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阿尼利定、哌替啶及其他N-取代苯基哌啶羧酸酯的放射免疫分析

Radioimmunoassay for anileridine, meperidine and other N-substituted phenylpiperidine carboxylic acid esters.

作者信息

Van Vunakis H, Freeman D S, Gjika H B

出版信息

Res Commun Chem Pathol Pharmacol. 1975 Oct;12(2):379-87.

PMID:1242820
Abstract

Antibodies that bind an 125I-tyramyl derivative of N-succinylanileridine have been produced in animals immunized with N-succinylanileridine-hemocyanin conjugate. Several congeners and metabolites have been tested as competitors of this antigen-antibody reaction. The concentrations (in picomoles) required for 50% inhibition have been found to be: anileridine (0.2), meperidine (3.5), piminodine (3.8), diphenoxylate (20.5), normeperidine (20.0), meperidine acid (45,000) and anileridine acid (3,400). Although ester hydrolysis results in changes in inhibiting capacities on the order of 10(4), major structural changes in the substituent on the nitrogen of the piperidine ring are not readily recognized by the antibody. This radioimmunoassay can be used to study a variety of N-substituted phenylpiperidine carboxylic acid esters by relating the results to the standard curve obtained for the drug under investigation. For all practical purposes, alphaprodine, morphine and methadone do not interfere with the assay.

摘要

用N-琥珀酰苯胺红蛋白结合物免疫动物后,产生了能与N-琥珀酰苯胺的125I-酪氨酰衍生物结合的抗体。已对几种同系物和代谢物作为这种抗原-抗体反应的竞争剂进行了测试。发现50%抑制所需的浓度(皮摩尔)为:苯胺利定(0.2)、哌替啶(3.5)、匹米诺定(3.8)、地芬诺酯(20.5)、去甲哌替啶(20.0)、哌替啶酸(45,000)和苯胺利定酸(3,400)。虽然酯水解导致抑制能力发生约10⁴ 量级的变化,但哌啶环氮原子上取代基的主要结构变化不易被抗体识别。通过将结果与所研究药物的标准曲线相关联,这种放射免疫测定法可用于研究各种N-取代苯基哌啶羧酸酯。实际上,阿法罗定、吗啡和美沙酮不干扰该测定。

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