- Copper-Mediated Radiofluorination of Arylstannanes with [18F]KF
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A copper-mediated nucleophilic radiofluorination of aryl- and vinylstannanes with [18F]KF is described. This method is fast, uses commercially available reagents, and is compatible with both electron-rich and electron-deficient arene substrates. This method has been applied to the manual synthesis of a variety of clinically relevant radiotracers including protected [18F]F-phenylalanine and [18F]F-DOPA. In addition, an automated synthesis of [18F]MPPF is demonstrated that delivers a clinically validated dose of 200 ± 20 mCi with a high specific activity of 2400 ± 900 Ci/mmol.
- Makaravage, Katarina J.,Brooks, Allen F.,Mossine, Andrew V.,Sanford, Melanie S.,Scott, Peter J. H.
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supporting information
p. 5440 - 5443
(2016/11/04)
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- Structural Insights into 5-HT1A/D4 Selectivity of WAY-100635 Analogues: Molecular Modeling, Synthesis, and in Vitro Binding
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The resurgence of interest in 5-HT1A receptors as a therapeutic target requires the existence of highly selective 5-HT1A ligands. To date, WAY-100635 has been the prototypical antagonist of these receptors. However, this compound als
- Dilly, Sébastien,Liégeois, Jean-Fran?ois
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p. 1324 - 1331
(2016/08/02)
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- 5HT1A ANTAGONIST USEFUL FOR IN VIVO IMAGING
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The present invention provides a novel compound of formula (I) useful for in vivo imaging of 5-HT1 A receptors in a subject. Also provided by the present invention is a precursor compound useful in the preparation of the compound of the inventi
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Page/Page column 21; 22
(2013/03/26)
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- NOVEL SYNTHESIS METHOD
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The present invention relates to a method of making compounds having affinity for the 1 A subtype of the serotonin receptor, i.e. 5HT1A. The method of the present invention provides advantages over the known methods of synthesis. The compounds
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Page/Page column 17
(2013/04/10)
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- EFFICIENT SYNTHETIC METHOD OF 18F-MEFWAY PRECURSOR
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The present invention relates a novel method for preparing an 18F-mefway precursor. The present invention provides an efficient synthetic method of an 18F-mefway precursor, which comprises an improved the acid chloride coupling react
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Page/Page column 6
(2012/06/16)
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- Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors
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The selectivity for 5-HT1A versus D4 receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tet
- Mangin, Floriane,Dilly, Sebastien,Joly, Benoit,Scuvee-Moreau, Jacqueline,Evans, Jon,Setola, Vincent,Roth, Bryan L.,Liegeois, Jean-Francois
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supporting information; experimental part
p. 4550 - 4554
(2012/08/08)
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- Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N -{2-[4-(2-methoxyphenyl)piperazin-1-yl] ethyl}- N -(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor
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Here we describe the design, synthesis, and pharmacological profile of 5-HT1A receptor ligands related to 1 (WAY-100635). The cyclohexyl moiety in 1 and its O-desmethylated analogue 3 were replaced by the bridgehead iodinated bridge-fused rings: adamantyl, cubyl, bicyclo[2.2.2]octyl, or bicyclo[2.2.1]heptyl. All analogues displayed a (sub)nanomolar affinity for the 5-HT1A receptor in vitro. Compounds 6b and 7b appeared to be selective for this receptor over other relevant receptors and could easily be iodinated with radioactive iodine-123. In humane hepatocytes, [ 123I]6b showed a low propensity for amide hydrolysis and a stable carbon-iodine bond. The biodistribution of [123I]6b and [ 123I]7b in rats revealed that the carbon-iodine bond was also stable in vivo. Unfortunately, the brain uptake and the specificity for both radioligands were significantly lower than those of the parent molecule 1. In conclusion, the designed tracers are not suitable for SPECT imaging.
- Al Hussainy, Rana,Verbeek, Joost,Van Der Born, Dion,Braker, Anton H.,Leysen, Josée E.,Knol, Remco J.,Booij, Jan,Herscheid
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supporting information; experimental part
p. 3480 - 3491
(2011/07/07)
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- Tc-labeled arylpiperazine derivatives for imaging serotonin receptor
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The present invention relates to Tc-labeled arylpiperazine derivatives for imaging serotonin receptor and, more particularly, to arylpiperazine derivatives coupled with MAMA-disulfide, N2S2 or dimethyl-N2S2 chel
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Page/Page column 6
(2008/06/13)
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- Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers
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Molecular imprinting produces network polymers with recognition sites for imprint molecules. The high binding affinity and selectivity in conjunction with the polymers' physical robustness positions molecular imprinted polymers (MIPs) as candidates for us
- O'Connor, Naphtali A.,Paisner, David A.,Huryn, Donna,Shea, Kenneth J.
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p. 1680 - 1689
(2007/10/03)
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- Highly efficient synthesis and imaging studies of an arylpiperazine derivative as a 5-HT1A receptor imaging agent
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A novel and straightforward microwave synthesis of a new arylpiperazine derivative 3 which has an N2S2 moiety has been developed and radiolabeled with an optimum radionuclide of technetium in the presence of a borohydride exchange re
- Park, Sang Hyun,Gwon, Hui Jeong,Jang, Seung Ho,Lee, Hyosun
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p. 1304 - 1305
(2008/02/05)
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- Pre-clinical Development of a Radioligand for Studies of Central 5-HT1A Receptors in Vivo - [11C]WAY-100635
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Syntheses of N-(2-(1-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl))-N-(2-pyridyl)-cyclohexanecarboxamide (WAY-100635) and its desmethyl and descyclohexylcarbonyl analogues are described. WAY-100635 has properties that favour its development as a radioligand f
- Pike, Victor W.,McCarron, Julie A.,Hume, Susan P.,Ashworth, Sharon,Opacka-Juffry, Jolanta,et al.
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p. 208 - 227
(2007/10/03)
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