Serotonin (5-HT)3 receptors: Antagonists and their pharmacological profiles.
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- MIYATA Keiji
- Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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- HONDA Kazuo
- Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
Bibliographic Information
- Other Title
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- 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
- 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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Description
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).
Journal
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- Folia Pharmacologica Japonica
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Folia Pharmacologica Japonica 104 (3), 143-152, 1994
The Japanese Pharmacological Society
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Keywords
Details 詳細情報について
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- CRID
- 1390001204270993536
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- NII Article ID
- 130000759704
- 10008732530
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- NII Book ID
- AN00198335
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- ISSN
- 13478397
- 00155691
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- NDL BIB ID
- 3898572
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- PubMed
- 7959407
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- Text Lang
- ja
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed