OPC-21268, an Orally Effective, Nonpeptide Vasopressin V1 Receptor Antagonist

• Yoshitaka Yamamura

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Hidenori Ogawa

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Tomihiko Chihara

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Kazumi Kondo

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Toshiyuki Onogawa

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Shigeki Nakamura

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Toyoki Mori

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Michiaki Tominaga

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

• Youichi Yabuuchi

  Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., 463-10 Kagasuno Kawauchi- cho Tokushima 771-01, Japan.

抄録

An orally effective, nonpeptide, vasopressin V1 receptor antagonist, OPC-21268, has been identified. This compound selectively antagonized binding to the V1 subtype of the vasopressin receptor in a competitive manner. In vivo, the compound acted as a specific antagonist of arginine vasopressin (AVP)-induced vasoconstriction. After oral administration in conscious rats, the compound also antagonized pressor responses to AVP. OPC-21268 can be used to study the physiological role of AVP and may be therapeutically useful in the treatment of hypertension and congestive heart failure.

収録刊行物

• Science

  Science 252 (5005), 572-574, 1991-04-26

  American Association for the Advancement of Science (AAAS)

キーワード

• Multidisciplinary

詳細情報

• CRID: 1363107371214110976
• NII論文ID: 80005853855
• DOI: 10.1126/science.1850553
• ISSN: 10959203
• ISSN: 00368075
• ISSN: http://id.crossref.org/issn/00368075
• Web Site: https://www.science.org/doi/pdf/10.1126/science.1850553
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