Adenosine A Receptor and Ligand Molecular Modeling.

This symposium provided a forum for presentations by the relevant groups on ligand design and ligand binding on the adenosine A, receptor. Agreement appears to exist that the "N-C" model of ligand binding to the receptor is the preferred mode. A consensus has not yet been reached on the actual placement of the ligand in the receptor and the exact amino acids which interact in its binding.

Molecular Characterization of A(1) and A(2a) Adenosine Receptors.

Detailed amino acid sequence analyses of A(1) and A(2a) adenosine receptors were assembled by analogy to other G-protein-coupled receptors and correlated with pharmacological observations. Sites for phosphorylation, palmitoylation, and sodium binding have been proposed. Striatal A(2a) receptors from human and other species were photoaffinity-labeled using the selective, radioiodinated agonist PAPA-APEC.