Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites

Paola Sabbatini; Petrine Wellendorph; Signe Høg; Martin Holst Friborg Pedersen; Hans Bräuner-Osborne; Lars Martiny; Bente Flensborg Frølund; Rasmus Prætorius Clausen

doi:10.1021/jm1006325

Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites

Paola Sabbatini, Petrine Wellendorph, Signe Høg, Martin Holst Friborg Pedersen, Hans Bräuner-Osborne, Lars Martiny, Bente Flensborg Frølund, Rasmus Prætorius Clausen

17 Citationer (Scopus)

Abstract

γ-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiological significance, the complete molecular mechanisms of action remain unexplained. To facilitate the isolation and identification of the high-affinity GHB binding site, we herein report the design and synthesis of the first ¹²⁵I-labeled radioligands in the field, one of which contains a photoaffinity label which enables it to bind irreversibly to the high-affinity GHB binding sites.

Originalsprog	Engelsk
Tidsskrift	Journal of Medicinal Chemistry
Vol/bind	53
Udgave nummer	17
Sider (fra-til)	6506-6510
ISSN	0022-2623
DOI	https://doi.org/10.1021/jm1006325
Status	Udgivet - 9 sep. 2010

Emneord

Det tidligere Farmaceutiske Fakultet

Adgang til dokumentet

10.1021/jm1006325

Fingeraftryk

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Citationsformater

Sabbatini, P., Wellendorph, P., Høg, S., Pedersen, M. H. F., Bräuner-Osborne, H., Martiny, L., Frølund, B. F., & Clausen, R. P. (2010). Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites. Journal of Medicinal Chemistry, 53(17), 6506-6510. https://doi.org/10.1021/jm1006325

Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites. / Sabbatini, Paola; Wellendorph, Petrine; Høg, Signe et al.
I: Journal of Medicinal Chemistry, Bind 53, Nr. 17, 09.09.2010, s. 6506-6510.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

Sabbatini, P, Wellendorph, P, Høg, S, Pedersen, MHF, Bräuner-Osborne, H, Martiny, L, Frølund, BF & Clausen, RP 2010, 'Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites', Journal of Medicinal Chemistry, bind 53, nr. 17, s. 6506-6510. https://doi.org/10.1021/jm1006325

Sabbatini P, Wellendorph P, Høg S, Pedersen MHF, Bräuner-Osborne H, Martiny L et al. Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites. Journal of Medicinal Chemistry. 2010 sep. 9;53(17):6506-6510. doi: 10.1021/jm1006325

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AU - Høg, Signe

AU - Pedersen, Martin Holst Friborg

AU - Bräuner-Osborne, Hans

AU - Martiny, Lars

AU - Frølund, Bente Flensborg

AU - Clausen, Rasmus Prætorius

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AB - γ-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiological significance, the complete molecular mechanisms of action remain unexplained. To facilitate the isolation and identification of the high-affinity GHB binding site, we herein report the design and synthesis of the first 125I-labeled radioligands in the field, one of which contains a photoaffinity label which enables it to bind irreversibly to the high-affinity GHB binding sites.

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