Abstract
The regulatory actions of adenosine are mediated via four subtypes
of G protein-coupled receptors distinguished as A1, A2A, A2B and
A3 receptors. Their presence on basically every cell makes them an
interesting target for the pharmacological intervention in many pathophysiological
situations. A large number of ligands have been synthesized over
the last two decades and provide agonists and antagonists that are
more or less selective for the known receptor subtypes. In addition,
many radioligands are available in tritiated or radioiodinated form.
The comparative pharmacological characterization of all four human
adenosine receptor subtypes revealed that some of the compounds thought
to be selective from data in other species have unexpected potencies
at human receptors. As a result, compounds that exhibit high affinity
to only one subtype are an exception. Although the selection of ligands
is immense, it is less than satisfying for most subtypes of adenosine
receptors.
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