Piperazine compounds possess anti-infective, anti-carcinogenic, anxiolytic, hypotensive, anti-hypertensive and vasorelaxant properties and are attractive candidates for the development of new analgesic and anti-inflammatory drugs. This study investigates the anti-nociceptive and anti-inflammatory effects of piperazine derivative 4-[(1-phenyl-1H-pyrazol-4-yl) methyl]1-piperazine carboxylic acid ethyl ester (LQFM-008) and the involvement of the serotonergic pathway. In the formalin test, treatments with LQFM-008 (15 and 30mg/kg p.o.) reduced the licking time in both neurogenic and inflammatory phases of this test. In the tail flick and hot plate tests, LQFM008 treatment (15 and 30mg/kg p.o.) increased latency to thermal stimulus, suggesting the involvement of central mechanisms in the anti-nociceptive effect of LQFM-008. In the carrageenan-induced paw edema test, LQFM-008 (p.o.) at the doses of 15 and 30mg/kg reduced the edema at all tested time points, while the dose of 7.5mg/kg reduced the edema only for the first hour. LQFM-008 (30mg/kg p.o.) reduced both cell migration and protein exudation in the carrageenan-induced pleurisy test. Furthermore, pre-treatment with NAN-190 (0.6mg/kgi.p.) and PCPA (100mg/kgi.p.) antagonized the anti-nociceptive effect of LQFM-008 in both phases of the formalin test. Our data suggest that LQFM-008 possesses anti-inflammatory and anti-nociceptive effects mediated through the serotonergic pathway.
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http://dx.doi.org/10.1016/j.pbb.2015.08.008 | DOI Listing |
Curr Drug Metab
December 2024
Department of Pharmacy, the Fourth Hospital of Hebei Medical University, Hebei Key Laboratory of Clinical Pharmacy, Shijiazhuang, China.
Objective: Tacrolimus, a calcineurin inhibitor (CNI), is the first-line treatment for chronic myeloid leukemia (CML) and advanced gastrointestinal stromal tumors (GIST). Imatinib and tacrolimus are both substrates of the hepatic enzymes CYP3A4/5 and efflux transporter P-gp, so drug-drug interactions may occur during their co-administration treatment. Therefore, this study aimed to evaluate the pharmacokinetic interaction between imatinib and tacrolimus in rats.
View Article and Find Full Text PDFPLoS One
October 2024
Department of Neurology, Biomedical Research Institute, Seoul National University Hospital, Seoul, South Korea.
The gut microbiome influences neurological disorders through bidirectional communication between the gut and the brain, i.e., the gut-brain axis.
View Article and Find Full Text PDFJ Pak Med Assoc
October 2024
Department of Pharmacology and Toxicology, Mustansiriyah University, Baghdad- Iraq.
Objective: To evaluate the potential protective effect of metformin against osteoarthritis development in rats.
Methods: The experimental study was conducted at the Iraqi Centre for Cancer Research and Medical Genetics, Mustansiriyah University, Baghdad, Iraq, from December 2021 to February 2022, and comprised male Sprague- Dawley mice who were divided into 5 equal groups: negative control group, osteoarthritis group subjected to monoiodoacetate induction, positive control group treated with celecoxib 30mg/kg, metformin 100mg/kg group, and metformin 200mg/kg group. Body mass index, inflammatory biomarkers, and serum C-terminal cross-linked telopeptide of type II collagen levels were noted for all the animals.
PLoS One
September 2024
Department of Biochemistry, College of Science, King Saud University, Riyadh, Saudi Arabia.
Minerva Anestesiol
May 2024
Department of Anesthesia and Intensive Care, Assiut University Hospital, Assiut, Egypt.
Background: We assessed the efficiency of intravenous adjuvants in decreasing opioid intake and pain scores after spine fusion surgery.
Methods: This study included 120 patients aged 18-60 listed for spine fusion surgery under general anesthesia. Patients were randomly assigned to four groups: Group (Lidocaine): received IV lidocaine 4 mg/kg in 50 mL volume over 30 min.
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