Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging was written by Andres, Jose-Ignacio;De Angelis, Meri;Alcazar, Jesus;Iturrino, Laura;Langlois, Xavier;Dedeurwaerdere, Stefanie;Lenaerts, Ilse;Vanhoof, Greet;Celen, Sofie;Bormans, Guy. And the article was included in Journal of Medicinal Chemistry in 2011.Name: 6-Methyl-2-pyridinemethanol This article mentions the following:
We have recently reported the phosphodiesterase 10A (PDE10A) inhibitor 2-[4-[1-(2-[18F]fluoroethyl)-4-pyridin-4-yl-1H-pyrazol-3-yl]-phenoxymethyl]-quinoline (I) as a promising candidate for in vivo imaging using positron emission tomog. (PET). We now describe the synthesis and biol. evaluation of a series of related pyridinyl analogs II (R1 = FCH2CH2, FCH2CH2CH2, F3CCH2; R2 = 3,5-di-Me, 5-methoxy, 6-bromo, etc.) that exhibit high potency and selectivity as PDE10A inhibitors. The most interesting compounds were injected in rats to measure their levels of PDE10A occupancy through an in vivo occupancy assay. The 3,5-dimethylpyridine derivative II (R1 = FCH2CH2, R2 = 3,5-di-Me) and the 5-methoxypyridine derivative II (R1 = FCH2CH2, R2 = 5-methoxy) showed a comparable level of occupancy to that of I. Because these derivatives showed lower in vitro activity and are slightly less lipophilic than I, we hypothesized that they could behave as better PET imaging ligands. Compounds II (R1 = 18FCH2CH2, R2 = 3,5-dimethyl; R1 = 18FCH2CH2, R2 = 5-methoxy; R1 = FCH2CH2, R2 = 5-11CH3O) were radio synthesized and subjected to biodistribution studies in rats for a preliminary evaluation as candidate PET radioligands for in vivo imaging of PDE10A in the brain. In the experiment, the researchers used many compounds, for example, 6-Methyl-2-pyridinemethanol (cas: 1122-71-0Name: 6-Methyl-2-pyridinemethanol).
6-Methyl-2-pyridinemethanol (cas: 1122-71-0) belongs to alcohols. Similar to water, an alcohol can be pictured as having an sp3 hybridized tetrahedral oxygen atom with nonbonding pairs of electrons occupying two of the four sp3 hybrid orbitals. The most common reactions of alcohols can be classified as oxidation, dehydration, substitution, esterification, and reactions of alkoxides.Name: 6-Methyl-2-pyridinemethanol
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