Selected GPCRs that function through Gq and/or Gs pathways

Their agonists were reported with EC50 value.

GPCRSignalingFunctionsAgonistsEC50 or Kd
GPER1 (Gpr30)GqActivated by estradiol and functions via Gq signaling (Revankar et al., 2005). A selective agonist G1 is beneficial in myocardial ischemia reperfusion injury model (Bologa et al., 2006; Deschamps and Murphy, 2009).G12 nM (Bologa et al., 2006)
BDKRB1GqBDKRB1 is a Gq-coupled GPCR, whereas BDKRB2 signals through Gq and Gi. In vivo activation of BDKRB2 attenuated kidney fibrosis (Schanstra et al., 2002).Bradykinin3.26 nM (Wiernas et al., 1997)
DRD1GsPleuropulmonary fibrosis was linked to the long-term use of dopamine agonist pergolide in patients with Parkinson (Tintner et al., 2005).A689302.5 nM (DeNinno et al., 1991)
PTGER2GqPGE2 is a potent bioactive eicosanoid that strongly inhibits fibroblast proliferation, migration, and collagen secretion (Bozyk and Moore, 2011).PGE2PTGER1, 25 nM; PTGER2, 13 nM; PTGER3, 3 nM; PTGER4, 3 nM (Markovič et al., 2017)
PTGER4GsTCS2510 is a highly selective EP4 agonist.TCS25102.5 nM (Billot et al., 2003)
TBXA2RGq/Gs/G12/13U46619 is a potent and stable TBXA2R agonist.U4661935 nM (Coleman et al., 1981)
OXTRGqOxytocin is a peptide hormone and neurotransmitter signaling through OXTR and Gq pathways (Gimpl and Fahrenholz, 2001). WAY-267464 is a potent, selective, nonpeptide OXTR agonist.Oxytocin9.0–10.8 nM (Gruber et al., 2012) 9.0 nM (Ring et al., 2010)
EDNRBGqEndothelin 3 is a vasoconstrictor that preferentially binds to EDNRB.Endothelin 31 nM (Sumner et al., 1992)
F2RL1 (PAR2)Gq/GiPAR2 is implicated in lung, kidney, liver, and cardiac fibrosis (Palygin et al., 2016; Shearer et al., 2016; Sun et al., 2017; Friebel et al., 2019).AC264613∼31 nM (Gardell et al., 2008)
S1PR3GqS1PR3 KO mice has attenuated inflammation and fibrosis upon bleomycin-induced lung injury (Murakami et al., 2014).CYM554172–132 nM (Jo et al., 2012)
HTR2B (5-HT2B receptor)GqSerotonin fibrosis in human and treatment of fenfluramine, a serotonin releasing agent, causes cardiac valve fibrosis in patients with obesity (Roth, 2007). 5-HT2B activation mediates valvular fibroblasts activation.BW723C865-HT2B, 1.1 nM; 5-HT2C, 93.3 nM (Porter et al., 1999)
HTR7 (5-HT7 receptor)GsAS-19 is a potent 5-HT7 receptor agonist.AS190.83 nM (Perez-Garcia and Meneses, 2005)
MC1RGsMC1R is anti-inflammatory and has been implicated in several inflammatory diseases.BMS47053916.8 nM (Kang et al., 2006)
  • EDNRB, endothelin receptor B; KO, knockout.