薬物受容体研究の新動向　セロトニン（５‐ＨＴ）３受容体：　きっ抗薬と消化器領域における薬理作用

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書誌事項

タイトル別名
  • Serotonin (5-HT)3 receptors: Antagonists and their pharmacological profiles.
  • セロトニン 5-HT 3 ジュヨウタイ キッコウヤク ト ショウカキ リョウイ
  • 薬物受容体研究の新動向

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説明

The pharmacology of 5-HT and the classification of 5-HT receptors have become increasingly complex. However, recent advances have produced a new nomenclature system for 5-HT receptors. 5-HT3 receptors are neuronal receptors coupled directly to cation channels. Recently, many selective 5-HT3-receptor antagonists including tropisetron, zacopride, ondansetron, granisetron, zatosetron, nazasetron, YM060 and YM114 (KAE-393) have been developed. Many actions attributable to the 5-HT3-receptor have been described in both the peripheral and central nervous systems, and clinical trials are already showing the potential use of these 5-HT3 receptor antagonists in a number of disorders of the gastrointestinal tract and central nervous system, such as nausea and vomiting induced by cancer chemotherapy, anxiety, depression, schizophrenia and migraine. In addition, endogenous 5-HT is suggested to be one of the substances that mediate stress-induced responses in gastrointestinal function, i.e., increase in fecal pellet output and diarrhea. Moreover, YM060, YM114 (KAE-393) and granisetron have been reported to inhibit restraint stress and 5-HT-induced increases in fecal pellet output and diarrhea in rats and mice, indicating that endogenous 5-HT may mediate stress-induced changes in bowel function through the 5-HT3 receptor. Therefore, 5-HT3-receptor antagonists are new therapeutic drugs for stress-induced gastrointestinal dysfunctions like irritable bowel syndrome (IBS).

収録刊行物

  • 日本薬理学雑誌

    日本薬理学雑誌 104 (3), 143-152, 1994

    公益社団法人 日本薬理学会

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