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Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT1A receptors

by: Enza Lacivita, Anna C. Masotti, Md Jafurulla, Roopali Saxena, Nandini Rangaraj, Amitabha Chattopadhyay, Nicola A. Colabufo, Francesco Berardi, Roberto Perrone, Marcello Leopoldo
Bioorganic & Medicinal Chemistry Letters, Vol. 20, No. 22. (21 November 2010), pp. 6628-6632, doi:10.1016/j.bmcl.2010.09.027  Key: citeulike:7883343

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Abstract

The 5-HT1A receptor subtype is the most thoroughly studied serotonin receptor subtype. We report here the design, synthesis and characterization of two new fluorescent ligands for the 5-HT1A receptor. The new 1-arylpiperazine-based red-emitting fluorescent compound 6 displayed good binding affinity at the 5-HT1A receptor (Ki = 35 nM) and was able to label specifically the human 5-HT1A receptor stably expressed in CHO cells visualized using confocal laser scanning microscopy.


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