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- W2004241446 abstract "Abstract A new generation of antidepressant agents could be represented by compounds with mixed activity as serotonin transporter (SERT) inhibitors and 5-HT1A receptor antagonists. We report here on the synthesis and evaluation of SERT and 5-HT1A receptor affinity of long-chain arylpiperazines obtained either by modifying 6-nitroquipazine into a long-chain arylpiperazine or by inserting a modified 6-nitroquipazine moiety or other structures endowed with SERT affinity into a long-chain arylpiperazine with 5-HT1A affinity. Among the compounds studied, 2-[4-(2-methoxyphenyl)piperazin-1-yl]-N-(6-nitro-2-quinolyl)ethylamine (21) and 1-(5-bromo-1,2,3,4-tetrahydronaphthalen-1-yl)-3-[4-(2-methoxyphenyl)-piperazin-1-yl]-1-propanone (24) showed good affinity values for SERT and 5-HT1A receptors (SERT: Ki (inhibition constant) = 71.8 and 62.8 nm; 5-HT1A Ki = 14.2 and 0.82 nm, respectively)." @default.
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- W2004241446 date "2005-10-01" @default.
- W2004241446 modified "2023-10-17" @default.
- W2004241446 title "Design and synthesis of long-chain arylpiperazines with mixed affinity for serotonin transporter (SERT) and 5-HT1A receptor" @default.
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- W2004241446 doi "https://doi.org/10.1211/jpp.57.10.0011" @default.
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