FLUPHENAZINE, ICS 205-930 AND DL-FENFLURAMINE DIFFERENTIALLY ANTAGONIZE DRUG-INDUCED EMESIS IN THE FERRET

FLUPHENAZINE, ICS 205-930 AND DL-FENFLURAMINE DIFFERENTIALLY ANTAGONIZE DRUG-INDUCED EMESIS IN THE FERRET
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DOI:
10.1016/0028-3908(90)90167-p
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发表时间:
1990-05-01
期刊:
影响因子:
4.7
通讯作者:
TATTERSALL, FD
TATTERSALL, FD
中科院分区:
医学2区
文献类型:
--
作者:
COSTALL, B;DOMENEY, AM;TATTERSALL, FD

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静脉注射顺铂(10 mg/kg)、皮下注射阿朴吗啡(0.125 - 1 mg/kg)和麦角乙脲(0.001- 0.1mg/kg)、口服吐根(0.3- 2.4mg/kg)和灌胃硫酸铜(25-100 mg/kg)可引起雪貂的呕吐和干呕反应。用dl-芬氟拉明(5 mg/kg i. p.)预防或减少由顺铂、阿扑吗啡、吐根和麦角脲引起的呕吐,但不能显著拮抗硫酸铜引起的呕吐。5-HT 3受体拮抗剂ICS 205-930(0.1mg/kg i. p.)预防由顺铂和吐根引起的呕吐,但不能预防或显著减少由阿扑吗啡、麦角乙脲或硫酸铜引起的呕吐。多巴胺受体拮抗剂,包括氟奋乃静(0.1 - 1.0 mg/kg,腹膜内),预防阿扑吗啡和麦角乙脲诱导的呕吐,但拮抗顺铂或吐根诱导的呕吐的效力较低或具有不一致的作用,并且不能抑制硫酸铜诱导的呕吐。这些数据表明,多巴胺和/或5-HT 3受体系统参与药物诱导的呕吐,但硫酸铜引起的胃刺激引起的呕吐是由不同的受体机制介导的。
The intravenous injection of cisplatin (10 mg/kg), the subcutaneous injection of apomorphine (0,125-I mg/kg) and lisuride (0.001-0.1 mg/kg), the oral administration of ipecacuanha (0.3-2.4 mg/kg) and the intragastric administration of copper sulphate (25-100 mg/kg), induced a vomiting and retching response in the ferret. Pretreatment with dl-fenfluramine (5 mg/kg i.p.) prevented or reduced the emesis induced by cisplatin, apomorphine, ipecacuanha and lisuride but failed to significantly antagonise copper sulphate-induced emesis. The 5-HT3 receptor antagonist ICS 205-930 (0.1 mg/kg i.p.) prevented emesis induced by cisplatin and ipecauanha but failed to prevent or significantly reduced the emesis induced by apomorphine, lisuride or copper sulphate. Dopamine receptor antagonists, including fluphenazine (0.1 - 1.0 mg/kg i.p.), prevented apomorphine- and lisuride-induced emesis but were less potent or had inconsistent actions to antagonise cisplatin- or ipecacuanha-induced emesis and failed to inhibit the emesis induced by copper sulphate. The data indicate that dopamine and/or 5-HT3 receptor systems are involved in drug-induced emesis but the emesis caused by gastric irritation induced by copper sulphate is mediated by different receptors mechanisms.