双甲脒及其代谢产物对肠道蠕动的影响。

Effect of amitraz and its metabolites on intestinal motility.

Pass M A, Mogg T D

Department of Physiology and Pharmacology, University of Queensland, St Luciá, Australia.

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1991;99(1-2):169-72. doi: 10.1016/0742-8413(91)90095-b.

Abstract

Amitraz was rapidly metabolised to BTS27271 after intravenous administration to sheep. 2. Amitraz and BTS27271 had significant H1-histamine antagonist activity on isolated guinea-pig ileum. BTS27271 was approximately 3.3 times as potent as amitraz. 3. Intravenous injection of amitraz and its metabolite BTS27271 caused an immediate cessation of caecal motility in sheep, which persisted for 74-245 min. 4. Caecal stasis induced by amitraz was reversed by yohimbine but only partially reversed by 2-pyridylethylamine. 5. The results suggest that despite the significant antihistamine activity of amitraz and BTS27271 in vitro, it is probably the alpha-2-adrenergic agonist activity that is the most important in causing large intestinal stasis in vivo.

摘要

对绵羊静脉注射双甲脒后，其迅速代谢为BTS27271。2. 双甲脒和BTS27271对离体豚鼠回肠具有显著的H1组胺拮抗剂活性。BTS27271的效力约为双甲脒的3.3倍。3. 静脉注射双甲脒及其代谢产物BTS27271可使绵羊盲肠运动立即停止，持续74 - 245分钟。4. 育亨宾可逆转双甲脒诱导的盲肠淤滞，但2 - 吡啶乙胺只能部分逆转。5. 结果表明，尽管双甲脒和BTS27271在体外具有显著的抗组胺活性，但在体内导致大肠淤滞的最重要因素可能是α-2-肾上腺素能激动剂活性。