Lacivita, Enza ; Leopoldo, Marcello ; Masotti, Anna Carmela ; Inglese, Carmela ; Berardi, Francesco ; Perrone, Roberto ; Ganguly, Sourav ; Jafurulla, Md. ; Chattopadhyay, Amitabha (2009) Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure Journal of Medicinal Chemistry, 52 (23). pp. 7892-7896. ISSN 0022-2623
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Official URL: http://pubs.acs.org/doi/abs/10.1021/jm900706d
Related URL: http://dx.doi.org/10.1021/jm900706d
Abstract
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-HT1A receptor affinity and good fluorescence properties.6-Amino-2-[5-[4-(2-methoxyphenyl)-1-piperazinyl]pentyl]-1H-benz[de]isoquinoline-1,3(2H)-dione (4) combined very high 5-HT1A receptor affinity (Ki = 0.67 nM), high fluorescence emission in CHCl3, and undetectable fluorescence emission in aqueous solution. It was evaluated for its ability to visualize 5-HT1A receptors overexpressed in CHO cells by fluorescence microscopy.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to American Chemical Society. |
| ID Code: | 85757 |
| Deposited On: | 05 Mar 2012 13:30 |
| Last Modified: | 05 Mar 2012 13:30 |
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