The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8 ) is researched.Related Products of 56621-48-8.Prante, Olaf; Tietze, Rainer; Hocke, Carsten; Loeber, Stefan; Huebner, Harald; Kuwert, Torsten; Gmeiner, Peter published the article 《Synthesis, Radiofluorination, and In Vitro Evaluation of Pyrazolo[1,5-a]pyridine-Based Dopamine D4 Receptor Ligands: Discovery of an Inverse Agonist Radioligand for PET》 about this compound( cas:56621-48-8 ) in Journal of Medicinal Chemistry. Keywords: pyrazolopyridine arylpiperazinylmethyl preparation radiofluorination dopamine receptor radioligand. Let’s learn more about this compound (cas:56621-48-8).
A series of fluoro-substituted analogs structurally derived from the aminomethyl-substituted pyrazolo[1,5-a]pyridine lead compounds FAUC 113 and FAUC 213 were synthesized and evaluated as high-affinity D4 receptor (D4R) ligands (Ki = 1.3-28 nM). The para-fluoroethoxy-substituted derivatives I and II revealed an outstanding D4 subtype selectivity of more than 3 orders of magnitude over both congeners D2 and D3 combined with inverse agonism at D4R. The corresponding 18F-labeled radioligands revealed high serum stability in vitro and log P values of 2-3. In vitro rat brain autoradiog. showed specific binding of [18F]-II in distinct brain regions, including the gyrus dentate of the hippocampus, that were inhibited by both eticlopride (65-80%) and the selective D4R antagonist 10 (78-93%). The observed binding pattern was mainly consistent with the known D4R distribution in the rat brain. Thus, [18F]-II (FAUC F41) represents a potential radioligand for studying the D4R in vivo by positron emission tomog. (PET).
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Ether | (C2H5)2O – PubChem