BIOMAT Database Logo BIOMAT Database Logo

Binding affinity of adenosine receptor agonists and antagonists at human cloned A3 adenosine receptors. 1998

K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
Dipartimento di Medicina Clinica e Sperimentale-Sezione di Farmacologia, Università degli Studi di Ferrara, Italy.

The A3 adenosine receptor is one of the four adenosine receptors which have thus far been identified. Cloning of the A3 receptor from animal species such as rat, sheep and human has shown that there are interspecies differences in its peripheral distribution, and binding affinity for various adenosine receptor ligands. The adenosine derivative, 4-aminobenzyl-5'-N-methylcarboxamidoadenosine (AB-MECA), is a potent A3 receptor agonist which is used as a reference drug. In this report we have characterized the binding of selected adenosine receptor agonists and antagonists to HEK 293 cells transfected with the human A3 adenosine receptor using [125I]AB-MECA as radioligand. HE-NECA and NECA were the most potent compounds showing Ki values in the low nanomolar range, while the recently discovered non-xanthine A2A receptor antagonists ZM 241385, SCH 58261 and SCH 63390 showed affinity values in the micromolar range. These data further indicate the need to examine the affinity of new adenosine receptor ligands directly in human A3 receptors.

UI MeSH Term Description Entries
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D011799 Quinazolines A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring. Quinazoline
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D003001 Cloning, Molecular The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells. Molecular Cloning
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000241 Adenosine A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter. Adenocard,Adenoscan
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
D014162 Transfection The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES. Transfections
D014227 Triazines Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES. Triazine,Benzotriazines

Related Publications

K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors.
August 1999, Naunyn-Schmiedeberg's archives of pharmacology,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
NUCLEOSIDE PRODRUGS OF A3 ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS.
January 2006, Collection of Czechoslovak chemical communications,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
A binding kinetics study of human adenosine A3 receptor agonists.
July 2018, Biochemical pharmacology,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
Medicinal chemistry of the A3 adenosine receptor: agonists, antagonists, and receptor engineering.
January 2009, Handbook of experimental pharmacology,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
Affinity prediction on A3 adenosine receptor antagonists: the chemometric approach.
November 2011, Bioorganic & medicinal chemistry,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
Cloned adenosine A3 receptors: pharmacological properties, species differences and receptor functions.
August 1994, Trends in pharmacological sciences,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
A3 adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.
January 2022, European journal of medicinal chemistry,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
A3 Adenosine Receptors: Protective vs. Damaging Effects Identified Using Novel Agonists and Antagonists.
January 1998, Drug development research,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
Therapeutic Potential of Agonists and Antagonists of A1, A2a, A2b and A3 Adenosine Receptors.
January 2019, Current pharmaceutical design,
K Varani, and B Cacciari, and P G Baraldi, and S Dionisotti, and E Ongini, and P A Borea
Development of potent and selective human A3 adenosine receptor agonists.
January 2005, Nucleic acids symposium series (2004),
Copied contents to your clipboard!