Analgesic activity of 3-mono-substituted derivatives of dihydrofuran-2-one in experimental rodent models of pain.
Three derivatives of dihydrofuran-2-one (L-PP, L-PP1, and L-SAL) were administered by intraperitoneal injection and their analgesic activity was assayed in several models of pain. The activity of these derivatives were tested using a hot plate test, a writhing test, capsaicin- and glutamate-induced nociception, along with two models of local anesthesia, including a test for infiltration anesthesia in guinea pigs and the modified tail immersion test in mice. The results of these in vivo experiments show that these three derivatives of dihydrofuran-2-one possess analgesic activity in rodents. The ED(50) values of the tested compounds are lower or comparable to the ED(50) values of reference compounds (acetylsalicylic acid or morphine). For the most active derivative of dihydrofuran-2-one, L-PP1 (3-[4-(3-trifluoromethylphenyl)-piperazin-1-yl]-dihydrofuran-2-one dihydrochloride), the ED(50) value was: 1.34 mg/kg, 0.79 mg/kg, 2.01 mg/kg and 3.99 mg/kg in the hot plate, writhing, capsaicin- and glutamate-induced pain tests, respectively.
Sałat
Kinga
K
Department of Pharmacodynamics, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Kraków, Poland. salat.kinga@gmail.com
Filipek
Barbara
B
Wieckowski
Krzysztof
K
Malawska
Barbara
B
D015107:4-Butyrolactone / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D000700:Analgesics / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001241:Aspirin / Q000008:administration & dosage / Q000494:pharmacology; D001549:Benzamides / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005663:Furans / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D006168:Guinea Pigs; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D009020:Morphine / Q000008:administration & dosage / Q000494:pharmacology; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D010879:Piperazines / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology
C547282:3-(4-(3-trifluoromethylphenyl)piperazin-1-yl)dihydrofuran-2-one; D000700:Analgesics; D001549:Benzamides; D005663:Furans; D010879:Piperazines; D009020:Morphine; D015107:4-Butyrolactone; D001241:Aspirin