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

Lacivita, Enza ; Masotti, Anna Carmela ; Jafurulla, Md. ; Saxena, Roopali ; Rangaraj, Nandini ; Chattopadhyay, Amitabha ; Colabufo, Nicola A. ; Berardi, Francesco ; Perrone, Roberto ; Leopoldo, Marcello (2010) Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT1A receptors Bioorganic & Medicinal Chemistry Letters, 20 (22). pp. 6628-6632. ISSN 0960-894X

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bmcl.2010.09.027

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.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:5-HT1A Receptor; Fluorescence; SAR; 1-Arylpiperazine; Confocal Laser Scanning Microscopy
ID Code:85731
Deposited On:05 Mar 2012 13:32
Last Modified:05 Mar 2012 13:32

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