P2X purinoceptors are the ATP-gated cation channels which consist of two transmembrane domains, a large extracellular loop contained ATP-binding site, and intracellular carboxyl and amino termini. They are activated by binding to extracellular ATP thereby mediating the permeability of cation such as Ca2+, Na+, and K+. P2X purinoceptors are widely expressed in most cell types including neurons, leukocytes, blood platelets, smooth muscle cells. They are involved in the physiological processes, including mediating fast ATP-dependent synaptic transmission and action potential propagation, contraction of smooth muscle cells, platelet aggregation, macrophage activation, mediation of nociception, and apoptosis. In addition, P2X purinoceptors can act as the therapeutic target for some diseases. It has been reported that P2X7 inhibitor is a potential drug for the treatment of rheumatoid arthritis and chronic obstructive pulmonary disease.
Here show P2X purinoceptors in humans including P2RX1-P2RX7. The P2X purinoceptors subtypes are expressed on specific cell types. For example, P2RX1 is particularly expressed in smooth muscle cells, P2RX2 is widely present in the nervous system. However, more than one subunit can be also expressed in most cell types. For example, it is found that P2X2 and P2X3 subunits are commonly co-expressed in sensory neurons.
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