OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist
| Autor: | Toshiyuki Onogawa, Yoshitaka Yamamura, Kazumi Kondo, Toyoki Mori, Michiaki Tominaga, Shigeki Nakamura, Youichi Yabuuchi, Hidenori Ogawa, Tomihiko Chihara |
|---|---|
| Rok vydání: | 1991 |
| Předmět: |
Vasopressin
medicine.medical_specialty Receptors Vasopressin Time Factors Arginine Administration Oral Blood Pressure Pharmacology Quinolones Kidney Binding Competitive Norepinephrine Piperidines Arginine vasopressin receptor 2 Internal medicine medicine Animals Vasopressin receptor Arginine vasopressin receptor 1B Multidisciplinary Receptors Angiotensin business.industry Angiotensin II Cell Membrane Antagonist Rats Arginine Vasopressin stomatognathic diseases Kinetics Endocrinology nervous system Liver Competitive antagonist medicine.symptom business hormones hormone substitutes and hormone antagonists Vasoconstriction |
| Zdroj: | Science (New York, N.Y.). 252(5005) |
| ISSN: | 0036-8075 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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