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Radioiodination of central nerves system dopamine D2 receptor imaging agent. IBZM preparation and preclinical study

Journal Article:

Abstract

To study preparation of central nerves system dopamine D2 imaging agent {sup 131}I-IBZM and its preclinical investigation, peracetic acid was used as the oxidant for preparing radioiodinated {sup 125}I-IBZM and {sup 131}I-IBZM, D2 binding properties of IBZM were examined by in vitro binding saturation analysis, rat whole body and regional brain biodistribution, rat brain autoradiography and rabbit SPECT static imaging, etc. The results are: 1. The radiolabelling yields of {sup 125}I-IBZM and {sup 131}I-IBZM were 84.18% +- 3.06% and 78.50% +- 3.47%. The radiochemical purity were over 95% after being isolated by HPLC; and were over 90% after being isolated by organic extraction. 2. Scatchard plot of D2 receptor saturation binding analysis showed: K{sub d} = 0.53 +- 0.06 nmol/L, B{sub max} = 466.45 +- 45.88 fmol/mg protein. 3. The rat brain autoradiography and analysis showed that there was high {sup 125}I-IBZM uptake in striatal area 2 hr after injection, the striatal/cerebellum ratio was 6.22 +- 0.48; the high {sup 125}-IBZM uptake can be blocked by haloperidol--a special dopamine D2 receptor antagonist. 4. {sup 131}I-IBZM rat biodistribution and rabbit SPECT planar imaging showed good initial brain uptake and retention, the initial uptake of rat brain was 1.893 +- 0.147% ID/g  More>>
Authors:
Yansong, Lin; Xiangtong, Lin; Mingyang, Hu; Shangren, Pan; Bocheng, Wang [1] 
  1. Huashan Hospital of Shanghai Medical Univ., Shanghai (China)
Publication Date:
Nov 01, 1996
Product Type:
Journal Article
Reference Number:
SCA: 400703; PA: AIX-28:044736; EDB-97:092727; SN: 97001814013
Resource Relation:
Journal Name: Chinese Journal of Nuclear Medicine (Zhonghua Heyixue Zazhi); Journal Volume: 16; Journal Issue: 4; Other Information: PBD: Nov 1996
Subject:
40 CHEMISTRY; CONTRAST MEDIA; HYDROXYL RADICALS; LABELLED COMPOUNDS; DOPAMINE; RECEPTORS; CENTRAL NERVOUS SYSTEM; IMAGES; IODINE 131; LABELLING; METHOXY RADICALS; RADIOISOTOPE SCANNING; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
OSTI ID:
493749
Country of Origin:
China
Language:
Chinese
Other Identifying Numbers:
Journal ID: CITCDE; ISSN 0253-9780; TRN: CN9701244044736
Submitting Site:
INIS
Size:
pp. 240-243
Announcement Date:

Journal Article:

Citation Formats

Yansong, Lin, Xiangtong, Lin, Mingyang, Hu, Shangren, Pan, and Bocheng, Wang. Radioiodination of central nerves system dopamine D2 receptor imaging agent. IBZM preparation and preclinical study. China: N. p., 1996. Web.
Yansong, Lin, Xiangtong, Lin, Mingyang, Hu, Shangren, Pan, & Bocheng, Wang. Radioiodination of central nerves system dopamine D2 receptor imaging agent. IBZM preparation and preclinical study. China.
Yansong, Lin, Xiangtong, Lin, Mingyang, Hu, Shangren, Pan, and Bocheng, Wang. 1996. "Radioiodination of central nerves system dopamine D2 receptor imaging agent. IBZM preparation and preclinical study." China.
@misc{etde_493749,
title = {Radioiodination of central nerves system dopamine D2 receptor imaging agent. IBZM preparation and preclinical study}
author = {Yansong, Lin, Xiangtong, Lin, Mingyang, Hu, Shangren, Pan, and Bocheng, Wang}
abstractNote = {To study preparation of central nerves system dopamine D2 imaging agent {sup 131}I-IBZM and its preclinical investigation, peracetic acid was used as the oxidant for preparing radioiodinated {sup 125}I-IBZM and {sup 131}I-IBZM, D2 binding properties of IBZM were examined by in vitro binding saturation analysis, rat whole body and regional brain biodistribution, rat brain autoradiography and rabbit SPECT static imaging, etc. The results are: 1. The radiolabelling yields of {sup 125}I-IBZM and {sup 131}I-IBZM were 84.18% +- 3.06% and 78.50% +- 3.47%. The radiochemical purity were over 95% after being isolated by HPLC; and were over 90% after being isolated by organic extraction. 2. Scatchard plot of D2 receptor saturation binding analysis showed: K{sub d} = 0.53 +- 0.06 nmol/L, B{sub max} = 466.45 +- 45.88 fmol/mg protein. 3. The rat brain autoradiography and analysis showed that there was high {sup 125}I-IBZM uptake in striatal area 2 hr after injection, the striatal/cerebellum ratio was 6.22 +- 0.48; the high {sup 125}-IBZM uptake can be blocked by haloperidol--a special dopamine D2 receptor antagonist. 4. {sup 131}I-IBZM rat biodistribution and rabbit SPECT planar imaging showed good initial brain uptake and retention, the initial uptake of rat brain was 1.893 +- 0.147% ID/g at 2 min and 1.044 +- 0.135% ID/g at 60 min. The results showed that the radioiodinated IBZM had high affinity, saturation and specificity to rat`s and rabbit`s central nerves system dopamine D2 receptors.}
journal = {Chinese Journal of Nuclear Medicine (Zhonghua Heyixue Zazhi)}
issue = {4}
volume = {16}
journal type = {AC}
place = {China}
year = {1996}
month = {Nov}
}