Characterization of the Synergistic Effect between Ligands of Opioid and Free Fatty Acid Receptors in the Mouse Model of Colitis

Autor:	Adam Makaro, Paula Mosińska, Adrian Bartoszek, Radzisław Kordek, Marcin Talar, Julia B. Krajewska, Aleksandra Tarasiuk, Jakub Fichna, Mikołaj Świerczyński, Agata Binienda, Maciej Sałaga, Karolina Niewinna, Katarzyna Dziedziczak, Adam Fabisiak
Rok vydání:	2021
Předmět:	Male colitis Narcotic Antagonists Receptors Opioid mu Pharmaceutical Science Pharmacology Ligands Receptors G-Protein-Coupled Analytical Chemistry Mice chemistry.chemical_compound QD241-441 Opioid receptor Receptors Opioid delta Drug Discovery Receptor chemistry.chemical_classification Mice Inbred BALB C Sulfonamides Aniline Compounds Naloxone DAMGO Drug Synergism Butyrates Chemistry (miscellaneous) Molecular Medicine medicine.drug Agonist medicine.drug_class Thiophenes Article lipids medicine Animals Physical and Theoretical Chemistry Colitis Peroxidase Inflammation Organic Chemistry Antagonist Fatty acid Enkephalin Ala(2)-MePhe(4)-Gly(5) free fatty acid receptors opioid receptor medicine.disease Disease Models Animal Xanthenes chemistry Opioid Receptors Opioid Enkephalin D-Penicillamine (2 5)
Zdroj:	Molecules Volume 26 Issue 22 Molecules, Vol 26, Iss 6827, p 6827 (2021)
ISSN:	1420-3049
Popis:	Background: Recent studies suggest that lipids, including free fatty acids (FFAs), are necessary for proper μ opioid receptor (MOR) binding and that activation of opioid receptors (ORs) improves intestinal inflammation. The objective of the study was to investigate a possible interaction between the ORs and FFA receptors (FFARs) ligands in the colitis. Methods: The potential synergistic effect of ORs and FFARs ligands was evaluated using mouse model of acute colitis induced by dextran sulfate sodium (DSS, 4%). Compounds were injected intraperitoneally (i.p.) once or twice daily at the doses of 0.01 or 0.02 mg/kg body weight (BW) (DAMGO—an MOR agonist), 0.3 mg/kg BW (DPDPE—a δ OR (DOR) agonist) and 1 mg/kg BW (naloxone—a non-selective OR antagonist, GLPG 0974—a FFAR2 antagonist, GSK 137647—a FFAR4 agonist and AH 7614—a FFAR4 antagonist) for 4 days. Results: Myeloperoxidase (MPO) activity was significantly decreased after DAMGO (0.02 mg/kg BW) and GSK 137647 (1 mg/kg BW) administration and co-administration as compared to DSS group. Conclusions: Treatment with ligands of ORs and FFARs may affect the immune cells in the inflammation however, no significant influence on the severity of colitis and no synergistic effect were observed.
Databáze:	OpenAIRE
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