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J Med Chem. 2008 Mar 13;51(5):1492-5. doi: 10.1021/jm7013919. Epub 2008 Feb 13.

N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands.

Author information

1
Dipartimento Farmaco-Chimico, Universita degli Studi di Bari, bari, Italy. lacivita@farmchim.uniba.it

Abstract

We here report on the design, synthesis, binding affinities, and fluorescent properties of a series of serotonin 5-HT 1A receptor ligands, with N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamine structure. Several of the new ligands displayed nanomolar affinity at 5-HT 1A receptor and good fluorescent properties. In particular, derivative 24 showed a favorable combination of 5-HT 1A receptor affinity ( K i = 0.4 nM), Stokes shift (excitation wavelength = 381 nm, emission wavelength = 455 nm), and quantum yield in ethanol (Phi = 0.45).

PMID:
18269229
DOI:
10.1021/jm7013919
[Indexed for MEDLINE]

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