Mas-related G protein-coupled receptor X1 (MRGPRX1)

Mas-related G protein-coupled receptor X1 (MRGPRX1) is a **primate-specific G protein-coupled receptor** highly expressed in a subset of primary sensory neurons, particularly nociceptors in the peripheral nervous system. MRGPRX1 is involved in the modulation of pain and itch sensation. Its restricted expression makes it an attractive therapeutic target for the development of novel analgesic and antipruritic agents, as it may allow pain inhibition with fewer off-target effects compared to other systems. MRGPRX1 can be activated by specific endogenous and synthetic peptides, as well as positive allosteric modulators, which modulate intracellular calcium channels to suppress pain signaling. Therapeutic efforts focus on targeting MRGPRX1 for conditions such as neuropathic pain, with research ongoing to identify selective and potent modulators for clinical development[1][2][3][4][8][9].

Other names

Mas-related G protein–coupled receptor member X1MRGPRX1MAS-related GPR X1

Agonists activate MRGPRX1, leading to inhibition of high-voltage-activated (HVA) calcium channels in sensory neurons, reducing pain transmission[2][3][8]. Positive allosteric modulators (PAMs) increase the efficacy and/or potency of agonists at MRGPRX1, enhancing pain inhibitory effects[2][3][4][8].