Radio-ligand receptor binding assay <italic style="font-style: italic">in vitro</italic> and animal biodistribution <italic style="font-style: italic">in vivo</italic> of 99Tcm-N-ethyl-N2S2-memantine as a potential NMDA receptor imaging agent

Yingtao LIU; Xingqin ZHOU; Guoxian CAO; Jiankang ZHANG; Xiaofeng QIN; Xijie XU; Meifen ZOU

doi:10.13538/j.1001-8042/nst.21.171-176

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Radio-ligand receptor binding assay in vitro and animal biodistribution in vivo of ⁹⁹Tc^m-N-ethyl-N₂S₂-memantine as a potential NMDA receptor imaging agent

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE | Updated：2021-01-29

- Radio-ligand receptor binding assay in vitro and animal biodistribution in vivo of ⁹⁹Tc^m-N-ethyl-N₂S₂-memantine as a potential NMDA receptor imaging agent
- Nuclear Science and Techniques Vol. 21, Issue 3, (2010)
- Affiliations：
  
  1.Jiangnan University, School of Medicine and Pharmaceutics, Wuxi 214122, China
  2.Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
- Author bio：
  
  Corresponding author. E-mail address: jswxcgx@126.com
- Funds：
- DOI：10.13538/j.1001-8042/nst.21.171-176
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Yingtao LIU, Xingqin ZHOU, Guoxian CAO, et al. Radio-ligand receptor binding assay in vitro and animal biodistribution in vivo of ⁹⁹Tc^m-N-ethyl-N₂S₂-memantine as a potential NMDA receptor imaging agent. [J]. Nuclear Science and Techniques 21(3):171-176(2010)
DOI：

Yingtao LIU, Xingqin ZHOU, Guoxian CAO, et al. Radio-ligand receptor binding assay in vitro and animal biodistribution in vivo of ⁹⁹Tc^m-N-ethyl-N₂S₂-memantine as a potential NMDA receptor imaging agent. [J]. Nuclear Science and Techniques 21(3):171-176(2010) DOI： 10.13538/j.1001-8042/nst.21.171-176.

摘要

Abstract

The pharmacologic characteristics of ,99,Tc,m,-N-ethyl-N,2,S,2,-memantine, an NMDA receptor imaging agent, was investigated. It was prepared by a one-step reaction from N-ethyl-N,2,S,2,-memantine. The affinity and specificity were determined by radio-ligand receptor binding assay (RRA). Biodistribution ,in vivo, in mice was performed. The results showed that ,99,Tc,m,-N-ethyl-N,2,S,2,-memantine bound to a single site on NMDA receptor with a ,K,d, of 584.32 nmol/L and a ,B,max, of 267.05 nmol/mg. A competitive analysis showed that such specific binding could be inhibited by specific inhibitors of NMDA receptor, such as ketamine and (+)-MK-801. The biodistribution exhibited rapid uptake and favorable retention in mice brains. The major radioactivity was metabolized by the hepatic system. A two-compartment model of ,C, = 4.49,e,–0.083,t, + 1.42,e,–0.0016,t, was established, and the half life was 8.35 min in blood. In conclusion, the new radio-ligand ,99,Tc,m,-N-ethyl-N,2,S,2,-Memantine has a moderate affinity and specific binding to NMDA receptor, and can easily cross the blood-brain barrier (BBB). Therefore, it may be a potential NMDA receptor imaging agent.

关键词

Keywords

99Tcm-N-ethyl-N2S2-memantineNMDA receptorRadio-ligand receptor binding assayBiodistributionimaging

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Research Center for Nuclear Medicine, Shariati Hospital, Tehran University of Medical Sciences

Department of Chemistry, University of Zanjan

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Radio-ligand receptor binding assay in vitro and animal biodistribution in vivo of 99Tcm-N-ethyl-N2S2-memantine as a potential NMDA receptor imaging agent

DOI：10.13538/j.1001-8042/nst.21.171-176

摘要

Abstract

关键词

Keywords

references

Radio-ligand receptor binding assay in vitro and animal biodistribution in vivo of ⁹⁹Tc^m-N-ethyl-N₂S₂-memantine as a potential NMDA receptor imaging agent