Synthesis and receptor binding properties of fluoro-and iodo-substituted high-affinity. sigma.-receptor ligands: identification of potential PET and SPECT. sigma.- …

B De Costa, L Radesca, C Dominguez…

文献索引：Costa, Brian de; Radesca, Lilian; Dominguez, Celia; Paolo, Lisa Di; Bowen, Wayne D. Journal of Medicinal Chemistry, 1992 , vol. 35, # 12 p. 2221 - 2230

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被引用次数: 19

摘要

SPECT compounds 1-[3-fluo~(l-propyl~ l-4 [2-(3, 4di~ orophenyl~ ethyllpi~~ e (6)(Ki= 4.24 nM,[%](+)-3--PPP), l-(5-fluoro-l-pentyl)-4-[2-(3, 4-dichlorophenyl) ethyl] piperazine (7)(Ki= 0.86 nM,[3H](+)-3-PPP), and 1-(3-iodo-1-propyl) 4 [2-(3, 4dichlorophenyl) ethyl] piperazine (9)(Ki= 1.32 nM,[3H](+)-3-PPP). Compound 7 was synthesized via N-alkylation of 1-(3, 4dichlorophenylacetyl) piperazine (19) with 11, followed by AlH3 reduction. Ligands 6 and ...