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

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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 ... continued below

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14 p.

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Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Lambert, C. R.; McPherson, D. W.; Mirzadeh, S. et al. May 1, 1994.

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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.

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14 p.

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OSTI as DE94011796; Paper copy available at OSTI: phone, 865-576-8401, or email, reports@adonis.osti.gov

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  • Other Information: PBD: 1 May 1994

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  • Other: DE94011796
  • Report No.: ORNL/TM--12707
  • Grant Number: AC05-84OR21400
  • DOI: 10.2172/10151067 | External Link
  • Office of Scientific & Technical Information Report Number: 10151067
  • Archival Resource Key: ark:/67531/metadc1313353

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  • May 1, 1994

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  • Nov. 3, 2018, 11:47 a.m.

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  • Nov. 14, 2018, 4:15 p.m.

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Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Lambert, C. R.; McPherson, D. W.; Mirzadeh, S. et al. Nuclear medicine program progress report for quarter ending March 31, 1994, report, May 1, 1994; Tennessee. (digital.library.unt.edu/ark:/67531/metadc1313353/: accessed December 10, 2018), University of North Texas Libraries, Digital Library, digital.library.unt.edu; crediting UNT Libraries Government Documents Department.