Wainer B H, Wung W E, Hill J H, Fitch F W, Fried J, Rothberg R M
J Pharmacol Exp Ther. 1976 Apr;197(1):163-70.
Meperidinic acid was converted to O-meperidinyl-glycollic acid and covalently attached to bovine serum albumin. Rabbits injected with this conjugate produced antibodies reactive with meperidine which were measured by the ammonium sulfate method. The specificities of these antisera were studied by competitive inhibition of the binding of 100 pmol/ml of 3H-meperidine to antibody by the prior addition of increasing concentrations of various unlabeled compounds. The concentrations in nanomoles per milliliter of various unlabeled opiods required to inhibit 3H-meperidine binding by 50% (I50) were: meperidine, 0.08; O-meperidinyl-glycollic acid, 1.7; methadone, 580; heroin, 1750; codeine, 2600; and morphine, 4200. Several psychopharmacologically active compounds were found to have I50 values comparable to the nonmeperidine opioids: hydroxyzine. HCl, 460; propoxyphene, 4,500; diazepam, 6,500; and cocaine, 10,800. The metabolites of meperidine exhibited the following I50 values: normeperidine, 0.7; meperidinic acid and normeperidinic acid, 210. A radioimmunoassay for meperidine which employs this antiserum was shown to be approximately 100 times more sensitive than the spectrophotometric method of Burns et al. (J. Pharmacol. Exp Ther. 114: 289-293, 1955). In this assay only normeperidine and some of the meperidine congeners might be expected to interfere with the measurement of meperidine. The degree of normeperidine interference was shown to be comparable to that present in the existing assay method.
哌替啶酸被转化为O-哌替啶基乙醇酸，并与牛血清白蛋白共价结合。给兔子注射这种结合物后产生了与哌替啶反应的抗体，通过硫酸铵法进行测定。通过预先加入浓度不断增加的各种未标记化合物来竞争性抑制100 pmol/ml的3H-哌替啶与抗体的结合，研究了这些抗血清的特异性。抑制3H-哌替啶结合50%（I50）所需的各种未标记阿片类药物的浓度（以每毫升纳摩尔计）分别为：哌替啶，0.08；O-哌替啶基乙醇酸，1.7；美沙酮，580；海洛因，1750；可待因，2600；吗啡，4200。发现几种具有精神药理学活性的化合物的I50值与非哌替啶类阿片类药物相当：盐酸羟嗪，460；丙氧芬，4500；地西泮，6500；可卡因，10800。哌替啶的代谢产物表现出以下I50值：去甲哌替啶，0.7；哌替啶酸和去甲哌替啶酸，210。使用这种抗血清的哌替啶放射免疫测定法显示比Burns等人（《药理学与实验治疗学杂志》114：289 - 293，1955年）的分光光度法灵敏度高约100倍。在该测定法中，预计只有去甲哌替啶和一些哌替啶同系物可能会干扰哌替啶的测量。去甲哌替啶的干扰程度与现有测定方法中的相当。
