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 Citations (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.

Original language	English
Journal	Journal of Medicinal Chemistry
Volume	53
Issue number	17
Pages (from-to)	6506-6510
ISSN	0022-2623
DOIs	https://doi.org/10.1021/jm1006325
Publication status	Published - 9 Sept 2010

Keywords

Former Faculty of Pharmaceutical Sciences

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10.1021/jm1006325

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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.

In: Journal of Medicinal Chemistry, Vol. 53, No. 17, 09.09.2010, p. 6506-6510.

Research output: Contribution to journal › Journal article › Research › 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, vol. 53, no. 17, pp. 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 Sept 9;53(17):6506-6510. doi: 10.1021/jm1006325

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