Publication

Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging

Shalgunov, V., van Waarde, A., Booij, J., Michel, M. C., Dierckx, R. & Elsinga, P. H., May-2019, In : Medicinal research reviews. 39, 3, p. 1014-1052 39 p.

Research output: Contribution to journalReview articleAcademicpeer-review

APA

Shalgunov, V., van Waarde, A., Booij, J., Michel, M. C., Dierckx, R., & Elsinga, P. H. (2019). Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging. Medicinal research reviews, 39(3), 1014-1052. https://doi.org/10.1002/med.21552

Author

Shalgunov, Vladimir ; van Waarde, Aren ; Booij, Jan ; Michel, Martin C ; Dierckx, Rudi ; Elsinga, Philip H. / Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers : Theoretical and practical considerations for positron emission tomography imaging. In: Medicinal research reviews. 2019 ; Vol. 39, No. 3. pp. 1014-1052.

Harvard

Shalgunov, V, van Waarde, A, Booij, J, Michel, MC, Dierckx, R & Elsinga, PH 2019, 'Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging', Medicinal research reviews, vol. 39, no. 3, pp. 1014-1052. https://doi.org/10.1002/med.21552

Standard

Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers : Theoretical and practical considerations for positron emission tomography imaging. / Shalgunov, Vladimir; van Waarde, Aren; Booij, Jan; Michel, Martin C; Dierckx, Rudi; Elsinga, Philip H.

In: Medicinal research reviews, Vol. 39, No. 3, 05.2019, p. 1014-1052.

Research output: Contribution to journalReview articleAcademicpeer-review

Vancouver

Shalgunov V, van Waarde A, Booij J, Michel MC, Dierckx R, Elsinga PH. Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging. Medicinal research reviews. 2019 May;39(3):1014-1052. https://doi.org/10.1002/med.21552


BibTeX

@article{5f209f7c74f74dc8aeac6e57857fa63b,
title = "Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging",
abstract = "The concept of the high-affinity state postulates that a certain subset of G-protein-coupled receptors is primarily responsible for receptor signaling in the living brain. Assessing the abundance of this subset is thus potentially highly relevant for studies concerning the responses of neurotransmission to pharmacological or physiological stimuli and the dysregulation of neurotransmission in neurological or psychiatric disorders. The high-affinity state is preferentially recognized by agonists in vitro. For this reason, agonist tracers have been developed as tools for the noninvasive imaging of the high-affinity state with positron emission tomography (PET). This review provides an overview of agonist tracers that have been developed for PET imaging of the brain, and the experimental paradigms that have been developed for the estimation of the relative abundance of receptors configured in the high-affinity state. Agonist tracers appear to be more sensitive to endogenous neurotransmitter challenge than antagonists, as was originally expected. However, other expectations regarding agonist tracers have not been fulfilled. Potential reasons for difficulties in detecting the high-affinity state in vivo are discussed.",
keywords = "agonist high-affinity state, experimental design, G-protein-coupled receptors, human brain, neurotransmitters, positron emission tomography, IN-VIVO BINDING, DOPAMINE D2(HIGH) RECEPTORS, TEST-RETEST REPRODUCIBILITY, ENDOGENOUS OPIOID RELEASE, BETA-ADRENERGIC-RECEPTOR, NONHUMAN PRIMATE BRAIN, D-2/3 AGONIST, 5-HT1A RECEPTORS, PET RADIOLIGAND, RAT-BRAIN",
author = "Vladimir Shalgunov and {van Waarde}, Aren and Jan Booij and Michel, {Martin C} and Rudi Dierckx and Elsinga, {Philip H.}",
year = "2019",
month = "5",
doi = "10.1002/med.21552",
language = "English",
volume = "39",
pages = "1014--1052",
journal = "Medicinal research reviews",
issn = "0198-6325",
publisher = "Wiley",
number = "3",

}

RIS

TY - JOUR

T1 - Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers

T2 - Theoretical and practical considerations for positron emission tomography imaging

AU - Shalgunov, Vladimir

AU - van Waarde, Aren

AU - Booij, Jan

AU - Michel, Martin C

AU - Dierckx, Rudi

AU - Elsinga, Philip H.

PY - 2019/5

Y1 - 2019/5

N2 - The concept of the high-affinity state postulates that a certain subset of G-protein-coupled receptors is primarily responsible for receptor signaling in the living brain. Assessing the abundance of this subset is thus potentially highly relevant for studies concerning the responses of neurotransmission to pharmacological or physiological stimuli and the dysregulation of neurotransmission in neurological or psychiatric disorders. The high-affinity state is preferentially recognized by agonists in vitro. For this reason, agonist tracers have been developed as tools for the noninvasive imaging of the high-affinity state with positron emission tomography (PET). This review provides an overview of agonist tracers that have been developed for PET imaging of the brain, and the experimental paradigms that have been developed for the estimation of the relative abundance of receptors configured in the high-affinity state. Agonist tracers appear to be more sensitive to endogenous neurotransmitter challenge than antagonists, as was originally expected. However, other expectations regarding agonist tracers have not been fulfilled. Potential reasons for difficulties in detecting the high-affinity state in vivo are discussed.

AB - The concept of the high-affinity state postulates that a certain subset of G-protein-coupled receptors is primarily responsible for receptor signaling in the living brain. Assessing the abundance of this subset is thus potentially highly relevant for studies concerning the responses of neurotransmission to pharmacological or physiological stimuli and the dysregulation of neurotransmission in neurological or psychiatric disorders. The high-affinity state is preferentially recognized by agonists in vitro. For this reason, agonist tracers have been developed as tools for the noninvasive imaging of the high-affinity state with positron emission tomography (PET). This review provides an overview of agonist tracers that have been developed for PET imaging of the brain, and the experimental paradigms that have been developed for the estimation of the relative abundance of receptors configured in the high-affinity state. Agonist tracers appear to be more sensitive to endogenous neurotransmitter challenge than antagonists, as was originally expected. However, other expectations regarding agonist tracers have not been fulfilled. Potential reasons for difficulties in detecting the high-affinity state in vivo are discussed.

KW - agonist high-affinity state

KW - experimental design

KW - G-protein-coupled receptors

KW - human brain

KW - neurotransmitters

KW - positron emission tomography

KW - IN-VIVO BINDING

KW - DOPAMINE D2(HIGH) RECEPTORS

KW - TEST-RETEST REPRODUCIBILITY

KW - ENDOGENOUS OPIOID RELEASE

KW - BETA-ADRENERGIC-RECEPTOR

KW - NONHUMAN PRIMATE BRAIN

KW - D-2/3 AGONIST

KW - 5-HT1A RECEPTORS

KW - PET RADIOLIGAND

KW - RAT-BRAIN

U2 - 10.1002/med.21552

DO - 10.1002/med.21552

M3 - Review article

VL - 39

SP - 1014

EP - 1052

JO - Medicinal research reviews

JF - Medicinal research reviews

SN - 0198-6325

IS - 3

ER -

ID: 66412686