Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid in rat and mouse

T. Kameyama, Toshitaka Nabeshima, S. Yamada, M. Sato

Research output: Contribution to journalArticle

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Abstract

Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid (CN-100) have been investigated pharmacologically in rats and mice. With bradykinin-induced pain responses, CN-100 proved to be the most potent of the commercial nonsteroidal antiinflammatory drugs which were tested in rats: The potency of CN-100 was 4 times stronger than that of indometacin. The analgesic effect of CN-100 on writhing induced by acetic acid, adjuvant-induced hyperalgesia, and carrageenin-induced hyperalgesia, and the effect on AgNO 3 -induced arthralgia were equipotent to or a little weaker than those of indometacin, but stronger than that of diclofenac sodium. In mice, CN-100 was found to be as active as indometacin against peritonitis induced by acetic acid and pain responses induced by mechanical stimulus (pressure). Against the peritonitis induced by acetylcholine and phenylquinone, CN-100 showed inhibitory actions and its potencies were much stronger than those of aminophenazone (aminopyrine) in mice. However, all the drugs tested failed to increase pain thresholds induced by thermal stimulus in rats and mice. CN-100 exerted potent inhibitory effects on carageenin-induced acute inflammatory edema and adjuvant-induced arthritis. The antiinflammatory effect of CN-100 on the former was equal to that of indometacin, but weaker on the latter. The ulcerogenic activity of CN-100 was less potent than that of indometacin. These results indicate that CN-100 may produce its analgesic effects through a peripheral mechanism and be preferable for clinical use, especially for the treatment of inflammatory conditions accompanied by pain.

Original languageEnglish
Pages (from-to)19-26
Number of pages8
JournalArzneimittel-Forschung/Drug Research
Volume37
Issue number1
Publication statusPublished - 01-01-1987
Externally publishedYes

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Thiepins
Analgesics
Anti-Inflammatory Agents
Indomethacin
Aminopyrine
Hyperalgesia
Peritonitis
Pain
Acetic Acid
propionic acid
CN 100
Pain Threshold
Experimental Arthritis
Diclofenac
Carrageenan
Arthralgia
Bradykinin
Pharmaceutical Preparations
Acetylcholine

All Science Journal Classification (ASJC) codes

  • Drug Discovery

Cite this

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abstract = "Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid (CN-100) have been investigated pharmacologically in rats and mice. With bradykinin-induced pain responses, CN-100 proved to be the most potent of the commercial nonsteroidal antiinflammatory drugs which were tested in rats: The potency of CN-100 was 4 times stronger than that of indometacin. The analgesic effect of CN-100 on writhing induced by acetic acid, adjuvant-induced hyperalgesia, and carrageenin-induced hyperalgesia, and the effect on AgNO 3 -induced arthralgia were equipotent to or a little weaker than those of indometacin, but stronger than that of diclofenac sodium. In mice, CN-100 was found to be as active as indometacin against peritonitis induced by acetic acid and pain responses induced by mechanical stimulus (pressure). Against the peritonitis induced by acetylcholine and phenylquinone, CN-100 showed inhibitory actions and its potencies were much stronger than those of aminophenazone (aminopyrine) in mice. However, all the drugs tested failed to increase pain thresholds induced by thermal stimulus in rats and mice. CN-100 exerted potent inhibitory effects on carageenin-induced acute inflammatory edema and adjuvant-induced arthritis. The antiinflammatory effect of CN-100 on the former was equal to that of indometacin, but weaker on the latter. The ulcerogenic activity of CN-100 was less potent than that of indometacin. These results indicate that CN-100 may produce its analgesic effects through a peripheral mechanism and be preferable for clinical use, especially for the treatment of inflammatory conditions accompanied by pain.",
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Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid in rat and mouse. / Kameyama, T.; Nabeshima, Toshitaka; Yamada, S.; Sato, M.

In: Arzneimittel-Forschung/Drug Research, Vol. 37, No. 1, 01.01.1987, p. 19-26.

Research output: Contribution to journalArticle

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