| Primary Identifier | IPR027338 | Type | Family |
| Short Name | MRGPCRX1/MRGPCRX2 |
| description | Members of the mas-related receptor family (also known as oncogene-like MAS and mas-related G-protein coupled receptor MRG) have been implicated in the development, regulation and function of nociceptive neurons, specifically in the modulation of pain. Most members are orphaned, with no endogeneous ligand identified. Of the human mas-related GPCRs, four (MRGPRD, MRGPRE, MRGPRF and MRGPRG) are also found in rodents, whereas MRGPRX1, MRGPRX2, MRGPRX3 and MRGPRX4 are found exclusively in primates. Certain rodent MRGs have been reported to respond to adenine []and to RF-amide peptides, including neuropeptide FF [, ], but the relevance of these findings to man is unclear. MRGs are expressed predominantly in small diameter sensory neurons of the dorsal root ganglia, where there is emerging evidence that they may be mediators of histamine-independent itch [, ].This entry represents Mas-related G protein-coupled receptor X1 and X2.Mas-related G protein-coupled receptor X1 (MRGPRX1) is thought to be involved with nociceptor function and development, and in the modulation of pain. The receptor is currently orphaned, no specific endogenous ligand having been identified. However, it may potently be activated by enkephalins: BAM22 evokes a large and dose-dependent release of intracellular calcium in cells stably transfected with the receptor []. Mas-related G protein-coupled receptor X2 (MRGPRX2) is thought to be involved with nociceptor function and development, and directly involved in the modulation of pain. The receptor is currently orphaned, no specific endogenous ligand having been identified. However, it may be activated by neuropeptides: stimulation by cortistatin-14 in receptor-expressing cells potently increases intracellular Ca2 [, ]. MRGPRX2 is also thought to be a human PAMP-12 receptor that regulates catecholamine secretion from adrenal glands []. |
