Neurokinin 1 receptor
The Neurokinin 1 receptor (NK1R), also known as the substance P receptor, is a G protein-coupled receptor that binds the neuropeptide substance P. It is encoded by the TACR1 gene in humans and is predominantly involved in the transmission of pain information into the central nervous system.
Function[edit | edit source]
The Neurokinin 1 receptor is part of the tachykinin receptor group that also includes NK2 and NK3 receptors. These receptors are activated by a family of neuropeptides known as tachykinins. Substance P is the most prominent member of this family and is responsible for the activation of NK1R. Upon binding of substance P, NK1R initiates a cascade of cellular responses involving phospholipase C, inositol trisphosphate, and diacylglycerol which lead to changes in calcium ion levels within the cell.
NK1R plays a crucial role in various physiological processes including pain perception, stress response, and inflammation. It is also implicated in the regulation of mood and anxiety, making it a potential target for the treatment of depression and anxiety disorders.
Clinical Significance[edit | edit source]
The activation of NK1R by substance P is associated with the transmission of pain and the induction of inflammatory responses. As such, NK1R antagonists have been studied for their potential use in treating conditions such as depression, anxiety, nausea, and vomiting, particularly in the context of chemotherapy-induced nausea and vomiting (CINV). Additionally, these antagonists are being explored for their therapeutic roles in pain management and inflammatory diseases.
Pharmacology[edit | edit source]
Several NK1R antagonists have been developed, including drugs like aprepitant and fosaprepitant, which are used clinically to prevent chemotherapy-induced nausea and vomiting. These antagonists work by blocking the binding of substance P to NK1R, thereby inhibiting the receptor's function.
Genetics[edit | edit source]
The gene encoding the Neurokinin 1 receptor, TACR1, is located on chromosome 2p13. It consists of multiple exons that undergo alternative splicing, resulting in different isoforms of the receptor.
See also[edit | edit source]
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