Petrillo P, Amato M, Tavani A
Neuropeptides. 1985 Feb;5(4-6):403-6. doi: 10.1016/0143-4179(85)90039-3.
The (+) and (-) isomers of tifluadom were assessed in rats for their opioid activities. In vitro (+)-tifluadom was almost equipotent at mu- and kappa- sites and about 10 times less potent at delta-sites: (-)-tifluadom had the same binding spectrum but was 10-20 times less potent. In vivo (+)-tifluadom delayed the hot-plate reaction time; this effect was antagonized by naloxone, but not by Ro 15-1788. (-)-Tifluadom up to 20 mg/kg had no antinociceptive effect. In the intestinal transit test analgesic doses of (+)-tifluadom did not delay the intestinal transit of a charcoal meal in rats and had weak antagonist activity against morphine-induced inhibition of intestinal transit, whereas (-)-tifluadom had neither agonist nor antagonist effect. It thus appears that (+)-and (-)-tifluadom are not selective in vitro and in vivo for one type of opioid binding site/receptor.
对替氟杜姆的（+）和（-）异构体在大鼠中进行了阿片样物质活性评估。体外实验中，（+）-替氟杜姆在μ和κ位点的活性几乎相当，在δ位点的活性约低10倍；（-）-替氟杜姆具有相同的结合谱，但活性低10至20倍。体内实验中，（+）-替氟杜姆延长了热板反应时间；此效应可被纳洛酮拮抗，但不能被Ro 15 - 1788拮抗。高达20mg/kg的（-）-替氟杜姆没有镇痛作用。在肠道转运试验中，镇痛剂量的（+）-替氟杜姆不会延迟大鼠炭末餐的肠道转运，并且对吗啡诱导的肠道转运抑制具有微弱的拮抗活性，而（-）-替氟杜姆既没有激动作用也没有拮抗作用。因此，（+）-和（-）-替氟杜姆在体外和体内对一种类型的阿片样物质结合位点/受体都没有选择性。
