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Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N′-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent
- Source :
- Bioorganic & Medicinal Chemistry Letters. 21:6820-6823
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- N-(2-Benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine (6, σ(1)K(i)=2.6 nM) was radiolabeled with fluorine-18 to provide a potential σ(1) receptor radioligand for use in positron emission tomography (PET). Radiofluorination of the appropriate tosylate precursor furnished [(18)F]6 with a specific activity of 45 GBq/μmol, in an average radiochemical yield of 18% and greater than 98% radiochemical purity. MicroPET imaging in Papio hamadryas baboon brain revealed [(18)F]6 uptake consistent with σ receptor distribution, and specificity for σ receptors was demonstrated in a haloperidol pre-treated animal. [(18)F]6 possesses suitable properties for PET imaging of σ(1) receptors, and further investigation of this σ(1) receptor tracer is warranted.
- Subjects :
- Fluorine Radioisotopes
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Piperazines
chemistry.chemical_compound
In vivo
Drug Discovery
medicine
Radioligand
Animals
Receptors, sigma
Receptor
Molecular Biology
medicine.diagnostic_test
Organic Chemistry
Radiochemistry
Brain
Pet imaging
Piperazine
chemistry
Positron emission tomography
Positron-Emission Tomography
Yield (chemistry)
Molecular Medicine
Specific activity
Radiopharmaceuticals
Papio
Nuclear chemistry
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....398be3554baf7304fc17dbf639d674a6