Calcitonin gene-related peptide receptor

Calcitonin gene-related peptide receptor (CGRP receptor) is a G protein-coupled receptor that in humans is encoded by the CALCRL gene. This receptor is found in various tissues throughout the body, such as the nervous system and cardiovascular system, and is involved in the transmission of pain and the dilation of blood vessels.

Structure[edit | edit source]

The CGRP receptor is a complex of a G protein-coupled receptor called CALCRL, a receptor activity-modifying protein (RAMP1), and a receptor component protein (RCP). The CALCRL protein interacts with RAMP1 to form the CGRP receptor, which can then interact with the RCP to mediate signal transduction.

Function[edit | edit source]

The CGRP receptor is primarily known for its role in the transmission of pain. When activated by the neuropeptide CGRP, it can lead to the sensation of pain. This has made the CGRP receptor a target for the development of new pain medications.

In addition to its role in pain, the CGRP receptor is also involved in the dilation of blood vessels. This is because CGRP is a potent vasodilator, and its interaction with the CGRP receptor can lead to the relaxation of smooth muscle cells in the walls of blood vessels, leading to their dilation.

Clinical significance[edit | edit source]

Because of its roles in pain and vasodilation, the CGRP receptor has been the target of a number of drugs. These include triptans, which are used to treat migraines, and monoclonal antibodies, which are being developed to treat conditions such as migraine and cluster headaches.