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American Chemical Society, Journal of Medicinal Chemistry, 5(51), p. 1492-1495, 2008

DOI: 10.1021/jm7013919

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N-[ω-[4-(2-Methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as High-Affinity Fluorescent 5-HT1A Receptor Ligands

Journal article published in 2008 by Enza Lacivita ORCID, Marcello Leopoldo
This paper was not found in any repository; the policy of its publisher is unknown or unclear.
This paper was not found in any repository; the policy of its publisher is unknown or unclear.

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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).