Analgesic effects of 1st generation anti-histamines in mice

Mebae Takahashi, Kazuhiro Shima, Masahiro Tsuchiya, Yoshihiro Hagiwara, Hirokazu Mizoguchi, Shinobu Sakurada, Shunji Sugawara, Takuo Fujita, Takeshi Tadano, Makoto Watanabe, Satoshi Fukumoto, Yasuo Endo

研究成果: ジャーナルへの寄稿記事

1 引用 (Scopus)

抄録

Pain is sensed, transmitted, and modified by a variety of mediators and receptors. Histamine is a wellknown mediator of pain. In addition to their anti-histaminic effects, the classical, or 1st generation, anti-histamines (1st AHs) possess, to various degrees, anti-muscarinic, anti-serotonergic, anti-adrenergic, and other pharmacologic effects. Although there have been attempts to use 1st AHs as analgesics and/or analgesic adjuvants, the advent of non-steroidal anti-inflammatory drugs (NSAIDs) discouraged such trials. We previously reported that in patients with temporomandibular disorders, osteoporosis, and/or osteoarthritis, the analgesic effects of certain 1st AHs (chlorpheniramine and diphenhydramine) are superior to those of the NSAIDs flurbiprofen and indomethacin. Here, we compared analgesic effects among 1st AHs and NSAIDs against responses shown by mice to intraperitoneally injected 0.7% acetic acid. Since 1st AHs are water soluble, we selected water-soluble NSAIDs. For direct comparison, drugs were intravenously injected 30 min before the above tests. Histamine-H1-receptor-deficient (H1R-KO) mice were used for evaluating H1-receptor-independent effects. The tested 1st AHs (especially cyproheptadine) displayed or tended to display analgesic effects comparable to those of NSAIDs in normal and H1R-KO mice. Our data suggest that the anti-serotonergic and/or anti-adrenergic effects of 1st AHs make important contributions to their analgesic effects. Moreover, combination of a 1st AH with an NSAID (cyclooxygenase-1 inhibitor) produced remarkably potent analgesic effects. We propose that a 1st AH, by itself or in combination with a cyclooxygenase-1 inhibitor, should undergo testing to evaluate its usefulness in analgesia.

元の言語英語
ページ(範囲)620-624
ページ数5
ジャーナルBiological and Pharmaceutical Bulletin
39
発行部数4
DOI
出版物ステータス出版済み - 4 2016

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Cohort Effect
Histamine
Analgesics
Anti-Inflammatory Agents
Pharmaceutical Preparations
Histamine H1 Receptors
Cyclooxygenase 1
Adrenergic Antagonists
Cyclooxygenase Inhibitors
Chlorpheniramine
Flurbiprofen
Cyproheptadine
Diphenhydramine
Pain
Temporomandibular Joint Disorders
Water
Indomethacin
Acetic Acid
Osteoarthritis
Adrenergic Agents

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science

これを引用

Takahashi, M., Shima, K., Tsuchiya, M., Hagiwara, Y., Mizoguchi, H., Sakurada, S., ... Endo, Y. (2016). Analgesic effects of 1st generation anti-histamines in mice. Biological and Pharmaceutical Bulletin, 39(4), 620-624. https://doi.org/10.1248/bpb.b15-00755

Analgesic effects of 1st generation anti-histamines in mice. / Takahashi, Mebae; Shima, Kazuhiro; Tsuchiya, Masahiro; Hagiwara, Yoshihiro; Mizoguchi, Hirokazu; Sakurada, Shinobu; Sugawara, Shunji; Fujita, Takuo; Tadano, Takeshi; Watanabe, Makoto; Fukumoto, Satoshi; Endo, Yasuo.

:: Biological and Pharmaceutical Bulletin, 巻 39, 番号 4, 04.2016, p. 620-624.

研究成果: ジャーナルへの寄稿記事

Takahashi, M, Shima, K, Tsuchiya, M, Hagiwara, Y, Mizoguchi, H, Sakurada, S, Sugawara, S, Fujita, T, Tadano, T, Watanabe, M, Fukumoto, S & Endo, Y 2016, 'Analgesic effects of 1st generation anti-histamines in mice', Biological and Pharmaceutical Bulletin, 巻. 39, 番号 4, pp. 620-624. https://doi.org/10.1248/bpb.b15-00755
Takahashi M, Shima K, Tsuchiya M, Hagiwara Y, Mizoguchi H, Sakurada S その他. Analgesic effects of 1st generation anti-histamines in mice. Biological and Pharmaceutical Bulletin. 2016 4;39(4):620-624. https://doi.org/10.1248/bpb.b15-00755
Takahashi, Mebae ; Shima, Kazuhiro ; Tsuchiya, Masahiro ; Hagiwara, Yoshihiro ; Mizoguchi, Hirokazu ; Sakurada, Shinobu ; Sugawara, Shunji ; Fujita, Takuo ; Tadano, Takeshi ; Watanabe, Makoto ; Fukumoto, Satoshi ; Endo, Yasuo. / Analgesic effects of 1st generation anti-histamines in mice. :: Biological and Pharmaceutical Bulletin. 2016 ; 巻 39, 番号 4. pp. 620-624.
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