Synthesis of arylpiperazines with a terminal naphthothiazole group and their evaluation on 5-HT, DA and a receptor

The synthesis, affinities for 5-HT 1A, 5-HT 2, D, D 2, α 1 and α 2 receptors and structure-activity relationships are described for a series of arylpiperazines substituted on the N-4 atom with an ω-(2-naphthothiazole)alkyl chain. The best affinity for 5-HT 1A receptors was obtained for 1-(2-methoxyp...

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Bibliographic Details
Published in:European journal of medicinal chemistry 1997-09, Vol.32 (9), p.739-746
Main Authors: Perrone, R, Berardi, F, Colabufo, NA, Tortorella, V, Fornaretto, MG, Caccia, C, McArthur, RA
Format: Article
Language:English
Subjects:
5-HT 1A
antipsychotic
arylpiperazine
D 2/α ligand
EPS
naphthothiazole
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Summary:The synthesis, affinities for 5-HT 1A, 5-HT 2, D, D 2, α 1 and α 2 receptors and structure-activity relationships are described for a series of arylpiperazines substituted on the N-4 atom with an ω-(2-naphthothiazole)alkyl chain. The best affinity for 5-HT 1A receptors was obtained for 1-(2-methoxyphenyl)piperazine derivatives with IC 50 values in the range 3.2–12 nM; however, for all the reported compounds mixed 5-HT 1A/D 2/α affinities were observed.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(97)88916-7