IC50: 67 nM for P2X2/3

Adenosine-5'-diphosphate is an agonist of purinergic receptors.

Purinergic receptors, also known as purinoceptors, are a family of plasma membrane molecules that are found in almost all mammalian tissues. Within the field of purinergic signalling, these receptors have been implicated in learning and memory, locomotor and feeding behavior, and sleep. More specifically, purinergic receptors are involved in several cellular functions, such as proliferation and migration of neural stem cells, vascular reactivity, apoptosis and cytokine secretion.

In vitro: Adenosine 5'-diphosphate (ADP) is an adenine nucleotide having two phosphate groups esterified to the sugar moiety at the 5’ position. ADP is formed through dephosphorylation of adenosine 5’-triphosphate (ATP) by ATPases and can be converted back to ATP by ATP synthases. ADP can also be metabolized to adenosine 5’-monophosphate (AMP) and 2’-deoxyadenosine 5’-diphosphate (dADP). ADP can modulate several receptors, such as activating certain purinergic receptors and inhibiting others, inhibiting rat ecto-5’nucleotidase (Ki = 0.91 nM), as well as regulating the phosphorylation status of AMP-activated protein kinase [1, 2].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

References:
1.  Azran, S.,Frster, D.,Danino, O., et al. Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists. J. Med. Chem. 56(12), 4938-4952 (2013).
2.  Jarvis, M.F.,Bianchi, B.,Uchic, J.T., et al. [3H]A-317491, a novel high-affinity non-nucleotide antagonist that specifically labels human P2X2/3 and P2X3 receptors. Journal of Pharmacology and Experimental Therapeutics 310(1), 407-416 (2004).