Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology. / Griem-Krey, Nane; Frolund, Bente; Marek, Ales; Wellendorph, Petrine.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 64, No. 2, 2021.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Griem-Krey, N, Frolund, B, Marek, A & Wellendorph, P 2021, 'Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology', Journal of Labelled Compounds and Radiopharmaceuticals, vol. 64, no. 2. https://doi.org/10.1002/jlcr.3870

APA

Griem-Krey, N., Frolund, B., Marek, A., & Wellendorph, P. (2021). Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology. Journal of Labelled Compounds and Radiopharmaceuticals, 64(2). https://doi.org/10.1002/jlcr.3870

Vancouver

Griem-Krey N, Frolund B, Marek A, Wellendorph P. Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology. Journal of Labelled Compounds and Radiopharmaceuticals. 2021;64(2). https://doi.org/10.1002/jlcr.3870

Author

Griem-Krey, Nane ; Frolund, Bente ; Marek, Ales ; Wellendorph, Petrine. / Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology. In: Journal of Labelled Compounds and Radiopharmaceuticals. 2021 ; Vol. 64, No. 2.

Bibtex

@article{828ba3e8422b458cb8e4c257f76d3f45,
title = "Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology",
abstract = "GHB (gamma-hydroxybutyrate) is not only an endogenously present small molecule but also a clinically prescribed drug for the symptomatic treatment of narcolepsy. However, GHB's mechanism of action remains to be uncovered. Within the CNS, GHB targets both GABA(B)receptors and a pharmacologically distinct population of high-affinity binding sites with unknown molecular identity. HOCPCA (3-hydroxycyclopent-1-enecarboxylic acid) is a structural analog of GHB selectively targeting GHB high-affinity binding sites. Here, we discuss the usefulness of(3)H- and(11)C-labeled HOCPCA as radioligands for selectively probing GHB high-affinity binding sites and their application in drug discovery. As such, [H-3]HOCPCA's exceptional affinity and selectivity makes it an indispensable tool in drug discovery, and its utility has been demonstrated in, for example, homogenate binding studies,in vitroas well asex vivoautoradiography. Moreover, the successful synthesis of [C-11]HOCPCA is a starting point for further ligand development for futurein vivoinvestigations of GHB high-affinity binding sites.",
keywords = "GHB high-affinity binding sites, MCT1 uptake, radioligand binding, selective GHB ligand, GAMMA-HYDROXYBUTYRIC ACID, AFFINITY BINDING-SITE, ETHANOIC ACID, GHB",
author = "Nane Griem-Krey and Bente Frolund and Ales Marek and Petrine Wellendorph",
year = "2021",
doi = "10.1002/jlcr.3870",
language = "English",
volume = "64",
journal = "Journal of Labelled Compounds and Radiopharmaceuticals",
issn = "0362-4803",
publisher = "JohnWiley & Sons Ltd",
number = "2",

}

RIS

TY - JOUR

T1 - Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology

AU - Griem-Krey, Nane

AU - Frolund, Bente

AU - Marek, Ales

AU - Wellendorph, Petrine

PY - 2021

Y1 - 2021

N2 - GHB (gamma-hydroxybutyrate) is not only an endogenously present small molecule but also a clinically prescribed drug for the symptomatic treatment of narcolepsy. However, GHB's mechanism of action remains to be uncovered. Within the CNS, GHB targets both GABA(B)receptors and a pharmacologically distinct population of high-affinity binding sites with unknown molecular identity. HOCPCA (3-hydroxycyclopent-1-enecarboxylic acid) is a structural analog of GHB selectively targeting GHB high-affinity binding sites. Here, we discuss the usefulness of(3)H- and(11)C-labeled HOCPCA as radioligands for selectively probing GHB high-affinity binding sites and their application in drug discovery. As such, [H-3]HOCPCA's exceptional affinity and selectivity makes it an indispensable tool in drug discovery, and its utility has been demonstrated in, for example, homogenate binding studies,in vitroas well asex vivoautoradiography. Moreover, the successful synthesis of [C-11]HOCPCA is a starting point for further ligand development for futurein vivoinvestigations of GHB high-affinity binding sites.

AB - GHB (gamma-hydroxybutyrate) is not only an endogenously present small molecule but also a clinically prescribed drug for the symptomatic treatment of narcolepsy. However, GHB's mechanism of action remains to be uncovered. Within the CNS, GHB targets both GABA(B)receptors and a pharmacologically distinct population of high-affinity binding sites with unknown molecular identity. HOCPCA (3-hydroxycyclopent-1-enecarboxylic acid) is a structural analog of GHB selectively targeting GHB high-affinity binding sites. Here, we discuss the usefulness of(3)H- and(11)C-labeled HOCPCA as radioligands for selectively probing GHB high-affinity binding sites and their application in drug discovery. As such, [H-3]HOCPCA's exceptional affinity and selectivity makes it an indispensable tool in drug discovery, and its utility has been demonstrated in, for example, homogenate binding studies,in vitroas well asex vivoautoradiography. Moreover, the successful synthesis of [C-11]HOCPCA is a starting point for further ligand development for futurein vivoinvestigations of GHB high-affinity binding sites.

KW - GHB high-affinity binding sites

KW - MCT1 uptake

KW - radioligand binding

KW - selective GHB ligand

KW - GAMMA-HYDROXYBUTYRIC ACID

KW - AFFINITY BINDING-SITE

KW - ETHANOIC ACID

KW - GHB

U2 - 10.1002/jlcr.3870

DO - 10.1002/jlcr.3870

M3 - Journal article

VL - 64

JO - Journal of Labelled Compounds and Radiopharmaceuticals

JF - Journal of Labelled Compounds and Radiopharmaceuticals

SN - 0362-4803

IS - 2

ER -

ID: 248498955