| Title | N-(4-[(18)F]-fluoropyridin-2-yl)-N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}carboxamides as analogs of WAY100635. New PET tracers of serotonin 5-HT(1A) receptors. |
| Publication Type | Journal Article |
| Year of Publication | 2014 |
| Authors | García G, Abet V, Alajarín R, Álvarez-Builla J, Delgado M, García-García L, Bascuñana-Almarcha P, Peña-Salcedo C, Kelly J, Pozo MA |
| Journal | Eur J Med Chem |
| Volume | 85 |
| Pagination | 795-806 |
| Date Published | 2014 Oct 06 |
| ISSN | 1768-3254 |
| Keywords | Animals, Binding, Competitive, Brain, Fluorine Radioisotopes, Male, Piperazines, Positron-Emission Tomography, Pyridines, Radioactive Tracers, Rats, Rats, Sprague-Dawley, Receptor, Serotonin, 5-HT1A |
| Abstract | N-(4-[(18)F]-Fluoropyridin-2-yl)-N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-carboxamides were prepared by labeling their 4-nitropyridin-2-yl precursors through nitro substitution by the (18)F anion. In vitro and in vivo tests showed that the cyclohexanecarboxamide derivative is a reversible, selective and high affinity 5-HT1A receptor antagonist (IC50 = 0.29 nM, ki = 0.18 nM) with high brain uptake, slow brain clearance and stability to defluorination when compared with conventional standards. This PET radioligand is a promising candidate for an improved in vivo quantification of 5-HT1A receptors in neuropsychiatric disorders. |
| DOI | 10.1016/j.ejmech.2014.07.096 |
| Alternate Journal | Eur J Med Chem |
| PubMed ID | 25171752 |
Related Institute:
Molecular Imaging Innovations Institute (MI3)