Kawashima Y, Ikemoto T, Horiguchi A, Hayashi M, Matsumoto K, Kawarasaki K, Yamazaki R, Okuyama S, Hatayama K
Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
J Med Chem. 1993 Apr 2;36(7):815-9. doi: 10.1021/jm00059a004.
A series of (nitrooxy)alkyl apovincaminates has been synthesized and evaluated for their effects on vertebral and femoral blood flow. These derivatives were prepared from apovincaminic acid (4). In cerebral circulation, compound 5 (0.03-1.0 mg/kg iv) caused a dose-dependent increase in cerebral blood flow (CerBF) without affecting the blood pressure. It was more potent than vinpocetine (2). The structures of 2 and 5, determined by X-ray crystallography, showed differences in the electrostatic potential image and in the conformation of the ethyl group at the 16-position.
已合成了一系列（硝氧基）烷基阿朴长春胺酸盐，并评估了它们对椎骨和股血流的影响。这些衍生物由阿朴长春胺酸（4）制备而成。在脑循环中，化合物5（静脉注射0.03 - 1.0毫克/千克）可使脑血流量（CerBF）呈剂量依赖性增加，且不影响血压。它比长春西汀（2）更有效。通过X射线晶体学确定的2和5的结构显示，在静电势图像和16位乙基的构象上存在差异。
