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N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists. 2006

Ran Zhu, and Cynthia R Frazier, and Joel Linden, and Timothy L Macdonald
Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA.

A series of N6-ethyl-2-alkynyl NECA (5'-N-ethylcarboxamidoadenosine) analogs were synthesized and their binding affinity with the four human adenosine receptors was evaluated. One of the compounds ZR1121 shows high affinity with hA3 receptor and its selectivity over hA1 receptor is 1-2 log orders greater than IB-MECA or Cl-IB-MECA, the currently employed selective A3 agonists.

UI MeSH Term Description Entries
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
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
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D058909 Adenosine A3 Receptor Agonists Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
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

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