Palluk R, Schilling J C, Stockhaus K, Peil H
Department of Pharmacology, Boehringer Ingelheim KG, Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1993 Jul;348(1):58-64. doi: 10.1007/BF00168537.
The interactions of talipexole (B-HT 920) and clonidine with selective alpha-adrenoceptor antagonists, yohimbine (alpha 2) and prazosin (alpha 1), as well as with dopamine receptor antagonists, metoclopramide (D2), domperidone (D2) and SCH23,390 (D1) were investigated in anaesthetized rabbits after i.v. administration. Both talipexole (0.03-0.1 mg/kg) and clonidine (0.01-0.03 mg/kg) dose-dependently induced hypotension and bradycardia. Talipexole had a shorter duration of action. The hypotensive effect of the alpha 2-adrenoceptor and D2 agonist talipexole (0.03 mg/kg) was antagonized by pretreatment with metoclopramide (3 mg/kg) or domperidone (0.3-3 mg/kg), but not with yohimbine (3 mg/kg), prazosin (0.1 mg/kg) or SCH23,390 (1 mg/kg). Its bradycardic effect was antagonized only by metoclopramide (3 mg/kg). The hypotensive and bradycardic effects of clonidine (0.03 mg/kg) were most effectively antagonized by yohimbine (0.3-3 mg/kg). These findings indicate that in anaesthetized rabbits after i.v. administration, talipexole may lower blood pressure by peripheral, and heart rate by central, dopamine D2 agonism.
静脉注射给药后，在麻醉兔中研究了他利克索（B-HT 920）和可乐定与选择性α-肾上腺素能受体拮抗剂育亨宾（α2）和哌唑嗪（α1）以及多巴胺受体拮抗剂甲氧氯普胺（D2）、多潘立酮（D2）和SCH23,390（D1）的相互作用。他利克索（0.03 - 0.1mg/kg）和可乐定（0.01 - 0.03mg/kg）均剂量依赖性地引起低血压和心动过缓。他利克索的作用持续时间较短。α2-肾上腺素能受体和D2激动剂他利克索（0.03mg/kg）的降压作用可被甲氧氯普胺（3mg/kg）或多潘立酮（0.3 - 3mg/kg）预处理拮抗，但不能被育亨宾（3mg/kg）、哌唑嗪（0.1mg/kg）或SCH23,390（1mg/kg）拮抗。其减慢心率的作用仅被甲氧氯普胺（3mg/kg）拮抗。可乐定（0.03mg/kg）的降压和减慢心率作用最有效地被育亨宾（0.3 - 3mg/kg）拮抗。这些发现表明，静脉注射给药后，在麻醉兔中，他利克索可能通过外周多巴胺D2激动作用降低血压，通过中枢多巴胺D2激动作用降低心率。
