Vilhardt H, Lundin S
J Endocrinol. 1987 Mar;112(3):439-42. doi: 10.1677/joe.0.1120439.
Using implanted minipumps it was shown over a period of 7 days that the vasopressin antagonist, 1-deamino-pentamethylene-2-D-Phe-4-Ile-arginine vasopressin, caused increased diuresis in normal rats and reversed vasopressin- or oxytocin-induced antidiuresis in Brattleboro rats. When the antagonist was infused alone in Brattleboro rats it induced a marked antidiuretic response, indicating that the analogue also possessed agonistic properties. The agonist action could not be demonstrated in anaesthetized, hydrated normal rats. In these animals the analogue behaved as a pure antagonist. It is concluded that analogues which behave as antagonists in one test model may display agonistic properties under different experimental conditions.
通过植入微型泵在7天的时间里观察到，血管加压素拮抗剂1-脱氨基-五亚甲基-2-D-苯丙氨酸-4-异亮氨酸-精氨酸血管加压素可使正常大鼠的尿量增加，并逆转Brattleboro大鼠中血管加压素或催产素诱导的抗利尿作用。当单独向Brattleboro大鼠输注该拮抗剂时，会诱导出明显的抗利尿反应，这表明该类似物也具有激动剂特性。在麻醉、水合的正常大鼠中未表现出激动剂作用。在这些动物中，该类似物表现为纯粹的拮抗剂。结论是，在一种测试模型中表现为拮抗剂的类似物在不同的实验条件下可能显示出激动剂特性。
