Huang, Yunsheng published the artcileSynthesis and Quantitative Structure-Activity Relationships of N-(1-Benzylpiperidin-4-yl)phenylacetamides and Related Analogs as Potent and Selective σ1 Receptor Ligands, HPLC of Formula: 33697-81-3, the publication is Journal of Medicinal Chemistry (1998), 41(13), 2361-2370, database is CAplus and MEDLINE.
A series of N-(1-benzylpiperidin-4-yl)phenylacetamide derivatives was synthesized and evaluated for affinity at Ï1 and Ï2 receptors. Most of these compounds showed a high affinity for Ï1 receptors and a low to moderate affinity for Ï2 receptors. The unsubstituted compound N-(1-benzylpiperidin-4-yl)phenylacetamide displayed a high affinity and selectivity for Ï1 receptors (Ki values of 3.90 nM for Ï1 receptors and 240 nM for Ï2 receptors). The influence of substitutions on the phenylacetamide aromatic ring on binding at both the Ï1 and Ï2 receptor has been examined through Hansch-type quant. structure-activity relationship (QSAR) studies. In general, all 3-substituted compounds, except for the OH group, had a higher affinity for both Ï1 and Ï2 receptors when compared with the corresponding 2- and 4-substituted analogs. The selectivity for Ï1 receptors displayed a trend of 3 > 2 â?4 for Cl, Br, F, NO2, and OMe substituted analogs. Halogen substitution on the aromatic ring generally increased the affinity for Ï2 receptors while maintaining a similar affinity for Ï1 receptors. Substitution with electron-donating groups, such as OH, OMe, or NH2, resulted in weak or negligible affinity for Ï2 receptors and a moderate affinity for Ï1 receptors. The compds tested had no affinity for dopamine D2 (IC50 > 10,000 nM) and D3 (IC50 > 10,000 nM) receptors. The nanomolar binding affinity and high selectivity for Ï1 receptors suggest that these compounds may be developed as potential radiotracers for positron emission tomog. or single photon emission computerized tomog. imaging studies.
Journal of Medicinal Chemistry published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, HPLC of Formula: 33697-81-3.
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