Hatanaka S, Kawarabayashi K, Iseri M, Tsubokura K, Furuhama K
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Life Sci. 1995;56(19):PL377-82. doi: 10.1016/0024-3205(95)00133-q.
The present study was designed to clarify the potential of DQ-2511 (3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]carbamoyl]methyl] amino-N-methylbenzamide: ecabapide) as a gastroprokinetic agent in spontaneously hypertensive rats (SHR). The gastric emptying of SHR was clearly retarded relative to that of weight-matched normotensive Wistar-Kyoto (WKY) rats when evaluated by the acetaminophen (APAP) method with the semi-solid test meal. There was, however, no significant difference between both strains in gastric mucosal blood flow (GMBF) determined by means of a laser doppler flowmetry. A 2-week treatment of SHR with DQ-2511 (1 mg/kg, oral) stimulated gastric emptying without affecting body weight gain or indirect systolic blood pressure (SBP), whereas cisapride (3 and 10 mg/kg, oral) had no effect under the same conditions. The pharmacological characteristics of DQ-2511 as a gastroprokinetic agent are discussed on the basis of these results.
本研究旨在阐明DQ - 2511(3 - [[[2 - (3,4 - 二甲氧基苯基)乙基]氨基甲酰基]氨基甲酰基]甲基]氨基 - N - 甲基苯甲酰胺:依卡必利)作为一种促胃动力剂在自发性高血压大鼠(SHR)中的潜力。当用对乙酰氨基酚(APAP)法和半固体试验餐评估时,SHR的胃排空相对于体重匹配的正常血压Wistar - Kyoto(WKY)大鼠明显延迟。然而,通过激光多普勒血流仪测定的胃黏膜血流量(GMBF)在这两种品系之间没有显著差异。用DQ - 2511(1 mg/kg,口服)对SHR进行为期2周的治疗可刺激胃排空,而不影响体重增加或间接收缩压(SBP),而在相同条件下西沙必利(3和10 mg/kg,口服)则没有效果。基于这些结果,对DQ - 2511作为促胃动力剂的药理学特性进行了讨论。