Yamamura Y, Ogawa H, Chihara T, Kondo K, Onogawa T, Nakamura S, Mori T, Tominaga M, Yabuuchi Y
Second Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Japan.
Science. 1991 Apr 26;252(5005):572-4. doi: 10.1126/science.1850553.
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.
已鉴定出一种口服有效的非肽类血管加压素V1受体拮抗剂OPC - 21268。该化合物以竞争性方式选择性拮抗与血管加压素受体V1亚型的结合。在体内，该化合物可作为精氨酸血管加压素（AVP）诱导的血管收缩的特异性拮抗剂。在清醒大鼠口服给药后，该化合物还可拮抗对AVP的升压反应。OPC - 21268可用于研究AVP的生理作用，在治疗高血压和充血性心力衰竭方面可能具有治疗价值。
