Casy A F, Ogungbamila F O
J Pharm Pharmacol. 1985 Feb;37(2):121-3. doi: 10.1111/j.2042-7158.1985.tb05019.x.
The preparation and stereochemical characterization of phenolic analogues of the reversed ester of pethidine, alpha- and beta-prodine and a 1-phenethyl congener are described. All the compounds were weakly active or inactive as agonists in rodent antinociceptive tests and failed to antagonize fentanyl in rats. The results substantiate the view that the morphine and 4-phenylpiperidine groups of analgesics differ in their modes of interaction with opiate receptors, except possibly when the piperidine derivative carries a C-4 carbon substituent.
本文描述了哌替啶反向酯、α-和β-丙哌啶以及一种1-苯乙基同系物的酚类类似物的制备及其立体化学表征。在啮齿动物抗伤害感受试验中，所有这些化合物作为激动剂的活性都很弱或无活性，并且在大鼠中未能拮抗芬太尼。这些结果证实了这样一种观点，即镇痛药的吗啡和4-苯基哌啶基团与阿片受体的相互作用方式不同，可能除了哌啶衍生物带有C-4碳取代基的情况。
