This paper describes the antinociceptive effects of tetrahydrophthalimides and related compounds in mice. Twenty compounds were obtained by the reaction of cis-1,2,3,6-tetrahydrophthalic anhydride with appropriate amines, dehydration, and addition to the imidic double bond. They were analyzed in the writhing test at 10 mg/kg given intraperitoneally. The most active compound 2-benzyl-5-morpholin-4-yl-hexahydroisoindole-1,3-dione (19) was studied on formalin, capsaicin, glutamate and hot plate models. The antinociceptive activity demonstrated by some studied compounds is promising, and some of them were more active than acetylsalicylic acid and paracetamol used as reference drugs in writhing tests in mice. Compound 19 was about 5-fold more potent than the reference drugs, being also effective by oral route and against the inflammatory response in the formalin test. The results suggest that compound 19 could be used as a model to obtain new and more potent antinociceptive agents. It exhibits an interesting antinociceptive profile, and does not interact with opioid systems.
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http://dx.doi.org/10.1515/znc-2007-3-408 | DOI Listing |
Eur J Pharmacol
January 2025
Laboratory of Pharmacology of Pain, Department of Pharmacology, Federal University of Paraná, Curitiba, PR, Brazil.
Neuropathy is the most common complication of diabetes, leading to painful symptoms like hyperalgesia. Current treatments for diabetic painful neuropathy often prove inadequate, necessitating the exploration of new pharmacological approaches. Therefore, this study aimed to investigate the potential antinociceptive effect of aspirin-triggered lipoxin A4 (ATL), a specialized pro-resolving lipid mediator, when administered alone or in combination with cannabinoid agonists, to alleviate diabetic neuropathic pain.
View Article and Find Full Text PDFComb Chem High Throughput Screen
January 2025
KIPS, Shri Shankaracharya Professional University, Bhilai, Chhattisgarh, India.
The discovery of novel counteractive pharmaceuticals, which have recently generated much interest, has played a significant role in the development of drugs derived from herbal medicines or botanical sources. Paederia foetida (P. foetida) is one such example of a role in both traditional and traditional medicine.
View Article and Find Full Text PDFPharmacol Res
January 2025
University Hospital of Jena, Institute of Physiology 1, D-07740 Jena, Germany. Electronic address:
Musculoskeletal pain has a high prevalence of transition to chronic pain and/or persistence as chronic pain for years or even a lifetime. Possible mechanisms for the development of such pain states are often reflected in inflammatory or neuropathic processes involving, among others, cytokines and other molecules. Since biologics such as blockers of TNF or IL-6 can attenuate inflammation and pain in a subset of patients with rheumatoid arthritis, the question arises to what extent cytokines are involved in the generation of pain in human musculoskeletal diseases.
View Article and Find Full Text PDFRSC Med Chem
November 2024
Department of Drug and Health Sciences, University of Catania Viale A. Doria 6 95125 Catania Italy (+39) 095 7384273.
Inflammatory pain represents one of the unmet clinical needs for patients, as conventional therapies cause several side effects. Recently, new targets involved in inflammatory pain modulation have been identified, including the sigma-1 receptor (σ1R). Selective σ1R antagonists have demonstrated analgesic efficacy in acute and chronic inflammatory pain models.
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
Laboratory of Pharmacology and Molecular Chemistry, Department of Chemical Biology, Regional University of Cariri (URCA), Rua Coronel Antônio Luis 1161, Pimenta, Crato 63105-000, Ceará, Brazil.
This study evaluated the antinociceptive effect of the L. bark extract (HEXA) and its primary component, caffeic acid (CA), through in vivo assays. : The antinociceptive properties were assessed using abdominal writhing, hot plate, and Von Frey tests.
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