Nasello A G, Gidali D, de Sá-Rocha L C, Felicio L F
School of Veterinary Medicine, University of São Paulo, Brazil.
Life Sci. 1995;56(3):151-6. doi: 10.1016/0024-3205(94)00429-v.
Bromopride (BRO) and domperidone (DOMP) are dopamine D2 blocking agents used in gastroenterology clinics because of their anti emetic effect as well as their central and peripheral actions of increasing gastrointestinal motor activity. The rationale for these experiments was to compare BRO- and DOMP-effects on plasma, brain, and intestinal cholinesterase activity in vitro. BRO and DOMP effects on cholinesterase activity in plasma, striatum, duodenum and ileum of adult male rats were measured for drug concentrations ranging from 0.006 to 3.134 microM for BRO and from 0.006 to 125 microM for DOMP. The results demonstrate that both BRO and DOMP can inhibit cholinesterase activity in all tissues studied, with DOMP being more potent than BRO in plasma and intestinal tissues. These data suggest the existence of a cholinergic mechanism of action for these dopamine blocking agents.
溴必利(BRO)和多潘立酮(DOMP)是多巴胺D2受体阻断剂,因其具有止吐作用以及增加胃肠运动活性的中枢和外周作用,而被用于胃肠病学诊所。这些实验的目的是比较BRO和DOMP在体外对血浆、脑和肠道胆碱酯酶活性的影响。测量了BRO浓度范围为0.006至3.134微摩尔/升、DOMP浓度范围为0.006至125微摩尔/升时,BRO和DOMP对成年雄性大鼠血浆、纹状体、十二指肠和回肠中胆碱酯酶活性的影响。结果表明,BRO和DOMP均可抑制所有研究组织中的胆碱酯酶活性,在血浆和肠道组织中DOMP比BRO更有效。这些数据表明这些多巴胺阻断剂存在胆碱能作用机制。