Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 79, Issue -, Pages 152-163Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.066
Keywords
5-HT7 receptor; PET; Radioligand; Arylpiperazine; SB-269970
Categories
Funding
- Intra European Fellowship [MC-IEF-275329]
- Toyota foundation
- John & Birthe Meyer Foundation
- Lundbeck Foundation [R90-2011-7722, R62-2010-5364] Funding Source: researchfish
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In the search for a novel serotonin 7 (5-HT7) receptor PET radioligand we synthesized and evaluated a new series of biphenylpiperazine derivatives in vitro. Among the studied compounds, (R)-1-[4-[2-(4-methoxyphenyl)phenyllpiperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol ((R)-16), showed the best combination of affinity, selectivity, and lipophilicity, and was thus chosen for carbon-11 labelling and evaluation in pigs. After intravenous injection, [C-11](R)-16 entered the pig brain and displayed reversible tracer kinetics. Pretreatment with the 5-HT7 receptor selective antagonist SB-269970 (1) resulted in limited decrease in the binding of [11C](R)-16, suggesting that this radioligand is not optimal for imaging the brain 5-HT7 receptor in vivo but it may serve as a lead compound for the design of novel 5-HT7 receptor PET radioligands. (C) 2014 Elsevier Masson SAS. All rights reserved.
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