Wang R F, Tafani J A, Francés B, Bergon M, Coulais Y, Zajac J M, Guiraud R
Department of Nuclear Medicine, First Hospital, Beijing Medical University, People's Republic of China.
Nucl Med Biol. 1997 Aug;24(6):553-8. doi: 10.1016/s0969-8051(97)00068-1.
A new iodinated diprenorphine analog, [125I]7 alpha-O-iodoallyl diprenorphine ([125I]7 alpha-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (Ki = 0.4 +/- 0.2 nM) and 63% of specific binding by in vitro and in vivo binding studies. Inhibition curves indicated that this tracer labeled with the same affinities to three opioid receptors (mu = delta = kappa). The findings demonstrate that this proposed compound appears to be potential radioprobe for future study of opioid receptors by in vivo SPECT.
通过碘脱锡反应制备并表征了一种新的碘化二丙诺啡类似物，即[125I]7α-O-碘烯丙基二丙诺啡（[125I]7α-O-IA-DPN）。作为一种阿片类拮抗剂，通过体外和体内结合研究表明，该药物显示出非常高的亲和力（Ki = 0.4±0.2 nM）和63%的特异性结合。抑制曲线表明，这种示踪剂对三种阿片受体（μ = δ = κ）具有相同的亲和力。研究结果表明，这种拟议的化合物似乎是未来通过体内单光子发射计算机断层扫描（SPECT）研究阿片受体的潜在放射性探针。
