Anti-inflammatory, analgesic and anti-pyretic effects of d-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid (M-5011), a new non-steroidal anti-inflammatory drug, in rats and guinea pigs.

Abstract

Anti-inflammatory, analgesic and anti-pyretic effects of d-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid (M-5011), a new non-steroidal anti-inflammatory drug (NSAID), were compared with those of indomethacin, diclofenac sodium and ketoprofen in rats and guinea pigs. Anti-inflammatory effect of M-5011 on ultraviolet-induced erythema in guinea pigs was 11.7 and 1.8 times more potent than that of indomethacin and ketoprofen, respectively. Inhibitory effect of M-5011 on carrageenin-induced paw edema was 2 and 1.5 times more potent than that of indomethacin and diclofenac sodium, respectively. Analgesic effect of M-5011 on dry yeast-induced hyperalgesia or adjuvant-induced arthritic pain was equipotent to that of indomethacin, diclofenac sodium or ketoprofen. Anti-pyretic effect of M-5011 on yeast-induced pyrexia in rats was 4.2 and 4.6 times more potent than that of indomethacin and ketoprofen, respectively. Inhibitory effect of M-5011 on prostaglandin E2 production in the exudate of air-pouch inflammation induced by carrageenin was 1.75 times more potent than that in the non-inflamed site (stomach). As a result, gastric ulcerogenic activity of M-5011 was half that of indomethacin in rat. These results suggest that M-5011 shows more potent anti-inflammatory and anti-pyretic effects and equipotent analgesic effect with low gastro-ulcerogenic activity compared with classical NSAIDs.

• Authors: H Kido, N Murakami, A Ito, K Kimura, N Kodera, T Doi, T Naruse
• Journal: Japanese journal of pharmacology (Jpn J Pharmacol) Vol. 76 Issue 1 Pg. 75-86 (Jan 1998) ISSN: 0021-5198 [Print] Japan
• PMID: 9517407 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Analgesics, Non-Narcotic
• Anti-Inflammatory Agents, Non-Steroidal
• Phenylpropionates
• Diclofenac
• 2-(4-(3-methyl-2-thienyl)phenyl)propionic acid
• Ketoprofen
• Dinoprostone
• Indomethacin

Topics

• Analgesics, Non-Narcotic (pharmacology, toxicity)
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (pharmacology, toxicity)
• Arthritis, Experimental (drug therapy, etiology)
• Diclofenac (pharmacology)
• Dinoprostone (biosynthesis)
• Edema (chemically induced, drug therapy)
• Erythema (drug therapy, etiology)
• Fever (drug therapy)
• Gastric Mucosa (drug effects, pathology)
• Guinea Pigs
• Hindlimb
• Hyperalgesia (chemically induced, drug therapy)
• Indomethacin (pharmacology)
• Intestinal Mucosa (drug effects, pathology)
• Ketoprofen (pharmacology)
• Male
• Phenylpropionates (pharmacology, toxicity)
• Rats
• Species Specificity
• Stomach Ulcer (chemically induced)
• Ultraviolet Rays