Adenosine A2B receptor

This integral membrane protein stimulates adenylate cyclase activity in the presence of adenosine. This protein also interacts with netrin-1, which is involved in axon elongation. ==Gene==

The gene is located near the Smith-Magenis syndrome region on chromosome 17. ==Ligands==

Research into selective A2B ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A2B-selective compounds have now been developed, and research into their potential therapeutic applications is ongoing. Agonists • BAY 60-6583 • NECA (N-ethylcarboxamidoadenosine) • (S)-PHPNECA - high affinity and efficacy at A2B, but poor selectivity over other adenosine receptor subtypes • LUF-5835 • LUF-5845 - partial agonist Antagonists and inverse agonists • Compound 38: antagonist, high affinity and good subtype selectivity • ISAM-R56A: non-xanthinic selective antagonist (Ki = 3.49 nM). • ISAM-R324A: Soluble and metabolically stable non-xanthinic selective antagonist (Ki = 6.10 nM). • ATL-801 • CVT-6883 • MRS-1706 • MRS-1754 • OSIP-339,391 • PSB-603: xanthinic antagonist • PSB-0788: xanthinic antagonist • PSB-1115: xanthinic antagonist • PSB-1901: xanthinic antagonist with picomolar potency == References ==