Nuclear medicine program progress report for quarter ending March 31, 1994
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.
- Research Organization:
- Oak Ridge National Lab. (ORNL), Oak Ridge, TN (United States)
- Sponsoring Organization:
- USDOE, Washington, DC (United States)
- DOE Contract Number:
- AC05-84OR21400
- OSTI ID:
- 10151067
- Report Number(s):
- ORNL/TM-12707; ON: DE94011796; TRN: AHC29411%%46
- Resource Relation:
- Other Information: PBD: 1 May 1994
- Country of Publication:
- United States
- Language:
- English
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