2-Chloro-N6-cyclopentyladenosine (CCPA), A1 agonist

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The Adenosine A1 Receptor Adenosine Receptor A2a and Adenosine A3 Receptor commonly referred to as A1 A2a and A3AR belong to the G protein-coupled receptor (GPCR) family. These receptors allow cells to respond to extracellular adenosine. The molecular mass of these receptors can vary: generally A1 is around 36-38 kDa A2a is about 45 kDa and A3AR ranges between 36-38 kDa. These receptors have widespread expression in various tissues. A1 receptors are prominently found in the brain heart and adipose tissues. A2a receptors are largely seen in the brain spleen and immune cells. A3AR is present in the testis brain and also a bit in the lung.

Biological function summary

These receptors mediate cellular responses to adenosine leading to changes in cellular activity. They are not part of a single complex but may interact with other proteins as part of signaling pathways. A1 receptors typically lead to an inhibitory effect by reducing cyclic AMP levels. A2a receptors however usually result in a stimulatory effect by increasing cyclic AMP levels. A3AR can have either effect depending on cellular context. These activities influence physiological processes like heart rate neurotransmitter release and immune response modulation.

Pathways

These receptors play significant roles in cardiovascular and neurological pathways. The A1 receptor participates importantly in the cardiac adenosine pathway influencing heart contractility and rhythm by working with proteins like Gi protein. The A2a receptor has a notable role in the dopaminergic signaling pathway within the central nervous system interacting with proteins such as dopamine receptors. A3AR is involved in inflammatory pathways sometimes linking with proteins like NF-kB to modulate immune cell activity.

The dysfunction or abnormal regulation of these adenosine receptors is linked to cardiovascular diseases and neurological disorders. For instance the A1 receptor's role in cardiac function connects it to conditions like myocardial ischemia. The A2a receptor's involvement in dopaminergic pathways relates to neurodegenerative diseases such as Parkinson's disease with interactions involving dopamine receptors. A3AR's role in inflammation associates it with disorders like asthma often involving proteins in inflammatory pathways.