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In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent.

In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Research Abstract Details 

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  • In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Abstract Text:

    nasima akhterNasima Akhter,kazuhiro shibaKazuhiro Shiba,kazuma ogawaKazuma Ogawa,seigo kinuyaSeigo Kinuya,kenichi nakajimaKenichi Nakajima,hirofumi moriHirofumi Mori,

    In this study, the (+)-enantiomer of radioiodinated 2-[4-(4-iodophenyl)piperidino]cyclohexanol [(+)-[(125)I]-p-iodovesamicol] [(+)-[(125)I]pIV], which is reported to bind with high affinity to sigma-1 receptors in vitro, was tested for its usefulness in imaging sigma-1 receptors in the central nervous system (CNS) in vivo. In biodistribution studies, significant amounts (approximately 3% of the injected dose) of (+)-[(125)I]pIV accumulated in rat brain, and its retention was prolonged. In blocking studies, the accumulation of (+)-[(125)I]pIV in the rat brain was significantly reduced by the coadministration of sigma-ligands such as pentazocine (5.0 micromol), haloperidol (0.5 micromol) or SA4503 (0.5 micromol). The blocking effect of pentazocine (selective sigma-1 ligand) was similar to the blocking effects of SA4503 and haloperidol [nonselective sigma (sigma-1 and sigma-2) ligands]. Ex vivo autoradiography of the rat brain at 45 min following intravenous injection of (+)-[(125)I]pIV showed high localization in brain areas rich in sigma-1 receptors. Thus, the distribution of (+)-[(125)I]pIV was thought to bind to sigma-1 receptors in the CNS in vivo. These results indicate that radioiodinated (+)-pIV may have the potential to image sigma-1 receptors in vivo.

    In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Publishing Authors By Initials

    n akhterN Akhter,k shibaK Shiba,k ogawaK Ogawa,s kinuyaS Kinuya,k nakajimaK Nakajima,h moriH Mori,

    For similar biochemical phenomena, metabolism, and nutrition: metabolism: pharmacokinetics: tissue distribution research abstracts see: biochemical phenomena, metabolism, and nutrition: metabolism: pharmacokinetics: tissue distribution research

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    In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Journal Published:

    PUBLICATION TYPE: Journal Article

    Journal: Nuclear medicine and biology

    VOLUME: 34

    Page Numbers: 697-702

    Journal Abbreviation: Nucl. Med. Biol.

    ISSN: 0969-8051

    DAY: 21

    MONTH: Aug

    YEAR: 2007

    In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Information

    Number of References:

    LANGUAGE: eng

    NlmUniqueID: 9304420

    In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Keywords Mesh Terms:

    KEYWORDS: Tissue Distribution

    MESH TERMS: metabolism

    Chemical & Substance for Abstract: In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent. Information

    Substance Name: Haloperidol

    Registry Number: 52-86-8

    Grant and Affiliation Information for In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent.

    AFFILIATION: Department of Biotracer Medicine, Kanazawa University, Kanazawa 920-8640, Japan.

    Country: England

    England Research Publication

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    MEDLINETA: Nucl Med Biol

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    In vivo characterization of radioiodinated +-2-4-4-iodophenyl piperidino cyclohexanol as a potential sigma-1 receptor imaging agent Related Publications

     

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