Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives. 1998

M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
GlaxoWellcome Medicines Research Center, Verona, Italy. mmacchia@farm.unipi.it

New fluorescent ligands for adenosine receptors are described; these compounds were obtained by the insertion, in the N6 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 A1 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 rate cerebellar cortex.

UI MeSH Term Description Entries
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D003619 Dansyl Compounds Compounds that contain a 1-dimethylaminonaphthalene-5-sulfonyl group. Dimethylaminonaphthalenesulfonyl Compounds,Compounds, Dansyl,Compounds, Dimethylaminonaphthalenesulfonyl
D005456 Fluorescent Dyes Chemicals that emit light after excitation by light. The wave length of the emitted light is usually longer than that of the incident light. Fluorochromes are substances that cause fluorescence in other substances, i.e., dyes used to mark or label other compounds with fluorescent tags. Flourescent Agent,Fluorescent Dye,Fluorescent Probe,Fluorescent Probes,Fluorochrome,Fluorochromes,Fluorogenic Substrates,Fluorescence Agents,Fluorescent Agents,Fluorogenic Substrate,Agents, Fluorescence,Agents, Fluorescent,Dyes, Fluorescent,Probes, Fluorescent,Substrates, Fluorogenic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D018047 Receptors, Purinergic P1 A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra). Adenosine Receptors,P1 Purinoceptors,Purinergic P1 Receptors,Receptors, Adenosine,Adenosine Receptor,P1 Purinoceptor,Receptor, Purinergic P1,P1 Receptor, Purinergic,P1 Receptors, Purinergic,Purinergic P1 Receptor,Purinoceptor, P1,Purinoceptors, P1,Receptor, Adenosine
D019830 Adenosine-5'-(N-ethylcarboxamide) A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. 5'-N-Ethylcarboxamidoadenosine,N-Ethylcarboxamidoadenosine,NECA,Adenosine-5'-N-ethyluronamide,N6-Ethyl-carboxamido Adenosine,5' N Ethylcarboxamidoadenosine,Adenosine 5' N ethyluronamide,Adenosine, N6-Ethyl-carboxamido,N Ethylcarboxamidoadenosine,N6 Ethyl carboxamido Adenosine

Related Publications

M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
January 2003, Nucleosides, nucleotides & nucleic acids,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
May 2003, Biochemical pharmacology,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
June 1974, Chemical & pharmaceutical bulletin,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
December 2001, Archives of pharmacal research,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
January 2004, Nucleosides, nucleotides & nucleic acids,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
March 1996, Journal of medicinal chemistry,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
February 1996, Journal of medicinal chemistry,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
June 1965, Chemische Berichte,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
July 2004, Bulletin of mathematical biology,
M Macchia, and F Salvetti, and S Barontini, and F Calvani, and M Gesi, and M Hamdan, and A Lucacchini, and A Pellegrini, and P Soldani, and C Martini
December 1991, Journal of medicinal chemistry,
Copied contents to your clipboard!