Alburges M E, Hanson G R, Gibb J W, Sakashita C O, Rollins D E
Department of Pharmacology and Toxicology, University of Utah, Salt Lake City 84112.
J Anal Toxicol. 1991 Nov-Dec;15(6):311-8. doi: 10.1093/jat/15.6.311.
Radioreceptor binding assays may be useful methods for determining the plasma and urine concentration of drugs. We have evaluated the possibility of employing CNS receptors in an assay to measure fentanyl and fentanyl-like drugs. This in vitro assay is based on the competition of these drugs with [3H]fentanyl for opioid receptors in membrane preparations of rat forebrain. The binding is stereospecific, reversible, and saturable. Scatchard plots of saturation suggest the presence of high and low affinity binding sites. Naloxonazine, which selectively binds to mu 1-opioid site, competed with [3H]fentanyl for its high affinity binding site. Morphine and hydromorphone competed with [3H]fentanyl for the opioid receptor, but other morphine-like compounds were relatively weak displacers of [3H]fentanyl. Many other commonly abused drugs did not displace [3H]fentanyl from the opiod receptors. Urine samples from animals injected with fentanyl were evaluated by other analytical techniques, including radioimmunoassay (RIA) and gas chromatography/mass spectrometry (GC/MS), and results were compared to those from the radioreceptor assay. Urinary analysis of fentanyl showed a good correlation between all three methods.
放射受体结合测定法可能是测定药物血浆和尿液浓度的有用方法。我们评估了在一种测定法中利用中枢神经系统受体来测量芬太尼及类芬太尼药物的可能性。这种体外测定法基于这些药物与[3H]芬太尼在大鼠前脑膜制剂中对阿片受体的竞争。该结合具有立体特异性、可逆性和饱和性。饱和的Scatchard图表明存在高亲和力和低亲和力结合位点。选择性结合μ1阿片位点的纳洛酮嗪与[3H]芬太尼竞争其高亲和力结合位点。吗啡和氢吗啡酮与[3H]芬太尼竞争阿片受体，但其他类吗啡化合物对[3H]芬太尼的置换作用相对较弱。许多其他常用的滥用药物不会从阿片受体上置换[3H]芬太尼。通过包括放射免疫测定法（RIA）和气相色谱/质谱联用（GC/MS）在内的其他分析技术对注射了芬太尼的动物的尿液样本进行了评估，并将结果与放射受体测定法的结果进行了比较。芬太尼的尿液分析显示这三种方法之间具有良好的相关性。
