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

Enza Lacivita; Anna Carmela Masotti; Md Jafurulla; Roopali Saxena; Nandini Rangaraj; Amitabha Chattopadhyay; Nicola A Colabufo; Francesco Berardi; Roberto Perrone; Marcello Leopoldo

doi:10.1016/j.bmcl.2010.09.027

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

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6628-32. doi: 10.1016/j.bmcl.2010.09.027. Epub 2010 Sep 21.

Authors

Enza Lacivita¹, Anna Carmela Masotti, Md Jafurulla, Roopali Saxena, Nandini Rangaraj, Amitabha Chattopadhyay, Nicola A Colabufo, Francesco Berardi, Roberto Perrone, Marcello Leopoldo

Affiliation

¹ Università degli Studi di Bari A. Moro, Dipartimento Farmaco-Chimico, via Orabona, 4, 70125 Bari, Italy.

PMID: 20888762
DOI: 10.1016/j.bmcl.2010.09.027

Abstract

The 5-HT(1A) 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-HT(1A) receptor. The new 1-arylpiperazine-based red-emitting fluorescent compound 6 displayed good binding affinity at the 5-HT(1A) receptor (K(i)=35 nM) and was able to label specifically the human 5-HT(1A) receptor stably expressed in CHO cells visualized using confocal laser scanning microscopy.

MeSH terms

Animals
CHO Cells
Cricetinae
Cricetulus
Fluorescent Dyes / chemistry*
Humans
Ligands
Microscopy, Confocal
Microscopy, Fluorescence
Receptor, Serotonin, 5-HT1A / chemistry*

Substances

Fluorescent Dyes
Ligands
Receptor, Serotonin, 5-HT1A