Gene Symbol: Hcar1
Description: hydrocarboxylic acid receptor 1
Alias: Gpr81, hydroxycarboxylic acid receptor 1, G-protein coupled receptor 81
Species: mouse
Products:     Hcar1

Top Publications

  1. Cai T, Ren N, Jin L, Cheng K, Kash S, Chen R, et al. Role of GPR81 in lactate-mediated reduction of adipose lipolysis. Biochem Biophys Res Commun. 2008;377:987-91 pubmed publisher
    ..Here we employ pharmacological and genetic approaches to show that GPR81, an orphan G-protein-coupled receptor with relatively restricted expression in the adipose tissues, functions as a ..
  2. Ahmed K, Tunaru S, Tang C, Muller M, Gille A, Sassmann A, et al. An autocrine lactate loop mediates insulin-dependent inhibition of lipolysis through GPR81. Cell Metab. 2010;11:311-9 pubmed publisher
    ..Here we show that lactate activates the G protein-coupled receptor GPR81, which is expressed in adipocytes and mediates antilipolytic effects through G(i)-dependent inhibition of adenylyl ..
  3. Hoque R, Farooq A, Ghani A, Gorelick F, Mehal W. Lactate reduces liver and pancreatic injury in Toll-like receptor- and inflammasome-mediated inflammation via GPR81-mediated suppression of innate immunity. Gastroenterology. 2014;146:1763-74 pubmed publisher
    ..We examined whether lactate and the lactate receptor, Gi-protein-coupled receptor 81 (GPR81), regulate TLR induction of signal 1 and limit inflammasome activation and organ injury...
  4. Errea A, Cayet D, Marchetti P, Tang C, Kluza J, Offermanns S, et al. Lactate Inhibits the Pro-Inflammatory Response and Metabolic Reprogramming in Murine Macrophages in a GPR81-Independent Manner. PLoS ONE. 2016;11:e0163694 pubmed publisher
    ..Recently, lactate was shown to signal through the G protein coupled receptor 81 (GPR81) and to thus modulate inflammatory processes...
  5. Liu C, Wu J, Zhu J, Kuei C, Yu J, Shelton J, et al. Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81. J Biol Chem. 2009;284:2811-22 pubmed publisher
    ..Here we show that GPR81, an orphan G-protein-coupled receptor highly expressed in fat, is in fact a sensor for lactate...
  6. Jeninga E, Bugge A, Nielsen R, Kersten S, Hamers N, Dani C, et al. Peroxisome proliferator-activated receptor gamma regulates expression of the anti-lipolytic G-protein-coupled receptor 81 (GPR81/Gpr81). J Biol Chem. 2009;284:26385-93 pubmed publisher
    ..Here we identified the anti-lipolytic human G-protein-coupled receptor 81 (GPR81), GPR109A, and the (human-specific) GPR109B genes as well as the mouse Gpr81 and Gpr109A genes as novel TZD-..
  7. Wanders D, Graff E, Judd R. Effects of high fat diet on GPR109A and GPR81 gene expression. Biochem Biophys Res Commun. 2012;425:278-83 pubmed publisher
    GPR109A (PUMA-G, NIACR1, HCA(2)) and GPR81 (HCA(1)) are G protein-coupled receptors located predominantly on adipocytes that mediate anti-lipolytic effects...
  8. Sakurai T, Davenport R, Stafford S, Grosse J, Ogawa K, Cameron J, et al. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing. Eur J Pharmacol. 2014;727:1-7 pubmed publisher
    b>GPR81, which exhibits a high degree of homology with GPR109a, has been recently identified as a lactate receptor...
  9. Shen Z, Jiang L, Yuan Y, Deng T, Zheng Y, Zhao Y, et al. Inhibition of G protein-coupled receptor 81 (GPR81) protects against ischemic brain injury. CNS Neurosci Ther. 2015;21:271-9 pubmed publisher
    Lactates accumulate in ischemic brains. G protein-coupled receptor 81 (GPR81) is an endogenous receptor for lactate. We aimed to explore whether lactate is involved in ischemic injury via activating GPR81...

More Information


  1. Madaan A, Nadeau Vallée M, Rivera J, Obari D, Hou X, Sierra E, et al. Lactate produced during labor modulates uterine inflammation via GPR81 (HCA1). Am J Obstet Gynecol. 2017;216:60.e1-60.e17 pubmed publisher
    ..Aside from its metabolic function, lactate has been shown to activate a G protein-coupled receptor, GPR81, reported to regulate inflammation...
  2. Ranganathan P, Shanmugam A, Swafford D, Suryawanshi A, Bhattacharjee P, Hussein M, et al. GPR81, a Cell-Surface Receptor for Lactate, Regulates Intestinal Homeostasis and Protects Mice from Experimental Colitis. J Immunol. 2018;200:1781-1789 pubmed publisher
    ..In this study, we report that signaling by GPR81, a receptor for lactate, in colonic dendritic cells and macrophages plays an important role in suppressing colonic ..
  3. Ge H, Weiszmann J, Reagan J, Gupte J, Baribault H, Gyuris T, et al. Elucidation of signaling and functional activities of an orphan GPCR, GPR81. J Lipid Res. 2008;49:797-803 pubmed publisher
    b>GPR81 is an orphan G protein-coupled receptor (GPCR) that has a high degree of homology to the nicotinic acid receptor GPR109A. GPR81 expression is highly enriched and specific in adipocytes...
  4. Feingold K, Moser A, Shigenaga J, Grunfeld C. Inflammation inhibits GPR81 expression in adipose tissue. Inflamm Res. 2011;60:991-5 pubmed publisher
    The aim of this study was to examine the expression of G protein-coupled receptor 81 (GPR81) in mouse adipose tissue in response to inflammatory stimuli. GPR81 is activated by lactate resulting in the inhibition of lipolysis...
  5. Morland C, Andersson K, Haugen Ø, Hadzic A, Kleppa L, Gille A, et al. Exercise induces cerebral VEGF and angiogenesis via the lactate receptor HCAR1. Nat Commun. 2017;8:15557 pubmed publisher
    ..Here we show that the lactate receptor (HCAR1) is highly enriched in pial fibroblast-like cells that line the vessels supplying blood to the brain, and in ..