GHB receptor targets in the CNS: Focus on high-affinity binding sites

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

Standard

GHB receptor targets in the CNS: Focus on high-affinity binding sites. / Bay, Tina; Eghorn, Laura Friis; Klein, Anders Bue; Wellendorph, Petrine.

In: Biochemical Pharmacology, Vol. 87, No. 2, 2014, p. 220-228.

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

Harvard

Bay, T, Eghorn, LF, Klein, AB & Wellendorph, P 2014, 'GHB receptor targets in the CNS: Focus on high-affinity binding sites', Biochemical Pharmacology, vol. 87, no. 2, pp. 220-228. https://doi.org/10.1016/j.bcp.2013.10.028

APA

Bay, T., Eghorn, L. F., Klein, A. B., & Wellendorph, P. (2014). GHB receptor targets in the CNS: Focus on high-affinity binding sites. Biochemical Pharmacology, 87(2), 220-228. https://doi.org/10.1016/j.bcp.2013.10.028

Vancouver

Bay T, Eghorn LF, Klein AB, Wellendorph P. GHB receptor targets in the CNS: Focus on high-affinity binding sites. Biochemical Pharmacology. 2014;87(2):220-228. https://doi.org/10.1016/j.bcp.2013.10.028

Author

Bay, Tina ; Eghorn, Laura Friis ; Klein, Anders Bue ; Wellendorph, Petrine. / GHB receptor targets in the CNS: Focus on high-affinity binding sites. In: Biochemical Pharmacology. 2014 ; Vol. 87, No. 2. pp. 220-228.

Bibtex

@article{edadec5176074253a17db2332eeef9fc,
title = "GHB receptor targets in the CNS: Focus on high-affinity binding sites",
abstract = "γ-Hydroxybutyric acid (GHB) is an endogenous compound in the mammalian brain with both low- and high-affinity receptor targets. GHB is used clinically in the treatment of symptoms of narcolepsy and alcoholism, but also illicitly abused as the recreational drug Fantasy. Major pharmacological effects of exogenous GHB are mediated by GABA subtype B (GABAB) receptors that bind GHB with low affinity. The existence of GHB high-affinity binding sites has been known for more than three decades, but the uncovering of their molecular identity has only recently begun. This has been prompted by the generation of molecular tools to selectively study high-affinity sites. These include both genetically modified GABAB knock-out mice and engineered selective GHB ligands. Recently, certain GABA subtype A (GABAA) receptor subtypes emerged as high-affinity GHB binding sites and potential physiological mediators of GHB effects. In this research update, a description of the various reported receptors for GHB is provided, including GABAB receptors, certain GABAA receptor subtypes and other reported GHB receptors. The main focus will thus be on the high-affinity binding targets for GHB and their potential functional roles in the mammalian brain.",
author = "Tina Bay and Eghorn, {Laura Friis} and Klein, {Anders Bue} and Petrine Wellendorph",
year = "2014",
doi = "10.1016/j.bcp.2013.10.028",
language = "English",
volume = "87",
pages = "220--228",
journal = "Biochemical Pharmacology",
issn = "0006-2952",
publisher = "Elsevier",
number = "2",

}

RIS

TY - JOUR

T1 - GHB receptor targets in the CNS: Focus on high-affinity binding sites

AU - Bay, Tina

AU - Eghorn, Laura Friis

AU - Klein, Anders Bue

AU - Wellendorph, Petrine

PY - 2014

Y1 - 2014

N2 - γ-Hydroxybutyric acid (GHB) is an endogenous compound in the mammalian brain with both low- and high-affinity receptor targets. GHB is used clinically in the treatment of symptoms of narcolepsy and alcoholism, but also illicitly abused as the recreational drug Fantasy. Major pharmacological effects of exogenous GHB are mediated by GABA subtype B (GABAB) receptors that bind GHB with low affinity. The existence of GHB high-affinity binding sites has been known for more than three decades, but the uncovering of their molecular identity has only recently begun. This has been prompted by the generation of molecular tools to selectively study high-affinity sites. These include both genetically modified GABAB knock-out mice and engineered selective GHB ligands. Recently, certain GABA subtype A (GABAA) receptor subtypes emerged as high-affinity GHB binding sites and potential physiological mediators of GHB effects. In this research update, a description of the various reported receptors for GHB is provided, including GABAB receptors, certain GABAA receptor subtypes and other reported GHB receptors. The main focus will thus be on the high-affinity binding targets for GHB and their potential functional roles in the mammalian brain.

AB - γ-Hydroxybutyric acid (GHB) is an endogenous compound in the mammalian brain with both low- and high-affinity receptor targets. GHB is used clinically in the treatment of symptoms of narcolepsy and alcoholism, but also illicitly abused as the recreational drug Fantasy. Major pharmacological effects of exogenous GHB are mediated by GABA subtype B (GABAB) receptors that bind GHB with low affinity. The existence of GHB high-affinity binding sites has been known for more than three decades, but the uncovering of their molecular identity has only recently begun. This has been prompted by the generation of molecular tools to selectively study high-affinity sites. These include both genetically modified GABAB knock-out mice and engineered selective GHB ligands. Recently, certain GABA subtype A (GABAA) receptor subtypes emerged as high-affinity GHB binding sites and potential physiological mediators of GHB effects. In this research update, a description of the various reported receptors for GHB is provided, including GABAB receptors, certain GABAA receptor subtypes and other reported GHB receptors. The main focus will thus be on the high-affinity binding targets for GHB and their potential functional roles in the mammalian brain.

U2 - 10.1016/j.bcp.2013.10.028

DO - 10.1016/j.bcp.2013.10.028

M3 - Review

C2 - 24269284

VL - 87

SP - 220

EP - 228

JO - Biochemical Pharmacology

JF - Biochemical Pharmacology

SN - 0006-2952

IS - 2

ER -

ID: 108655693