1414941-73-3Relevant articles and documents
Synthesis, radiolabeling and in vivo evaluation of [11C](R)-1- [4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, a potential PET radioligand for the 5-HT7receptor
Hansen, Hanne D.,Lacivita, Enza,Di Pilato, Pantaleo,Herth, Matthias M.,Lehel, Szabolcs,Ettrup, Anders,Andersen, Valdemar L.,Dyssegaard, Agnete,De Giorgio, Paola,Perrone, Roberto,Berardi, Francesco,Colabufo, Nicola Antonio,Niso, Mauro,Knudsen, Gitte M.,Leopoldo, Marcello
, p. 152 - 163 (2014/05/06)
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) phenyl]piperazin-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, [11C](R)-16 entered the pig brain and displayed reversible tracer kinetics. Pretreatment with the 5-HT7receptor 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-HT7receptor in vivo but it may serve as a lead compound for the design of novel 5-HT7receptor PET radioligands.
NEW 1-ARYLPIPERAZINIC LIGANDS OF 5-HT7 RECEPTOR AND USE THEREOF
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Page/Page column 18, (2012/12/13)
The invention relates to a new class of compounds able to inhibit with high affinity and selectivity the 5-HT7 receptor. The invention also relates to the utilization of such compounds as medicaments useful in the treatment and prevention of 5-HT7 receptor relating disorders of the central nervous system. The invention also relates to the isotopically labeled compounds for use in vivo diagnosis or imaging of a 5-HT7 condition.
