Mas-related G-protein coupled receptor member X1

Definition:

Orphan receptor. Probably involved in the function of nociceptive neurons. May regulate nociceptor function and/or development, including the sensation or modulation of pain. Potently activated by enkephalins including BAM22 (bovine adrenal medulla peptide 22) and BAM (8-22). BAM22 is the most potent compound and evoked a large and dose-dependent release of intracellular calcium in stably transfected cells. G(alpha)q proteins are involved in the calcium-signaling pathway. Activated by the antimalarial drug, chloroquine. May mediate chloroquine-induced itch, in a histamine-independent manner.

References:

[1]. Qin Liu, et al. Sensory neuron-specific GPCR Mrgprs are itch receptors mediating chloroquine-induced pruritus. Cell. 2009 Dec 24;139(7):1353-65. [Content Brief]

[2]. Paola M C Lembo, et al. Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs. Nat Neurosci. 2002 Mar;5(3):201-9. [Content Brief]

[3]. Daniel Heller, et al. Novel Probes Establish Mas-Related G Protein-Coupled Receptor X1 Variants as Receptors with Loss or Gain of Function. J Pharmacol Exp Ther. 2016 Feb;356(2):276-83. [Content Brief]

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