Bateman D N
Br J Clin Pharmacol. 1985 Oct;20(4):339-44. doi: 10.1111/j.1365-2125.1985.tb05074.x.
Three compounds with differing pharmacological properties have been studied with respect to their effects on gastric emptying, BP, pulse rate and sedation in comparison with placebo in three groups of normal male volunteers. BRL 20627 (10 mg i.v.), a benzamide without dopamine antagonist activity, increased gastric emptying rate (t0.5 BRL 20627 8.3 +/- 0.87 min, placebo 13.8 +/- 2.29 min, P less than 0.005). Zetidoline (20 mg orally), a dopamine D2-receptor antagonist had no significant effect on gastric emptying parameters. BK 34/530 (50 and 100 mg orally) a compound with mixed dopamine agonist and alpha-adrenoceptor antagonist activity, impaired gastric adaptive relaxation as measured by the volume 5 min after the drink and at the higher dose delayed gastric emptying (placebo--5 min volume 256 +/- 44.3 ml, t0.5 15.3 +/- 1.32 min: 50 mg BK 34/530-5 min volume 247 +/- 38 ml, t0.5 14.2 +/- 1.94 min: 100 mg BK 34/530-5 min volume 228 +/- 43.7 ml, t0.5 21.1 +/- 3.82 min). All three drugs resulted in small but significant falls in blood pressure, and in the case of BK 34/530 the 100 mg dose caused significant tachycardia. These studies suggest that dopamine antagonist activity is not a prerequisite for 'gastrokinetic' effects in man, and that there is no inhibitory dopaminergic tone on gastric emptying in normal subjects.
在三组正常男性志愿者中，研究了三种具有不同药理特性的化合物与安慰剂相比对胃排空、血压、脉搏率和镇静作用的影响。BRL 20627（静脉注射10毫克），一种无多巴胺拮抗剂活性的苯甲酰胺，可提高胃排空率（BRL 20627的t0.5为8.3±0.87分钟，安慰剂为13.8±2.29分钟，P<0.005）。泽替多林（口服20毫克），一种多巴胺D2受体拮抗剂，对胃排空参数无显著影响。BK 34/530（口服50和100毫克），一种具有多巴胺激动剂和α肾上腺素能受体拮抗剂混合活性的化合物，通过饮用后5分钟的容量测量，损害胃适应性舒张，且高剂量时延迟胃排空（安慰剂——5分钟容量256±44.3毫升，t0.5为15.3±1.32分钟；50毫克BK 34/530——5分钟容量247±38毫升，t0.5为14.2±1.94分钟；100毫克BK 34/530——5分钟容量228±43.7毫升，t0.5为21.1±3.82分钟）。所有三种药物均导致血压小幅但显著下降，就BK 34/530而言，100毫克剂量引起显著心动过速。这些研究表明，多巴胺拮抗剂活性并非人类“胃肠动力”作用的先决条件，且正常受试者胃排空不存在抑制性多巴胺能张力。
