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1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3.

作者信息

Perrone R, Berardi F, Leopoldo M, Tortorella V, Fornaretto M G, Caccia C, McArthur R A

机构信息

Dipartimento Farmaco-chimico, Università di Bari, Italy.

出版信息

J Med Chem. 1996 Aug 2;39(16):3195-202. doi: 10.1021/jm960087s.

DOI:10.1021/jm960087s
PMID:8759642
Abstract

The synthesis and binding profile on 5-HT1A, 5-HT2, D-1, D-2, alpha 1, and alpha 2 receptors of the N-4 long-chain arylpiperazines 22-40 are reported, where an amino or amido function is inserted into the intermediate chain linked to the alpha position of the tetralin nucleus. Unlike the buspirone analogues, for the amido derivatives studied in this paper, the terminal amide function of long-chain piperazines is not important for 5-HT1A receptor affinity binding, and its removal yields high-affinity 5-HT1A receptor agents.

摘要

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