Metabolic imaging with gallium-68- and indium-111-labeled low-density lipoprotein

S. M. Moerlein; A. Daugherty; B. E. Sobel; M. J. Welch

Metabolic imaging with gallium-68- and indium-111-labeled low-density lipoprotein

S. M. Moerlein, A. Daugherty, B. E. Sobel, M. J. Welch

Research output: Contribution to journal › Article › peer-review

Abstract

Low-density lipoprotein (LDL) labeled with either gallium-68 (⁶⁸Ga) or indium-111 (¹¹¹In) was evaluated as a potential PET or SPECT radiopharmaceutical for determination of hepatic lipoprotein metabolism in rabbits. Gallium-68 or ¹¹¹In was linked to LDL via diethylenetriaminepentaacetic acid (DTPA) with a 25-70% radiochemical yield. Studies in vivo that compared ⁶⁸Ga- or ¹¹¹In-DTPA-LDL with dilactitol-[¹²⁵I]-tyramine LDL and ¹³¹I-LDL showed that both ⁶⁸Ga- and ¹¹¹In-labeled LDL behaved as residualizing radiotracers. Localization of radioactivity within the liver of normal rabbits was visualized clearly with [⁶⁸Ga]DTPA-LDL by PET and with [¹¹¹In]DTPA-LDL by gamma scintigraphy. Significant differences were observed in hepatic uptake of normal compared with hypercholesterolemic rabbits in which low-capacity LDL receptor-mediated catabolism was saturated. Gallium-68 and ¹¹¹In-DTPA-LDL are attractive radiopharmaceuticals for noninvasive delineation of tissue LDL metabolism under normal and pathophysiologic conditions.

Original language	English
Pages (from-to)	300-307
Number of pages	8
Journal	Journal of Nuclear Medicine
Volume	32
Issue number	2
State	Published - 1991

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title = "Metabolic imaging with gallium-68- and indium-111-labeled low-density lipoprotein",

abstract = "Low-density lipoprotein (LDL) labeled with either gallium-68 (68Ga) or indium-111 (111In) was evaluated as a potential PET or SPECT radiopharmaceutical for determination of hepatic lipoprotein metabolism in rabbits. Gallium-68 or 111In was linked to LDL via diethylenetriaminepentaacetic acid (DTPA) with a 25-70% radiochemical yield. Studies in vivo that compared 68Ga- or 111In-DTPA-LDL with dilactitol-[125I]-tyramine LDL and 131I-LDL showed that both 68Ga- and 111In-labeled LDL behaved as residualizing radiotracers. Localization of radioactivity within the liver of normal rabbits was visualized clearly with [68Ga]DTPA-LDL by PET and with [111In]DTPA-LDL by gamma scintigraphy. Significant differences were observed in hepatic uptake of normal compared with hypercholesterolemic rabbits in which low-capacity LDL receptor-mediated catabolism was saturated. Gallium-68 and 111In-DTPA-LDL are attractive radiopharmaceuticals for noninvasive delineation of tissue LDL metabolism under normal and pathophysiologic conditions.",

author = "Moerlein, {S. M.} and A. Daugherty and Sobel, {B. E.} and Welch, {M. J.}",

year = "1991",

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volume = "32",

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journal = "Journal of Nuclear Medicine",

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T1 - Metabolic imaging with gallium-68- and indium-111-labeled low-density lipoprotein

AU - Moerlein, S. M.

AU - Daugherty, A.

AU - Sobel, B. E.

AU - Welch, M. J.

PY - 1991

Y1 - 1991

N2 - Low-density lipoprotein (LDL) labeled with either gallium-68 (68Ga) or indium-111 (111In) was evaluated as a potential PET or SPECT radiopharmaceutical for determination of hepatic lipoprotein metabolism in rabbits. Gallium-68 or 111In was linked to LDL via diethylenetriaminepentaacetic acid (DTPA) with a 25-70% radiochemical yield. Studies in vivo that compared 68Ga- or 111In-DTPA-LDL with dilactitol-[125I]-tyramine LDL and 131I-LDL showed that both 68Ga- and 111In-labeled LDL behaved as residualizing radiotracers. Localization of radioactivity within the liver of normal rabbits was visualized clearly with [68Ga]DTPA-LDL by PET and with [111In]DTPA-LDL by gamma scintigraphy. Significant differences were observed in hepatic uptake of normal compared with hypercholesterolemic rabbits in which low-capacity LDL receptor-mediated catabolism was saturated. Gallium-68 and 111In-DTPA-LDL are attractive radiopharmaceuticals for noninvasive delineation of tissue LDL metabolism under normal and pathophysiologic conditions.

AB - Low-density lipoprotein (LDL) labeled with either gallium-68 (68Ga) or indium-111 (111In) was evaluated as a potential PET or SPECT radiopharmaceutical for determination of hepatic lipoprotein metabolism in rabbits. Gallium-68 or 111In was linked to LDL via diethylenetriaminepentaacetic acid (DTPA) with a 25-70% radiochemical yield. Studies in vivo that compared 68Ga- or 111In-DTPA-LDL with dilactitol-[125I]-tyramine LDL and 131I-LDL showed that both 68Ga- and 111In-labeled LDL behaved as residualizing radiotracers. Localization of radioactivity within the liver of normal rabbits was visualized clearly with [68Ga]DTPA-LDL by PET and with [111In]DTPA-LDL by gamma scintigraphy. Significant differences were observed in hepatic uptake of normal compared with hypercholesterolemic rabbits in which low-capacity LDL receptor-mediated catabolism was saturated. Gallium-68 and 111In-DTPA-LDL are attractive radiopharmaceuticals for noninvasive delineation of tissue LDL metabolism under normal and pathophysiologic conditions.

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C2 - 1992034

AN - SCOPUS:0026099946

SN - 0161-5505

VL - 32

SP - 300

EP - 307

JO - Journal of Nuclear Medicine

JF - Journal of Nuclear Medicine

IS - 2

ER -

Metabolic imaging with gallium-68- and indium-111-labeled low-density lipoprotein

Abstract

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