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Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites

Research output: Contribution to journalLetterResearchpeer-review

Standard

Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites. / Jensen, Claus H; Hansen, Hanne D; Bay, Tina; Vogensen, Stine B; Lehel, Szabolcs; Thiesen, Louise; Bundgaard, Christoffer; Clausen, Rasmus P; Knudsen, Gitte M; Herth, Matthias M; Wellendorph, Petrine; Frølund, Bente.

In: A C S Chemical Neuroscience, Vol. 8, No. 1, 18.01.2017, p. 22-27.

Research output: Contribution to journalLetterResearchpeer-review

Harvard

Jensen, CH, Hansen, HD, Bay, T, Vogensen, SB, Lehel, S, Thiesen, L, Bundgaard, C, Clausen, RP, Knudsen, GM, Herth, MM, Wellendorph, P & Frølund, B 2017, 'Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites', A C S Chemical Neuroscience, vol. 8, no. 1, pp. 22-27. https://doi.org/10.1021/acschemneuro.6b00335

APA

Jensen, C. H., Hansen, H. D., Bay, T., Vogensen, S. B., Lehel, S., Thiesen, L., ... Frølund, B. (2017). Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites. A C S Chemical Neuroscience, 8(1), 22-27. https://doi.org/10.1021/acschemneuro.6b00335

Vancouver

Jensen CH, Hansen HD, Bay T, Vogensen SB, Lehel S, Thiesen L et al. Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites. A C S Chemical Neuroscience. 2017 Jan 18;8(1):22-27. https://doi.org/10.1021/acschemneuro.6b00335

Author

Jensen, Claus H ; Hansen, Hanne D ; Bay, Tina ; Vogensen, Stine B ; Lehel, Szabolcs ; Thiesen, Louise ; Bundgaard, Christoffer ; Clausen, Rasmus P ; Knudsen, Gitte M ; Herth, Matthias M ; Wellendorph, Petrine ; Frølund, Bente. / Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites. In: A C S Chemical Neuroscience. 2017 ; Vol. 8, No. 1. pp. 22-27.

Bibtex

@article{6b9bc445306f47c9828bd65adf7096b3,
title = "Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites",
abstract = "γ-Hydroxybutyric acid (GHB) is an endogenous neuroactive substance and proposed neurotransmitter with affinity for both low- and high-affinity binding sites. A radioligand with high and specific affinity toward the high-affinity GHB binding site would be a unique tool toward a more complete understanding of this population of binding sites. With its high specific affinity and monocarboxylate transporter (MCT1) mediated transport across the blood-brain barrier in pharmacological doses, 3-hydroxycyclopent-1-enecarboxylic acid (HOCPCA) seems like a suitable PET radiotracer candidate. Here, we report the (11)C-labeling and subsequent evaluation of [(11)C]HOCPCA in a domestic pig, as a PET-radioligand for visualization of the high-affinity GHB binding sites in the live pig brain. To investigate the regional binding of HOCPCA in pig brain prior to in vivo PET studies, in vitro quantitative autoradiography on sections of pig brain was performed using [(3)H]HOCPCA. In vivo evaluation of [(11)C]HOCPCA showed no brain uptake, possibly due to a limited uptake of HOCPCA by the MCT1 transporter at tracer doses of [(11)C]HOCPCA.",
author = "Jensen, {Claus H} and Hansen, {Hanne D} and Tina Bay and Vogensen, {Stine B} and Szabolcs Lehel and Louise Thiesen and Christoffer Bundgaard and Clausen, {Rasmus P} and Knudsen, {Gitte M} and Herth, {Matthias M} and Petrine Wellendorph and Bente Fr{\o}lund",
year = "2017",
month = "1",
day = "18",
doi = "10.1021/acschemneuro.6b00335",
language = "English",
volume = "8",
pages = "22--27",
journal = "A C S Chemical Neuroscience",
issn = "1948-7193",
publisher = "American Chemical Society",
number = "1",

}

RIS

TY - JOUR

T1 - Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites

AU - Jensen, Claus H

AU - Hansen, Hanne D

AU - Bay, Tina

AU - Vogensen, Stine B

AU - Lehel, Szabolcs

AU - Thiesen, Louise

AU - Bundgaard, Christoffer

AU - Clausen, Rasmus P

AU - Knudsen, Gitte M

AU - Herth, Matthias M

AU - Wellendorph, Petrine

AU - Frølund, Bente

PY - 2017/1/18

Y1 - 2017/1/18

N2 - γ-Hydroxybutyric acid (GHB) is an endogenous neuroactive substance and proposed neurotransmitter with affinity for both low- and high-affinity binding sites. A radioligand with high and specific affinity toward the high-affinity GHB binding site would be a unique tool toward a more complete understanding of this population of binding sites. With its high specific affinity and monocarboxylate transporter (MCT1) mediated transport across the blood-brain barrier in pharmacological doses, 3-hydroxycyclopent-1-enecarboxylic acid (HOCPCA) seems like a suitable PET radiotracer candidate. Here, we report the (11)C-labeling and subsequent evaluation of [(11)C]HOCPCA in a domestic pig, as a PET-radioligand for visualization of the high-affinity GHB binding sites in the live pig brain. To investigate the regional binding of HOCPCA in pig brain prior to in vivo PET studies, in vitro quantitative autoradiography on sections of pig brain was performed using [(3)H]HOCPCA. In vivo evaluation of [(11)C]HOCPCA showed no brain uptake, possibly due to a limited uptake of HOCPCA by the MCT1 transporter at tracer doses of [(11)C]HOCPCA.

AB - γ-Hydroxybutyric acid (GHB) is an endogenous neuroactive substance and proposed neurotransmitter with affinity for both low- and high-affinity binding sites. A radioligand with high and specific affinity toward the high-affinity GHB binding site would be a unique tool toward a more complete understanding of this population of binding sites. With its high specific affinity and monocarboxylate transporter (MCT1) mediated transport across the blood-brain barrier in pharmacological doses, 3-hydroxycyclopent-1-enecarboxylic acid (HOCPCA) seems like a suitable PET radiotracer candidate. Here, we report the (11)C-labeling and subsequent evaluation of [(11)C]HOCPCA in a domestic pig, as a PET-radioligand for visualization of the high-affinity GHB binding sites in the live pig brain. To investigate the regional binding of HOCPCA in pig brain prior to in vivo PET studies, in vitro quantitative autoradiography on sections of pig brain was performed using [(3)H]HOCPCA. In vivo evaluation of [(11)C]HOCPCA showed no brain uptake, possibly due to a limited uptake of HOCPCA by the MCT1 transporter at tracer doses of [(11)C]HOCPCA.

U2 - 10.1021/acschemneuro.6b00335

DO - 10.1021/acschemneuro.6b00335

M3 - Letter

VL - 8

SP - 22

EP - 27

JO - A C S Chemical Neuroscience

T2 - A C S Chemical Neuroscience

JF - A C S Chemical Neuroscience

SN - 1948-7193

IS - 1

ER -

ID: 172370664