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. Author manuscript; available in PMC: 2012 Jan 1.

Published in final edited form as: Adv Pharmacol. 2011;61:187–220. doi: 10.1016/B978-0-12-385526-8.00007-2

Fig. 1 — Allosteric modulators of the A₁ AR, including benzoylthiophene derivatives (A) and an amiloride derivative lacking subtype selectivity (B), and of the A_2A AR (C). The miminal, principal pharmacophore of the class of aroylthiophenes as A₁ AR PAMs is shown in a box on PD81,723 2. Compound 11 is a bitopic modulator, containing an agonist (6-phenyl substituted adenosine) moiety. In part (D) there are recently published 2-amino-3-substituted thiophene derivatives as allosteric modulators for A₁ adenosine receptors. Numbering of ring substitutions is shown for compound 1.

Fig. 1 — Allosteric modulators of the A₁ AR, including benzoylthiophene derivatives (A) and an amiloride derivative lacking subtype selectivity (B), and of the A_2A AR (C). The miminal, principal pharmacophore of the class of aroylthiophenes as A₁ AR PAMs is shown in a box on PD81,723 2. Compound 11 is a bitopic modulator, containing an agonist (6-phenyl substituted adenosine) moiety. In part (D) there are recently published 2-amino-3-substituted thiophene derivatives as allosteric modulators for A₁ adenosine receptors. Numbering of ring substitutions is shown for compound 1.