Inhibition of the Angiotensin II Type 1 Receptor by TCV-116: Quantitation by In Vitro Autoradiography.
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- Song Keifu
- Department of Pharmacology, Osaka Medical College
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- Kanehara Hironori
- Department of Pharmacology, Osaka Medical College
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- Takai Shinji
- Department of Pharmacology, Osaka Medical College
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- Shiota Naotaka
- Department of Pharmacology, Osaka Medical College
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- Wada Takeo
- Pharmaceutical Research Division, Takeda Chemical Industry Co., Ltd.
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- Inada Yoshiyuki
- Pharmaceutical Research Division, Takeda Chemical Industry Co., Ltd.
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- Miyazaki Mizuo
- Department of Pharmacology, Osaka Medical College
書誌事項
- タイトル別名
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- Inhibition of the Angiotensin 2 Type 1 Receptor by TCV-116 Quantitation by In Vitro Autoradiography
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抄録
Inhibition of angiotensin (Ang) II type 1 (AT1) receptors in various target tissues of adult Sprague-Dawley rats was studied after single oral administration of TCV-116. The effects of TCV-116 on Ang II-receptor binding were assessed by quantitative in vitro autoradiography using 125I-[Sar1, Ile8]Ang II as a ligand. Four hours after the administration of TCV-116 (1 mg/kg), Ang II-receptor binding was mark- edly inhibited in the kidney (20% of control), adrenal cortex (27%), thoracic aorta (57%), heart (55%) and testis (76%) where AT1 receptors predominate. In the brain, orally administered TCV-116 produced a significant inhibition of binding both to the circumventricular organs (38%), which are devoid of the bloodbrain barrier (BBB), and to the discrete regions within the BBB such as the paraventricular hypothalamic nucleus (48%), nucleus of the solitary tract (60%). Twenty-four hours after the administration, Ang IIreceptor binding had partly recovered to approximately 50 - 85% of control levels. In contrast, throughout the experimental period, Ang II-receptor binding was little affected in sites where Ang II type 2 (AT2) receptors predominate such as the adrenal medulla and the nucleus of the inferior olive. These data indicate that orally administered TCV-116 specifically binds to AT1 receptors both in peripheral tissues and the central nervous system.
収録刊行物
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- Jpn.J.Pharmacol.
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Jpn.J.Pharmacol. 79 (2), 131-139, 1999
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390282679261316352
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- NII論文ID
- 10008682107
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- NII書誌ID
- AA00691188
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- COI
- 1:CAS:528:DyaK1MXhsFyksbk%3D
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- ISSN
- 13473506
- 00215198
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- NDL書誌ID
- 4663065
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- PubMed
- 10202848
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- Web Site
- https://ndlsearch.ndl.go.jp/books/R000000004-I4663065
- https://api.elsevier.com/content/article/PII:S0021519819309631?httpAccept=text/xml
- https://api.elsevier.com/content/article/PII:S0021519819309631?httpAccept=text/plain
- https://www.jstage.jst.go.jp/article/jjp/79/2/79_2_131/_pdf
- https://search.jamas.or.jp/link/ui/1999156499
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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- PubMed
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