineB site NMDA antagonists in vitro, are selective and systemically active NMDA antagonists in vivo. In electrophysiological tests in alpha-chloralose anaesthetised rats, these compounds reduced nociceptive reflex responses. In conscious rats they displayed analgesic properties. These glycineB antagonists were compared electrophysiologically with several uncompetitive NMDA channel blockers. The degree of voltage dependence previously reported in vitro related to the effectiveness of the agents against different amplitude nociceptive responses of spinal cord neurones in vivo.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/BF01345265 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The involvement of orexin-1 receptors in modulation of feeding and anxiety-like behavior in rats with complete Freund's adjuvant-induced temporomandibular joint disorder.
Odontology
January 2025
Department of Orofacial Pain and Dysfunction, Academic Centre for Dentistry Amsterdam (ACTA), University of Amsterdam and Vrije Universiteit Amsterdam, Amsterdam, The Netherlands.
Orexin-A (OXA), a neuropeptide produced in the hypothalamus, is recognized for its role in modulating orofacial nociception and regulating feeding behaviors, as well as its impact on psychophysiological responses. This study investigated the role of orexin-1 receptors (OX1R) in modulating nociceptive behaviors induced by noxious stimulation of the temporomandibular joint (TMJ) and the associated changes in mood and feeding behaviors in rats with complete Freund's adjuvant (CFA)-induced temporomandibular disorders (TMDs). Bilateral cannulation of the lateral ventricles was performed in rats.
View Article and Find Full Text PDFSynergistic attenuation of complete freund's adjuvant-induced inflammation in mice using shinbaro-pelubiprofen: a novel therapeutic complex.
Mol Med
January 2025
Jaseng Spine and Joint Research Institute, Jaseng Medical Foundation, Gangnamdae-ro 540, Seoul, 135-896, Republic of Korea.
Background: Inflammation is a critical protective response in the body, essential for combating infections and healing injuries. However, chronic inflammation can be harmful and significantly contribute to the development and progression of chronic diseases, with macrophage-mediated responses being central to these processes. This study presents "SBR-Pel," a new therapeutic blend of Shinbaro tab (SBR), a traditional herbal formula, and pelubiprofen (Pel), a non-steroidal anti-inflammatory drug, and investigated their combined anti-inflammatory effects to create a treatment that both improves efficacy and reduces side effects.
View Article and Find Full Text PDFPPARγ activation attenuates neonatal CRD-induced visceral pain sensitization and anxiety in male rats by alleviating oxidative stress.
BMC Gastroenterol
January 2025
Department of Anesthesiology, First Affiliated Hospital, Fujian Medical University, No. 20, Cha Zhong Road, Fuzhou, Fujian Province, People's Republic of China.
Background: Visceral pain sensitization and emotional reactions due to irritable bowel syndrome (IBS) occur frequently in the general population. Oxidative stress plays a crucial role in the pathogenesis of IBS. Previous studies have demonstrated that activation of peroxisome proliferator-activated receptor gamma (PPARγ) has analgesic effects.
View Article and Find Full Text PDFPostcolitis Alterations in Dose-Dependent Effects of 5-HT1A Agonist Buspirone on Nociceptive Activity of the Raphe Magnus and Dorsal Raphe Neurons in Rats.
Eur J Neurosci
January 2025
Laboratory of Cortico-Visceral Physiology, Pavlov Institute of Physiology of the Russian Academy of Sciences, Saint Petersburg, Russia.
The serotonergic raphe magnus (RMg) and dorsal raphe (DR) nuclei are crucial pain-regulating structures, which nociceptive activity is shown to be altered in gut pathology, but the underlying neuroplastic changes remain unclear. Considering the importance of 5-HT1A receptors in modulating both pain and raphe neuronal activity, in this study, we aimed to determine whether 5-HT1A-dependent visceral and somatic nociceptive processing within the RMg and DR is modified in postcolitis conditions. In anaesthetised male Wistar rats, healthy control and recovered from TNBS-induced colitis, the microelectrode recordings of RMg and DR neuron responses to noxious colorectal distension (CRD) or tail squeezing (TS) were performed prior and after intravenous administration of 5-HT1A agonist, buspirone.
View Article and Find Full Text PDFElectrophisiological monitoring of pain in non-communicative critically ill patients.
Enferm Intensiva (Engl Ed)
January 2025
Grupo de Trabajo de Analgesia, Sedación, Contenciones y Delirio de la Sociedad Española de Enfermería Intensiva y Unidades Coronarias (GT-ASCyD-SEEIUC), Spain; Área del paciente crítico, Reanimación y Anestesia, Hospital Universitario de Girona Dr. Josep Trueta, Girona, Spain; Departamento de Enfermería, Universitat de Girona (UdG), Girona, Spain.
Electrophysiological monitoring of pain provides objective measures that allow for pain control and adjustment of analgesia in non-communicative patients. Among the available electrophysiological devices, automated infrared pupillometry, Analgesia Nociception Index (ANI), and Nociception Level Index (NOL®) stand out. These non-invasive measurement systems analyze the sympathetic or parasympathetic nervous system response to painful stimuli by observing pupillary dilatation and reactivity (pupillometry), heart rate during respiration (ANI), or a combination of multiple parameters from the nociceptive-autonomic medullary circuit (NOL®).
View Article and Find Full Text PDFWant 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!