Suppressive Effects of Glycyrrhetinic Acid Derivatives on Tachykinin Receptor Activation and Hyperalgesia
スポンサーリンク
概要
- 論文の詳細を見る
Glycyrrhetinic acid (GA), an aglycone of glycyrrhizin, isolated from the licorice root (Glycyrrhizia), and its semi-synthetic derivatives have a wide range of pharmacological effects. To investigate whether GA derivatives may be used as a new class of analgesics, we examined the effects of these compounds on human tachykinin receptors expressed in CHO-K1 cells. Among the GA derivatives examined, the disodium salt of olean-11,13(18)-dien-3β,30-O-dihemiphthalate inhibited the mobilization of [Ca2+]i induced by substance P, neurokinin A, and neurokinin B in CHO-K1 cells expressing the human NK1, NK2, and NK3 tachykinin receptors, respectively. In an inflammatory pain model, Compound 5 suppressed the capsaicin-induced flinching behavior in a dose-dependent manner. Compound 5 was also effective in suppressing pain-related behaviors in the late phase of the formalin test and reducing thermal hyperalgesia in the neuropathic pain state caused by sciatic nerve injury. Collectively, Compound 5 may be an analgesic candidate via tachykinin receptor antagonism.
- 2011-11-20
著者
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Tsukahara Michiko
Research Laboratory Minophagen Pharmaceutical Co. Ltd.
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Inoue Hideo
Research Laboratory Minophagen Pharmaceutical Co. Ltd.
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Suzuki Hidenori
Department Of Pharmacology Nippon Medical School
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Sakai Atsushi
Department Of Biochemistry Faculty Of Veterinary Medicine Hokkaido University
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Sakai Atsushi
Department Of Pharmacology Nippon Medical School
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Inoue Hideo
Research Laboratory Minophagen Pharmaceutical Co.
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Akasaka Yuko
Research Laboratory, Minophagen Pharmaceutical Co., Ltd., Japan
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Takasu Kumiko
Department of Pharmacology, Nippon Medical School, Japan
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Suzuki Hidenori
Department Of Cardiovascular Research The Tokyo Metropolitan Institute Of Medical Science
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Hatta Akira
Research Laboratory Minophagen Pharmaceutical Co. Ltd.
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Akasaka Yuko
Research Laboratory Minophagen Pharmaceutical Co. Ltd.
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Takasu Kumiko
Department Of Pharmacology Nippon Medical School
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Suzuki Hidenori
Department of Applied Physics, Tokyo University of Science, 1-3 Kagurazaka, Shinjuku-ku, Tokyo 162-8601
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INOUE Hideo
Research Laboratory, Minophagen Pharmaceutical Co., Ltd.
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