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.
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.
Kido
H
H
Research & Development Laboratories, Maruho Co., Ltd., Osaka, Japan.
Murakami
N
N
Ito
A
A
Kimura
K
K
Kodera
N
N
Doi
T
T
Naruse
T
T
D018712:Analgesics, Non-Narcotic / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000633:toxicity; D001169:Arthritis, Experimental / Q000188:drug therapy / Q000209:etiology; D004008:Diclofenac / Q000494:pharmacology; D015232:Dinoprostone / Q000096:biosynthesis; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D004890:Erythema / Q000188:drug therapy / Q000209:etiology; D005334:Fever / Q000188:drug therapy; D005753:Gastric Mucosa / Q000187:drug effects / Q000473:pathology; D006168:Guinea Pigs; D006614:Hindlimb; D006930:Hyperalgesia / Q000139:chemically induced / Q000188:drug therapy; D007213:Indomethacin / Q000494:pharmacology; D007413:Intestinal Mucosa / Q000187:drug effects / Q000473:pathology; D007660:Ketoprofen / Q000494:pharmacology; D008297:Male; D010666:Phenylpropionates / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013045:Species Specificity; D013276:Stomach Ulcer / Q000139:chemically induced; D014466:Ultraviolet Rays
D018712:Analgesics, Non-Narcotic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D010666:Phenylpropionates; D004008:Diclofenac; C104139:2-(4-(3-methyl-2-thienyl)phenyl)propionic acid; D007660:Ketoprofen; D015232:Dinoprostone; D007213:Indomethacin