Selective fluorescent ligands for pharmacological receptors

Abstract

Receptor-selective fluorescent ligands have come into increasing use as scientific tools for the study of receptor physiology and pathophysiology at the cellular and even the subcellular level. Furthermore, they are being increasingly investigated as tools in drug discovery research. In both cases, techniques employing receptor-selective fluorescent ligands have proved to be complementary to, and in several cases even superior to, the traditional-radioligand based techniques. increasing costs and public concerns associated with radioactive isotope use and dispersal are also making the use of fluoresecent ligands more attractive in research and diagnostic use. With the increasing rate of discovery of new receptors and receptor subtypes and newer more potent and/or selective receptor ligands and drugs, there will be an accompanying need for the design and development of new highly potent and selective fluorescent ligands to aid in the investigation of the physiological and pathophysiological functions of these new receptors and also in the development of drugs acting specifically at these receptors. This review presents a background of development of selected fluorescent ligands, primarily those for small molecule and small peptide based ligands. o 1994 \ViIey-Li<s, Inc.

Fluorescent GPCR Ligands as New Tools in Pharmacology

“…Several review papers have been published up to 2000 describing a number of novel fluorescent ligands [1,12,13]. Herein, we review the results recently described in the literature (since 2000) in the field of the fluorescent GPCR small, non-peptide ligands according to the affinity for receptors to which they bind as well as to the type of fluorophores that have been used to tag the molecules (e.g.…”

Development and validation of fluorescent receptor assays based on the human recombinant estrogen receptor subtypes alpha and beta

“…Since the development of receptor assays in the 1970s, mostly radioactive labelled compounds were used as a ligand. Due to practical limitations related to the use of radioactivity, nonradioactive ligands, such as autofluorescent ligands or fluorescent-labeled ligands, have been used for different receptor-types [13][14][15].…”

Competitive MS Binding Assays for Dopamine D2Receptors Employing Spiperone as a Native Marker

“…3 H, 35 S or 125 I) or with a fluorescent moiety is used. [1][2][3][4] However, both methods have serious drawbacks. The synthesis of radioligands is, in general, expensive, and special safety precautions have to be observed when radioligand-binding assays are performed.…”

“…Most frequently, either a ligand labelled with a radioisotope (e.g. 3 H, 35 S or 125 I) or with a fluorescent moiety is used. [1][2][3][4] However, both methods have serious drawbacks.…”