Improved synthesis of [18F] fallypride and characterization of a Huntington’s disease mouse model, zQ175DN KI, using longitudinal PET imaging of D2/D3 receptors

Tuulia Huhtala, Pekka Poutiainen, Jussi Rytkönen, Kimmo Lehtimäki, Teija Parkkari, Iiris Kasanen, Anu J. Airaksinen, Teija Koivula, Patrick Sweeney, Outi Kontkanen, John Wityak, Celia Dominiquez, Larry C. Park

Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

Kuvaus

Dopamine receptors are involved in pathophysiology of neuropsychiatric diseases, including Huntington’s disease (HD). PET imaging of dopamine D2 receptors (D2R) in HD patients has demonstrated 40% decrease in D2R binding in striatum, and D2R could be a reliable quantitative target to monitor disease progression. A D2/3R antagonist, [18F] fallypride, is a high-affinity radioligand that has been clinically used to study receptor density and occupancy in neuropsychiatric disorders. Here we report an improved synthesis method for [18F]fallypride. In addition, high molar activity of the ligand has allowed us to apply PET imaging to characterize D2/D3 receptor density in striatum of the recently developed zQ175DN knock-in (KI) mouse model of HD.
Alkuperäiskielienglanti
LehtiEJNMMI Radiopharmacy and Chemistry
Vuosikerta4
Numero1
ISSN2365-421X
DOI - pysyväislinkit
TilaJulkaistu - 5 elokuuta 2019
OKM-julkaisutyyppiA1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä, vertaisarvioitu

Tieteenalat

  • 317 Farmasia
  • 116 Kemia

Lainaa tätä

Huhtala, Tuulia ; Poutiainen, Pekka ; Rytkönen, Jussi ; Lehtimäki, Kimmo ; Parkkari, Teija ; Kasanen, Iiris ; Airaksinen, Anu J. ; Koivula, Teija ; Sweeney, Patrick ; Kontkanen, Outi ; Wityak, John ; Dominiquez, Celia ; Park, Larry C. / Improved synthesis of [18F] fallypride and characterization of a Huntington’s disease mouse model, zQ175DN KI, using longitudinal PET imaging of D2/D3 receptors. Julkaisussa: EJNMMI Radiopharmacy and Chemistry. 2019 ; Vuosikerta 4, Nro 1.
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title = "Improved synthesis of [18F] fallypride and characterization of a Huntington’s disease mouse model, zQ175DN KI, using longitudinal PET imaging of D2/D3 receptors",
abstract = "Dopamine receptors are involved in pathophysiology of neuropsychiatric diseases, including Huntington’s disease (HD). PET imaging of dopamine D2 receptors (D2R) in HD patients has demonstrated 40{\%} decrease in D2R binding in striatum, and D2R could be a reliable quantitative target to monitor disease progression. A D2/3R antagonist, [18F] fallypride, is a high-affinity radioligand that has been clinically used to study receptor density and occupancy in neuropsychiatric disorders. Here we report an improved synthesis method for [18F]fallypride. In addition, high molar activity of the ligand has allowed us to apply PET imaging to characterize D2/D3 receptor density in striatum of the recently developed zQ175DN knock-in (KI) mouse model of HD.",
keywords = "317 Pharmacy, 116 Chemical sciences",
author = "Tuulia Huhtala and Pekka Poutiainen and Jussi Rytk{\"o}nen and Kimmo Lehtim{\"a}ki and Teija Parkkari and Iiris Kasanen and Airaksinen, {Anu J.} and Teija Koivula and Patrick Sweeney and Outi Kontkanen and John Wityak and Celia Dominiquez and Park, {Larry C.}",
year = "2019",
month = "8",
day = "5",
doi = "10.1186/s41181-019-0071-6",
language = "English",
volume = "4",
journal = "EJNMMI Radiopharmacy and Chemistry",
issn = "2365-421X",
publisher = "Springer International Publishing AG",
number = "1",

}

Improved synthesis of [18F] fallypride and characterization of a Huntington’s disease mouse model, zQ175DN KI, using longitudinal PET imaging of D2/D3 receptors. / Huhtala, Tuulia; Poutiainen, Pekka; Rytkönen, Jussi; Lehtimäki, Kimmo; Parkkari, Teija; Kasanen, Iiris; Airaksinen, Anu J.; Koivula, Teija; Sweeney, Patrick; Kontkanen, Outi; Wityak, John; Dominiquez, Celia; Park, Larry C.

julkaisussa: EJNMMI Radiopharmacy and Chemistry, Vuosikerta 4, Nro 1, 05.08.2019.

Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

TY - JOUR

T1 - Improved synthesis of [18F] fallypride and characterization of a Huntington’s disease mouse model, zQ175DN KI, using longitudinal PET imaging of D2/D3 receptors

AU - Huhtala, Tuulia

AU - Poutiainen, Pekka

AU - Rytkönen, Jussi

AU - Lehtimäki, Kimmo

AU - Parkkari, Teija

AU - Kasanen, Iiris

AU - Airaksinen, Anu J.

AU - Koivula, Teija

AU - Sweeney, Patrick

AU - Kontkanen, Outi

AU - Wityak, John

AU - Dominiquez, Celia

AU - Park, Larry C.

PY - 2019/8/5

Y1 - 2019/8/5

N2 - Dopamine receptors are involved in pathophysiology of neuropsychiatric diseases, including Huntington’s disease (HD). PET imaging of dopamine D2 receptors (D2R) in HD patients has demonstrated 40% decrease in D2R binding in striatum, and D2R could be a reliable quantitative target to monitor disease progression. A D2/3R antagonist, [18F] fallypride, is a high-affinity radioligand that has been clinically used to study receptor density and occupancy in neuropsychiatric disorders. Here we report an improved synthesis method for [18F]fallypride. In addition, high molar activity of the ligand has allowed us to apply PET imaging to characterize D2/D3 receptor density in striatum of the recently developed zQ175DN knock-in (KI) mouse model of HD.

AB - Dopamine receptors are involved in pathophysiology of neuropsychiatric diseases, including Huntington’s disease (HD). PET imaging of dopamine D2 receptors (D2R) in HD patients has demonstrated 40% decrease in D2R binding in striatum, and D2R could be a reliable quantitative target to monitor disease progression. A D2/3R antagonist, [18F] fallypride, is a high-affinity radioligand that has been clinically used to study receptor density and occupancy in neuropsychiatric disorders. Here we report an improved synthesis method for [18F]fallypride. In addition, high molar activity of the ligand has allowed us to apply PET imaging to characterize D2/D3 receptor density in striatum of the recently developed zQ175DN knock-in (KI) mouse model of HD.

KW - 317 Pharmacy

KW - 116 Chemical sciences

U2 - 10.1186/s41181-019-0071-6

DO - 10.1186/s41181-019-0071-6

M3 - Article

VL - 4

JO - EJNMMI Radiopharmacy and Chemistry

JF - EJNMMI Radiopharmacy and Chemistry

SN - 2365-421X

IS - 1

ER -