Ogawa H, Yamamura Y, Miyamoto H, Kondo K, Yamashita H, Nakaya K, Chihara T, Mori T, Tominaga M, Yabuuchi Y
Second Institute of New Drug Research, Otsuka Pharmaceutical Co., Tokushima, Japan.
J Med Chem. 1993 Jul 9;36(14):2011-7. doi: 10.1021/jm00066a010.
A series of compounds has been synthesized and demonstrated to be antagonists of V1 receptors both in vitro and in vivo. These compounds are structurally related to the 1-(4-piperidyl)-2(1H)-quinolinones, including OPC-21268, an orally bioavailable AVP V1 antagonist with high V1 specificity. It has been found that the introduction of an acetamide group on the terminal alkoxy chain of 41-44 leads to an increase in oral activity. Certain of these compounds may have efficacy in the study of AVP V1 receptors.
已合成了一系列化合物，并证明它们在体外和体内均为V1受体拮抗剂。这些化合物在结构上与1-(4-哌啶基)-2(1H)-喹啉酮有关，包括OPC-21268，一种具有高V1特异性的口服生物可利用的AVP V1拮抗剂。已发现，在41-44的末端烷氧基链上引入乙酰胺基团会导致口服活性增加。其中某些化合物可能在AVP V1受体研究中具有疗效。
