• Register
Forgot Password

If you have forgotten your password you can enter your email here and get a temporary password sent to your email.


Leaving Community

Are you sure you want to leave this community? Leaving the community will revoke any permissions you have been granted in this community.


Sensory neuron-specific GPCR Mrgprs are itch receptors mediating chloroquine-induced pruritus.

The cellular and molecular mechanisms mediating histamine-independent itch in primary sensory neurons are largely unknown. Itch induced by chloroquine (CQ) is a common side effect of this widely used antimalarial drug. Here, we show that Mrgprs, a family of G protein-coupled receptors expressed exclusively in peripheral sensory neurons, function as itch receptors. Mice lacking a cluster of Mrgpr genes display significant deficits in itch induced by CQ but not histamine. CQ directly excites sensory neurons in an Mrgpr-dependent manner. CQ specifically activates mouse MrgprA3 and human MrgprX1. Loss- and gain-of-function studies demonstrate that MrgprA3 is required for CQ responsiveness in mice. Furthermore, MrgprA3-expressing neurons respond to histamine and coexpress gastrin-releasing peptide, a peptide involved in itch sensation, and MrgprC11. Activation of these neurons with the MrgprC11-specific agonist BAM8-22 induces itch in wild-type but not mutant mice. Therefore, Mrgprs may provide molecular access to itch-selective neurons and constitute novel targets for itch therapeutics.

Pubmed ID: 20004959


  • Liu Q
  • Tang Z
  • Surdenikova L
  • Kim S
  • Patel KN
  • Kim A
  • Ru F
  • Guan Y
  • Weng HJ
  • Geng Y
  • Undem BJ
  • Kollarik M
  • Chen ZF
  • Anderson DJ
  • Dong X



Publication Data

December 24, 2009

Associated Grants

  • Agency: NIAMS NIH HHS, Id: AR056318
  • Agency: NIDDK NIH HHS, Id: DK074480
  • Agency: NHLBI NIH HHS, Id: HL038095
  • Agency: NINDS NIH HHS, Id: NS048499
  • Agency: NINDS NIH HHS, Id: NS054791
  • Agency: NINDS NIH HHS, Id: R01 NS054791
  • Agency: NINDS NIH HHS, Id: R01 NS054791-01A1
  • Agency: NINDS NIH HHS, Id: R01 NS054791-02
  • Agency: NINDS NIH HHS, Id: R01 NS054791-03
  • Agency: NINDS NIH HHS, Id: R01 NS054791-04
  • Agency: NEI NIH HHS, Id: T32 EY017203
  • Agency: Howard Hughes Medical Institute, Id:

Mesh Terms

  • Animals
  • Capsaicin
  • Chloroquine
  • Ganglia, Spinal
  • Histamine
  • Humans
  • Mice
  • Pruritus
  • Receptors, G-Protein-Coupled
  • Sensory Receptor Cells