Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT 1A receptors

…, AC Masotti, M Jafurulla, R Saxena, N Rangaraj…

Index: Lacivita, Enza; Masotti, Anna Carmela; Jafurulla, Md.; Saxena, Roopali; Rangaraj, Nandini; Chattopadhyay, Amitabha; Colabufo, Nicola A.; Berardi, Francesco; Perrone, Roberto; Leopoldo, Marcello Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6628 - 6632

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Citation Number: 9

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= 35nM) and was able to label specifically the human 5-HT1A receptor stably expressed in CHO cells visualized using ...