Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain

Nafiseh Ghazanfari; Aren van Waarde; Janine Doorduin; Jürgen W.A. Sijbesma; Maria Kominia; Martin Koelewijn; Khaled Attia; Antoon T.M. Willemsen; Ton J. Visser; André Heeres; Rudi A. J. O.  Dierckx; Erik de Vries; Philip Elsinga

doi:10.1021/acs.molpharmaceut.1c00889

Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain

Nafiseh Ghazanfari, Aren van Waarde, Janine Doorduin, Jürgen W.A. Sijbesma, Maria Kominia, Martin Koelewijn, Khaled Attia, Antoon T.M. Willemsen, Ton J. Visser, André Heeres, Rudi A. J. O. Dierckx, Erik de Vries, Philip Elsinga

Research output: Contribution to journal › Article › Academic › peer-review

Abstract

The histamine H3 receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective histamine H3 receptor antagonist [11C]GSK-189254 in rodents could be used to examine the mechanisms of action of novel therapeutic drugs or to assess changes of regional H3 receptor density in animal models of neurodegenerative disease. [11C]GSK-189254 was intravenously administered to healthy Wistar rats (n = 10), and a 60 min dynamic PET scan was carried out. Arterial blood samples were obtained during the scan to generate a metabolite-corrected plasma input function. PET data were analyzed using a one-tissue compartment model (1T2k), irreversible (2T3k) or reversible two-tissue compartment models (2T4k), graphical analysis (Logan and Patlak), reference tissue models (SRTM and SRTM2), and standard uptake values (SUVs). The Akaike information criterion and the standard error of the estimated parameters were used to select the most optimal quantification method. This study demonstrated that the 2T4k model with a fixed blood volume fraction and Logan graphical analysis can best describe the kinetics of [11C]GSK-189254 in the rat brain. SUV40–60 and the reference tissue-based measurements DVR(2T4k), BPND(SRTM), and SUV ratio could also be used as a simplified method to estimate H3 receptor availability in case blood sampling is not feasible.

Original language	English
Pages (from-to)	918–928
Number of pages	11
Journal	Molecular Pharmaceutics
Volume	19
Issue number	3
DOIs	https://doi.org/10.1021/acs.molpharmaceut.1c00889
Publication status	Published - 16 Feb 2022
Externally published	Yes

Keywords

central nervous system
positron emission tomography
receptors

Access to Document

10.1021/acs.molpharmaceut.1c00889Licence: CC BY

11 Article
1 Report
1 Poster
1 Patent

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Research output: Contribution to journal › Article › Academic › peer-review

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Research output: Contribution to journal › Article › Academic › peer-review

Open Access

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1 Oral presentation

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Cite this

Ghazanfari, N., van Waarde, A., Doorduin, J., Sijbesma, J. W. A., Kominia, M., Koelewijn, M., Attia, K., T.M. Willemsen, A., Visser, T. J., Heeres, A., Dierckx, R. A. J. O., de Vries, E., & Elsinga, P. (2022). Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain. Molecular Pharmaceutics, 19(3), 918–928. https://doi.org/10.1021/acs.molpharmaceut.1c00889

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title = "Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain",

abstract = "The histamine H3 receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective histamine H3 receptor antagonist [11C]GSK-189254 in rodents could be used to examine the mechanisms of action of novel therapeutic drugs or to assess changes of regional H3 receptor density in animal models of neurodegenerative disease. [11C]GSK-189254 was intravenously administered to healthy Wistar rats (n = 10), and a 60 min dynamic PET scan was carried out. Arterial blood samples were obtained during the scan to generate a metabolite-corrected plasma input function. PET data were analyzed using a one-tissue compartment model (1T2k), irreversible (2T3k) or reversible two-tissue compartment models (2T4k), graphical analysis (Logan and Patlak), reference tissue models (SRTM and SRTM2), and standard uptake values (SUVs). The Akaike information criterion and the standard error of the estimated parameters were used to select the most optimal quantification method. This study demonstrated that the 2T4k model with a fixed blood volume fraction and Logan graphical analysis can best describe the kinetics of [11C]GSK-189254 in the rat brain. SUV40–60 and the reference tissue-based measurements DVR(2T4k), BPND(SRTM), and SUV ratio could also be used as a simplified method to estimate H3 receptor availability in case blood sampling is not feasible.",

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doi = "10.1021/acs.molpharmaceut.1c00889",

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Ghazanfari, N, van Waarde, A, Doorduin, J, Sijbesma, JWA, Kominia, M, Koelewijn, M, Attia, K, T.M. Willemsen, A, Visser, TJ, Heeres, A, Dierckx, RAJO, de Vries, E & Elsinga, P 2022, 'Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain', Molecular Pharmaceutics, vol. 19, no. 3, pp. 918–928. https://doi.org/10.1021/acs.molpharmaceut.1c00889

TY - JOUR

T1 - Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain

AU - Ghazanfari, Nafiseh

AU - van Waarde, Aren

AU - Doorduin, Janine

AU - Sijbesma, Jürgen W.A.

AU - Kominia, Maria

AU - Koelewijn, Martin

AU - Attia, Khaled

AU - T.M. Willemsen, Antoon

AU - Visser, Ton J.

AU - Heeres, André

AU - Dierckx, Rudi A. J. O.

AU - de Vries, Erik

AU - Elsinga, Philip

PY - 2022/2/16

Y1 - 2022/2/16

N2 - The histamine H3 receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective histamine H3 receptor antagonist [11C]GSK-189254 in rodents could be used to examine the mechanisms of action of novel therapeutic drugs or to assess changes of regional H3 receptor density in animal models of neurodegenerative disease. [11C]GSK-189254 was intravenously administered to healthy Wistar rats (n = 10), and a 60 min dynamic PET scan was carried out. Arterial blood samples were obtained during the scan to generate a metabolite-corrected plasma input function. PET data were analyzed using a one-tissue compartment model (1T2k), irreversible (2T3k) or reversible two-tissue compartment models (2T4k), graphical analysis (Logan and Patlak), reference tissue models (SRTM and SRTM2), and standard uptake values (SUVs). The Akaike information criterion and the standard error of the estimated parameters were used to select the most optimal quantification method. This study demonstrated that the 2T4k model with a fixed blood volume fraction and Logan graphical analysis can best describe the kinetics of [11C]GSK-189254 in the rat brain. SUV40–60 and the reference tissue-based measurements DVR(2T4k), BPND(SRTM), and SUV ratio could also be used as a simplified method to estimate H3 receptor availability in case blood sampling is not feasible.

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KW - centraal zenuwstelsel

KW - positronemissietomografie

KW - receptoren

KW - central nervous system

KW - positron emission tomography

KW - receptors

U2 - 10.1021/acs.molpharmaceut.1c00889

DO - 10.1021/acs.molpharmaceut.1c00889

M3 - Article

SN - 1543-8392

VL - 19

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JO - Molecular Pharmaceutics

JF - Molecular Pharmaceutics

IS - 3

ER -

Pharmacokinetic Modeling of [11C]GSK-189254, PET Tracer Targeting H3 Receptors, in Rat Brain

Abstract

Keywords

Access to Document

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Research output

Substituted anilides from chitin-based 3-acetamido-furfural

Advantages of Producing Aromatics from Propene over Ethene Using Zeolite-Based Catalysts

A time- and space-resolved catalyst deactivation study on the conversion of glycerol to aromatics using H-ZSM-5

Activities

Biobased/circular chemistry at the Hanze.

Sustainable building blocks at the Hanze

De biobased/circulaire transitie (Hanze) - Konnect-lezing Eemshaven

Cite this