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

Research output: Contribution to journalArticle

2 Citations (Scopus)

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 languageEnglish
Pages (from-to)1298-1308
Number of pages11
JournalChemistry and Biodiversity
Volume11
Issue number9
DOIs
StatePublished - 1 Sep 2014

Fingerprint

Dopamine D4 Receptors
Positron emission tomography
Positron-Emission Tomography
Rodentia
Brain
Eye Proteins
Pineal Gland
Dopamine Receptors
Neurology
Rats
Dopamine
Central Nervous System
Availability
Ligands
Proteins
N-(2-(4-(3-cyanopyridin-2-yl)piperazin-1-yl)ethyl)-3-methoxybenzamide
In Vitro Techniques

Keywords

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

Cite this

Leopoldo, Marcello ; Selivanova, Svetlana V. ; Müller, Adrienne ; Lacivita, Enza ; Schetz, John A. ; Ametamey, Simon M. / 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. In: Chemistry and Biodiversity. 2014 ; Vol. 11, No. 9. pp. 1298-1308.
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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.",
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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; Lacivita, Enza; Schetz, John A.; Ametamey, Simon M.

In: Chemistry and Biodiversity, Vol. 11, No. 9, 01.09.2014, p. 1298-1308.

Research output: Contribution to journalArticle

TY - JOUR

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AU - Lacivita, Enza

AU - Schetz, John A.

AU - Ametamey, Simon M.

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