Mas-Related GPCR Family Subtypes and Products

What Are Mas-Related Receptors?

The Mas-related G protein-coupled receptor (MRGPR) family is a unique Class A GPCR subfamily primarily expressed in peripheral sensory neurons and immune cells. These receptors are increasingly recognized for their roles in pain, itch (pruritus), and neuroimmune signaling, making them attractive targets for therapeutic discovery.

Mas-related receptors (MRGPRs) are a diverse group of GPCRs originally identified through homology to the Mas proto-oncogene. This family includes both the well-characterized human MRGPRX subtypes and related receptors such as MRGD (MRGPRD) and MAS1, which share structural and evolutionary relationships. While several members remain orphan receptors, others respond to neuropeptides and small endogenous ligands involved in sensory and inflammatory pathways.

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Mas-Related Receptor Information

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MRGX1

MRGX2

MAS1

MRGX1 (MAS-related GPR member X1) is also known as SNSR4 (sensory neuron-specific G-protein-coupled receptor 4). It can be potently activated by enkephalins including BAM22 and BAM(8-22). MRGX1 receptor is expressed solely in small diameter primary sensory neurons. This restricted expression pattern is of considerable therapeutic interest because small nociceptors transmit chronic pain messages.

MRGX1 (MAS-related GPR member X1) is also known as SNSR4 (sensory neuron-specific G-protein-coupled receptor 4). It can be potently activated by enkephalins including BAM22 and BAM(8-22). MRGX1 receptor is expressed solely in small diameter primary sensory neurons. This restricted expression pattern is of considerable therapeutic interest because small nociceptors transmit chronic pain messages.

MRGX2 (MAS-related GPR member X2) is a receptor for cortistatin. It is probably involved in the function of nociceptive neurons and regulation of nociceptor function and/or development, including the sensation or modulation of pain. Cortistatin-14, a high potency agonist at the receptor, has biological functions including sleep regulation, locomotor activity and cortical function.

MRGPRs exhibit significant sequence diversity and species-specific expansion. In humans, the MRGPRX subfamily (MRGPRX1–X4) is the most well characterized. MRGD (MRGPRD) is a conserved receptor expressed in sensory neurons and implicated in mechanosensation and pain signaling, while MAS1, the prototypical member of the family, is associated with cardiovascular and protective signaling pathways through ligands such as angiotensin-(1–7). Together, these receptors span roles in nociception, itch, inflammation, and broader physiological regulation.

Mas-Related Cell Lines

Mas-relatedMRGX1humanCHO dhfr-Gαqi5C1256DC1256MC1256
MRGX1humanHEK293TC1256aDC1256aMC1256a
MRGX2humanHEK293T Gαqi5C1257DC1257MC1257
MRGX2humanHEK293TC1257aDC1257aMC1257a
MRGX2humanHEK293TC1257bDC1257bMC1257b
MRGX2rhesus monkeyCHO-K1Cpr1257-1DCpr1257-1MCpr1257-1
MRGX2humanHEK293T β-Arrestin2CA1257aBA2DCA1257aBA2MCA1257aBA2
MRGX2humanHEK293T β-Arrestin2CA1257bBA2DCA1257bBA2MCA1257bBA2
MRGX4humanHEK293TC1259DC1259MC1259
MAS1humanHEK293TC1225DC1225MC1225
MRGDhumanHEK293Tc1366Dc1366Mc1366

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