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Title: Nuclear medicine program progress report for quarter ending March 31, 1994

Abstract

The authors` new radioiodinated ``IQNP`` agent, an analogue of ``4-IQNB``, has a high affinity for the muscarinic-cholinergic receptor (m-AChR). Iodine is stabilized in ``IQNP`` by attachment as a vinyl iodide. To evaluate the potential usefulness of a [Br-76]-labeled analogue as a candidate for positron emission tomography (PET), they have synthesized the trans-3-bromopropenyl analogue (BrQNP) and evaluated its ability in vivo to block uptake of [I-125]-Z-(R,R)-IQNP. Reaction of bromine with the trans-tributylstannyl substrate prepared from ethyl -{alpha}-hydroxy -{alpha}-phenyl-{alpha}-(1-propyn-3-yl)acetate, followed by column purification and transesterification with (R,S)-3-quinuclidinol gave BrQNP. Female rats were pre-treated with the oxalate salt of BrQNP one hour prior to I.V. injection of [I-125]-IQNP. While the brain and heart uptake in BrQNP pre-treated animals was significantly decreased, the control animals showed the expected high uptake of IQNP in these tissues. The ease of preparation and ability to block m-AChR suggest that [Br-76]-labeled BrQNP is a potential candidate for PET studies. In this report, the authors also summarize their current on-going collaborative studies assessing the usefulness of various rhenium-188-labeled therapeutic agents. In addition, collaborative programs have been established to evaluate rhenium-188-labeled particles for treatment of arthritis (synovectomy), treatment of bone pain resulting from cancer metastheses with rhenium-188-phosphonates (palliation), and othermore » applications.« less

Authors:
; ; ; ; ; ;
Publication Date:
Research Org.:
Oak Ridge National Lab., TN (United States)
Sponsoring Org.:
USDOE, Washington, DC (United States)
OSTI Identifier:
10151067
Report Number(s):
ORNL/TM-12707
ON: DE94011796; TRN: AHC29411%%46
DOE Contract Number:  
AC05-84OR21400
Resource Type:
Technical Report
Resource Relation:
Other Information: PBD: 1 May 1994
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; NUCLEAR MEDICINE; RESEARCH PROGRAMS; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; UPTAKE; PROGRESS REPORT; THERAPEUTIC USES; RADIOIMMUNOTHERAPY; DIAGNOSTIC USES; 550601; 550604; UNSEALED RADIONUCLIDES IN DIAGNOSTICS; UNSEALED RADIONUCLIDES IN THERAPY

Citation Formats

Knapp, Jr, F F, Ambrose, K R, Beets, A L, Lambert, C R, McPherson, D W, Mirzadeh, S, and Luo, H. Nuclear medicine program progress report for quarter ending March 31, 1994. United States: N. p., 1994. Web. doi:10.2172/10151067.
Knapp, Jr, F F, Ambrose, K R, Beets, A L, Lambert, C R, McPherson, D W, Mirzadeh, S, & Luo, H. Nuclear medicine program progress report for quarter ending March 31, 1994. United States. doi:10.2172/10151067.
Knapp, Jr, F F, Ambrose, K R, Beets, A L, Lambert, C R, McPherson, D W, Mirzadeh, S, and Luo, H. Sun . "Nuclear medicine program progress report for quarter ending March 31, 1994". United States. doi:10.2172/10151067. https://www.osti.gov/servlets/purl/10151067.
@article{osti_10151067,
title = {Nuclear medicine program progress report for quarter ending March 31, 1994},
author = {Knapp, Jr, F F and Ambrose, K R and Beets, A L and Lambert, C R and McPherson, D W and Mirzadeh, S and Luo, H},
abstractNote = {The authors` new radioiodinated ``IQNP`` agent, an analogue of ``4-IQNB``, has a high affinity for the muscarinic-cholinergic receptor (m-AChR). Iodine is stabilized in ``IQNP`` by attachment as a vinyl iodide. To evaluate the potential usefulness of a [Br-76]-labeled analogue as a candidate for positron emission tomography (PET), they have synthesized the trans-3-bromopropenyl analogue (BrQNP) and evaluated its ability in vivo to block uptake of [I-125]-Z-(R,R)-IQNP. Reaction of bromine with the trans-tributylstannyl substrate prepared from ethyl -{alpha}-hydroxy -{alpha}-phenyl-{alpha}-(1-propyn-3-yl)acetate, followed by column purification and transesterification with (R,S)-3-quinuclidinol gave BrQNP. Female rats were pre-treated with the oxalate salt of BrQNP one hour prior to I.V. injection of [I-125]-IQNP. While the brain and heart uptake in BrQNP pre-treated animals was significantly decreased, the control animals showed the expected high uptake of IQNP in these tissues. The ease of preparation and ability to block m-AChR suggest that [Br-76]-labeled BrQNP is a potential candidate for PET studies. In this report, the authors also summarize their current on-going collaborative studies assessing the usefulness of various rhenium-188-labeled therapeutic agents. In addition, collaborative programs have been established to evaluate rhenium-188-labeled particles for treatment of arthritis (synovectomy), treatment of bone pain resulting from cancer metastheses with rhenium-188-phosphonates (palliation), and other applications.},
doi = {10.2172/10151067},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1994},
month = {5}
}