In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[11C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D4 receptors, in rodents

Marcello Leopoldo; Svetlana V. Selivanova; Adrienne Müller; Enza Lacivita; John A. Schetz; Simon M. Ametamey

doi:10.1002/cbdv.201400178

In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[¹¹C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D₄ receptors, in rodents

Marcello Leopoldo, Svetlana V. Selivanova, Adrienne Müller, Enza Lacivita, John A. Schetz, Simon M. Ametamey

School of Biomedical Sciences

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3 Scopus citations

Abstract

The D₄ dopamine receptor belongs to the D₂-like family of dopamine receptors, and its exact regional distribution in the central nervous system is still a matter of considerable debate. The availability of a selective radioligand for the D₄ receptor with suitable properties for positron emission tomography (PET) would help resolve issues of D₄ receptor localization in the brain, and the presumed diurnal change of expressed protein in the eye and pineal gland. We report here on in vitro and in vivo characteristics of the high-affinity D₄ receptor-selective ligand N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[¹¹C]methoxybenzamide ([¹¹C]2) in rat. The results provide new insights on the in vitro properties that a brain PET dopamine D₄ radioligand should possess in order to have improved in vivo utility in rodents.

Original language	English
Pages (from-to)	1298-1308
Number of pages	11
Journal	Chemistry and Biodiversity
Volume	11
Issue number	9
DOIs	https://doi.org/10.1002/cbdv.201400178
State	Published - 1 Sep 2014

Keywords

Dopamine D receptors
G-Protein-coupled receptors (GPCR)
Piperazine, 1-aryl-
Positron emission tomography (PET)
Rodent

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10.1002/cbdv.201400178

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Leopoldo, M., Selivanova, S. V., Müller, A., Lacivita, E., Schetz, J. A., & Ametamey, S. M. (2014). In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[¹¹C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D₄ receptors, in rodents. Chemistry and Biodiversity, 11(9), 1298-1308. https://doi.org/10.1002/cbdv.201400178

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title = "In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[11C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D4 receptors, in rodents",

abstract = "The D4 dopamine receptor belongs to the D2-like family of dopamine receptors, and its exact regional distribution in the central nervous system is still a matter of considerable debate. The availability of a selective radioligand for the D4 receptor with suitable properties for positron emission tomography (PET) would help resolve issues of D4 receptor localization in the brain, and the presumed diurnal change of expressed protein in the eye and pineal gland. We report here on in vitro and in vivo characteristics of the high-affinity D4 receptor-selective ligand N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[11C]methoxybenzamide ([11C]2) in rat. The results provide new insights on the in vitro properties that a brain PET dopamine D4 radioligand should possess in order to have improved in vivo utility in rodents.",

keywords = "Dopamine D receptors, G-Protein-coupled receptors (GPCR), Piperazine, 1-aryl-, Positron emission tomography (PET), Rodent",

author = "Marcello Leopoldo and Selivanova, {Svetlana V.} and Adrienne M{\"u}ller and Enza Lacivita and Schetz, {John A.} and Ametamey, {Simon M.}",

note = "Publisher Copyright: Copyright {\textcopyright} 2014 Verlag Helvetica Chimica Acta AG, Z{\"u}rich.",

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doi = "10.1002/cbdv.201400178",

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Leopoldo, M, Selivanova, SV, Müller, A, Lacivita, E, Schetz, JA & Ametamey, SM 2014, 'In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[¹¹C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D₄ receptors, in rodents', Chemistry and Biodiversity, vol. 11, no. 9, pp. 1298-1308. https://doi.org/10.1002/cbdv.201400178

In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[¹¹C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D₄ receptors, in rodents. / Leopoldo, Marcello; Selivanova, Svetlana V.; Müller, Adrienne et al.
In: Chemistry and Biodiversity, Vol. 11, No. 9, 01.09.2014, p. 1298-1308.

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

TY - JOUR

T1 - In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[11C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D4 receptors, in rodents

AU - Leopoldo, Marcello

AU - Selivanova, Svetlana V.

AU - Müller, Adrienne

AU - Lacivita, Enza

AU - Schetz, John A.

AU - Ametamey, Simon M.

PY - 2014/9/1

Y1 - 2014/9/1

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AB - The D4 dopamine receptor belongs to the D2-like family of dopamine receptors, and its exact regional distribution in the central nervous system is still a matter of considerable debate. The availability of a selective radioligand for the D4 receptor with suitable properties for positron emission tomography (PET) would help resolve issues of D4 receptor localization in the brain, and the presumed diurnal change of expressed protein in the eye and pineal gland. We report here on in vitro and in vivo characteristics of the high-affinity D4 receptor-selective ligand N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[11C]methoxybenzamide ([11C]2) in rat. The results provide new insights on the in vitro properties that a brain PET dopamine D4 radioligand should possess in order to have improved in vivo utility in rodents.

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KW - G-Protein-coupled receptors (GPCR)

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SN - 1612-1872

VL - 11

SP - 1298

EP - 1308

JO - Chemistry and Biodiversity

JF - Chemistry and Biodiversity

IS - 9

ER -

In vitro and in vivo evaluation of N-{2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[¹¹C]methoxybenzamide, a positron emission tomography (PET) radioligand for dopamine D₄ receptors, in rodents

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