pelubiprofen and Inflammation

Although drugs such as acetaminophen, opioids, and nonsteroidal anti-inflammatory drugs (NSAIDs), are commonly used for pain management, the side effects of these drugs such as hepatotoxicity, nephrotoxicity, nausea, and vomiting, can not be neglected. Therefore, combinations of analgesics with different mechanisms raise the possibility of developing novel analgesics. Therefore, the aim of the present study was to evaluate whether DW-1021, the ionic complex of pelubiprofen (NSAID) and tramadol (opioid), has synergic antinociceptive and anti-inflammatory effects in nociceptive as well as inflammation-induced nociceptive models compared to pelubiprofen- or tramadol-only administration. Strong synergistic antinociceptive efficacy of DW-1021 was observed in the mouse writhing test and von Frey paw withdrawal threshold test in the carrageenan-induced rats. The hot plate test in mice and the Randall-Selitto mechanical paw pressure test in carrageenan-induced rats revealed that DW-1021 had a preferable effect on relieving pain to pelubiprofen, but not as much as tramadol. In the carrageenan-induced rats, DW-1021 had a more potent effect on reducing paw inflammation (paw volume, width, and thickness) via the suppression of PGE

Topics: Analgesics; Analgesics, Opioid; Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Inflammation; Mice; Pain; Rats; Rodentia; Tramadol

The immunomodulatory properties of RS-2131, 2-[4-(2-oxocyclohexylidenemethyl)phenyl]propionic acid, were studied using normal and autoimmune mice. RS-2131 suppressed the Arthus-type footpad reaction in BALB/c mice when administered orally at the time of immunization with sheep red blood cells, in contrast to indomethacin. This drug also suppressed the direct plaque-forming cell response against sheep erythrocytes in BALB/c mice. Under the same experimental conditions, the percentage ratio of Lyt 2+ cells to Thy 1.2+ cells were increased in the spleen cells. When used in non-immunized normal BALB/c mice, however, RS-2131 produced no effect on the ratio of Lyt 2+ cells to Thy 1.2+ cells in the spleen cells and on the percent distribution of T lymphocyte subsets. In MRL/Mp-lpr/lpr (MRL/lpr) mice, which have been known as a model of autoimmune disease, Lyt 2 cells in the thymus and the lymph node increased on oral treatment with RS-2131. These findings suggest that this drug may induce suppressor T cells only when the immune response in host animals is increased and then results in inhibition of immune responses in mice.

Topics: Adjuvants, Immunologic; Animals; Anti-Inflammatory Agents, Non-Steroidal; Female; Hemolytic Plaque Technique; Indomethacin; Inflammation; Mice; Mice, Inbred BALB C; Phenylpropionates; Spleen; T-Lymphocytes

[(Cycloalkylmethyl)phenyl]acetic acid derivatives and related compounds were synthesized to test their antiinflammatory and analgesic activities. Some of the compounds in this series were found to have good activity in the carrageenan edema test. Among them, sodium 2-[4-[(2-oxocyclopentyl)methyl] phenyl]propionate dihydrate (15) and 2-[4-[(2-oxocyclohexylidene)methyl]phenyl]propionic acid (13b) showed potent analgesic and antiadjuvant arthritis activities with excellent antipyretic properties.

Topics: Analgesics; Animals; Chemical Phenomena; Chemistry; Female; Fever; Ibuprofen; Indomethacin; Inflammation; Male; Phenylacetates; Phenylpropionates; Rats; Rats, Inbred Lew; Rats, Inbred Strains; Structure-Activity Relationship