1. Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives
- Author
-
Claudia Martini, Marco Macchia, Antonio Pellegrini, F Salvetti, Silvia Barontini, Mahmoud Hamdan, Paola Soldam, Antonio Lucacchini, Federico Calvani, and Marco Gesi
- Subjects
Agonist ,Stereochemistry ,medicine.drug_class ,Clinical Biochemistry ,Pharmaceutical Science ,Adenosine-5'-(N-ethylcarboxamide) ,Biochemistry ,Chemical synthesis ,Radioligand Assay ,Structure-Activity Relationship ,Drug Discovery ,Fluorescence microscope ,medicine ,Animals ,Molecular Biology ,Alkyl ,Fluorescent Dyes ,chemistry.chemical_classification ,Dansyl Compounds ,Chemistry ,Organic Chemistry ,Receptors, Purinergic P1 ,Adenosine receptor ,Fluorescence ,Adenosine ,Rats ,Cerebellar cortex ,Molecular Medicine ,medicine.drug - Abstract
New fluorescent ligands for adenosine receptors are described; these compounds were obtained by the insertion, in the N 6 position of NECA (a potent adenosine agonist), of dansylaminoalkyl moieties with alkyl spacers of increasing carbon chain length (from 3 to 12). Among them, the compound with a C6 alkyl spacer proved to be the most interesting one, showing a marked selectivity for the A 1 receptor subtype; furthermore, in fluorescence microscopy assays it proved to be able to visualize and localize this receptor subtype at the level of the molecular layer of the rat cerebellar cortex.
- Published
- 1999