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Lacivita E, Leopoldo M, Masotti AC, Inglese C, Berardi F, Perrone R, Ganguly S, Jafurulla M, Chattopadhyay A: Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure. J Med Chem. 2009 Dec 10;52(23):7892-6.
A series of "long-chain" 1-(2-methoxyphenyl) piperazine derivatives containing an environment-sensitive fluorescent moiety (4-amino-1,8-naphthalimide, 4-dimethylaminophthalimide, dansyl) was synthesized. The compounds displayed very high to moderate 5-HT (1A) receptor affinity and good fluorescence properties. 6-Amino-2-[5-[4-(2-methoxyphenyl)-1-piperazinyl] pentyl]-1H-benz [de] isoquin oline-1,3 (2H)-dione (4) combined very high 5-HT (1A) receptor affinity (K (i) = 0.67 nM), high fluorescence emission in CHCl (3), and undetectable fluorescence emission in aqueous solution. It was evaluated for its ability to visualize 5-HT (1A) receptors overexpressed in CHO cells by fluorescence microscopy. |
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