論文 - 詳細
RRC ID | 18177 |
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著者 | Akasaka Y, Sakai A, Takasu K, Tsukahara M, Hatta A, Suzuki H, Inoue H. |
タイトル | Suppressive effects of glycyrrhetinic acid derivatives on tachykinin receptor activation and hyperalgesia. |
ジャーナル | J Pharmacol Sci |
Abstract |
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 [Ca(2+)](i) induced by substance P, neurokinin A, and neurokinin B in CHO-K1 cells expressing the human NK(1), NK(2), and NK(3) 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. |
巻・号 | 117(3) |
ページ | 180-8 |
公開日 | 2011-1-1 |
DOI | 10.1254/jphs.11116fp |
PII | JST.JSTAGE/jphs/11116FP |
PMID | 22032861 |
MeSH | Analgesics / therapeutic use* Animals CHO Cells Calcium / metabolism Capsaicin Cricetinae Disease Models, Animal Formaldehyde Glycyrrhetinic Acid / analogs & derivatives Glycyrrhetinic Acid / therapeutic use* Hot Temperature Humans Hyperalgesia / drug therapy* Inflammation / chemically induced Inflammation / drug therapy* Ligation Male Neuralgia / drug therapy Neuralgia / etiology Neurokinin A / pharmacology Neurokinin B / pharmacology Pain / chemically induced Pain / drug therapy* Rats Rats, Sprague-Dawley Receptors, Tachykinin / antagonists & inhibitors* Sciatic Nerve / surgery Substance P / pharmacology |
IF | 2.835 |
引用数 | 4 |
WOS 分野 | PHARMACOLOGY & PHARMACY |
リソース情報 | |
ヒト・動物細胞 | CHO-K1(RCB0285) |