5-羟色胺3受体拮抗剂[11C]Y-25130和[11C]YM060的合成。

Synthesis of 5-HT3 receptor antagonists, [11C]Y-25130 and [11C]YM060.

作者信息

Ishiwata K, Ishii K, Ishii S, Senda M

机构信息

Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Japan.

出版信息

Appl Radiat Isot. 1995 Sep;46(9):907-10. doi: 10.1016/0969-8043(95)00147-6.

DOI:10.1016/0969-8043(95)00147-6

PMID:7581293

Abstract

Two high-affinity 5-HT3 receptor ligands, Y-25130 and YM 060, have been labeled with 11C for use in PET studies to measure 5-HT3 receptors. The [11C]Y-25130 was prepared by N-methylation of nor-Y-25130-BH3 complex with [11C]CH3I in the presence of K2CO3 followed by HCl hydrolysis. Likewise, N-methylation of nor-YM060 gave [11C]YM060. After HPLC separation, the decay-corrected radiochemical yield of the two 11C-labeled ligands was 34-40% based on [11C]CH3I, the specific activity was 10-12 GBq/mumol at 35-40 min from EOB, and the radiochemical and chemical purities were > 99%. In mice, the brain uptake of the two compounds was the lowest among the tissues investigated, but the level of the brain radioactivity increased with time.

摘要

两种高亲和力的5-羟色胺3（5-HT3）受体配体Y-25130和YM 060已用11C进行标记，用于正电子发射断层扫描（PET）研究以测量5-HT3受体。[11C]Y-25130是通过在碳酸钾存在下用[11C]CH3I对去甲Y-25130-BH3络合物进行N-甲基化，随后进行盐酸水解来制备的。同样，对去甲YM060进行N-甲基化得到[11C]YM060。经过高效液相色谱（HPLC）分离后，基于[11C]CH3I，两种11C标记配体的衰变校正放射化学产率为34-40%，从给药结束（EOB）起35-40分钟时的比活度为10-12 GBq/μmol，放射化学纯度和化学纯度均>99%。在小鼠中，在所研究的组织中，这两种化合物的脑摄取量最低，但脑放射性水平随时间增加。