Antinociceptive activity of Paederosidic Acid Methyl Ester (PAME), a chemical compound isolated from the n-butanol fraction of Paederia scandens, was evaluated in mice using chemical and thermal models of nociception. PAME given by intraperitoneal injection at doses of 20, 40 and 60 mg/kg produced significant inhibitions on chemical nociception induced by intraperitoneal acetic acid, subplantar formalin or capsaicin injections and on thermal nociception in the tail-flick test and the hot plate test. In the pentobarbital sodium-induced sleep time test and the open-field test, PAME neither significantly enhanced the pentobarbital sodium-induced sleep time nor impaired the motor performance, indicating that the observed antinociceptive activity of PAME was unlikely due to sedation or motor abnormality. Core body temperature measurement showed that PAME did not affect temperature within a 2-h period. Moreover, PAME-induced antinociception in the hot plate test was insensitive to naloxone or nimodipine but significantly antagonized by L-NAME (N (G)-nitro-L-arginine methyl ester), methylene blue and glibenclamide. These results suggested that PAME-produced antinociception was possibly related to the pathway of NO-cGMP-ATP sensitive K(+) channels, which merited further studies regarding the precise site and mechanisms of action.
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http://dx.doi.org/10.1016/j.pbb.2009.04.016 | DOI Listing |
Ann Agric Environ Med
December 2024
Department of Experimental Pharmacology, Institute of Rural Health, Lublin, Poland.
Introduction And Objective: The aim of the study was to investigate the effect of bee venom on the activity of two analgesics: ketoprofen (a non-steroidal anti-inflammatory drug) and tramadol (an opioid drug) in the acute thermal pain model (hot-plate test) in mice.
Material And Methods: Linear regression analysis was used to evaluate the dose-response relationship between logarithms of drug doses and their resultant maximum possible anti-nociceptive effects in the mouse hot-plate test. Doses that increased the anti-nociceptive effect by 20% (ED values) for bee venom, ketoprofen and tramadol, and their combination were calculated from linear equations.
ChemMedChem
December 2024
Uniwersytet Jagielloński Collegium Medicum, Department of Medicinal Chemistry, POLAND.
This study aimed to design new hybrid compounds with imidazolidin-2,4-dione and morpholine rings as broad spectrum anticonvulsants. To achieve this goal, all compounds were evaluated in animal seizure models, namely the maximal electroshock (MES), the subcutaneous pentylenetetrazole (scPTZ), and selected in the 6 Hz (32 mA) tests. The most promising compound, 5-isopropyl-3-(morpholinomethyl)-5-phenylimidazolidine-2,4-dione (19), demonstrated broader anticonvulsant activity than phenytoin or levetiracetam, with ED50 of 26.
View Article and Find Full Text PDFArch Razi Inst
June 2024
Department of Pharmacy Practice, Faculty of Pharmacy, University of Sindh, Jamshoro, Pakistan.
Today, the current chemical agents used for the management of pain cause numerous complications. They are associated with the occurrence of disorders in the digestive system, damage to the kidney, or addiction, which has prompted individuals to seek novel drugs that, apart from removing the side effects, are cost-effective and available. The present survey aimed to assess the antinociceptive and anti-inflammatory activity of Korovin methanolic extract (FEME) in male Swiss mice.
View Article and Find Full Text PDFReprod Sci
December 2024
Department of Gynecology and Obstetrics, Division of Reproductive Sciences & Women's Health Re-search, Johns Hopkins Medicine, Baltimore, MD, 21205, USA.
Pomegranate (Punica granatum) is a widely cultivated fruit historically recognized for its health benefits and is regarded as a nutritional powerhouse. Pomegranate has a unique composition of bioactive compounds including hydrolysable tannins, anthocyanins, and other polyphenolic components. Of those, punicalagin and its subsequent metabolites are the most extensively studied, demonstrating antioxidant, anti-inflammatory, anti-cancer, and anti-nociceptive activity.
View Article and Find Full Text PDFEur J Med Chem
December 2024
A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, bld. 1, Moscow, 119334, Russia. Electronic address:
Thevinols and their 3-O-demethylated relatives, orvinols, are derivatives of the Diels-Alder adduct of natural alkaloid thebaine with methyl vinyl ketone. Taken together, thevinols and orvinols constitute an important family of opioid receptor (OR) ligands playing an important role in both the OR mediated antinociception and OR antagonism. Herein, we disclose for the first time the antagonist activity of the N-allyl substituted orvinol derivative fluorinated within the pharmacophore associated with C(20) and its surrounding.
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