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Gene Review

C5ar1  -  complement component 5a receptor 1

Rattus norvegicus

Synonyms: C5a anaphylatoxin chemotactic receptor, C5a anaphylatoxin chemotactic receptor 1, C5a-R, C5aR, C5r1
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Disease relevance of C5r1


Psychiatry related information on C5r1


High impact information on C5r1

  • RESULTS: In vivo treatment of rats with LPS induced C5a receptor mRNA and protein in hepatocytes with a maximum after 8-10 hours [8].
  • Lipopolysaccharide (LPS) has been reported to enhance C5a receptor expression in murine livers [8].
  • Expression of C3aR and C5aR mRNAs and proteins was also observed in vitro in cultured cerebellar granule cells [9].
  • Our results provide the first evidence that C3aR and C5aR are both expressed in cerebellar granule cells during development and that C5a, but not C3a, is a potent inhibitor of apoptotic cell death in cultured granule neurons [9].
  • The neuroprotective effect of the C5aR agonist was associated with a marked inhibition of caspase-9 activity and partial restoration of mitochondrial integrity [9].

Biological context of C5r1


Anatomical context of C5r1

  • A cDNA clone, DTJP03, encoding an orphan receptor, was isolated from a canine thyroid library, and found to exhibit 68.6% amino-acid identity with the recently described human C5a receptor [14].
  • Binding studies performed on membranes from COS-7 cells expressing the recombinant receptor demonstrated that DTJP03 encoded a high-affinity C5a receptor, with a Kd of 1.2 nM [14].
  • In order to corroborate this mechanism, the distribution of anaphylatoxin receptors in the different cell types of rat liver was determined by quantitative RT-PCR with primers specific for the rat C5a receptor (rC5aR) using RNA isolated from KC, sinusoidal endothelial cells (SEC), hepatic stellate cells (HSC) and HC [15].
  • Expression of a functional C5a receptor in regenerating hepatocytes and its involvement in a proliferative signaling pathway in rat [16].
  • Expression and function of the C5a receptor in rat alveolar epithelial cells [17].

Associations of C5r1 with chemical compounds

  • Extracellular EGTA partially prevented this response, suggesting that activation of the C5a receptor promotes both the release of calcium from intracellular stores, and the influx of extracellular calcium [14].
  • Intracellular free calcium concentrations were measured by Quin-2 fluorescence assays in Chinese hamster ovary cells stably transfected with the canine C5a receptor [14].
  • C5aR was usually expressed at the site of exposure to pathogens, such as in salivary gland or lung, and was up-regulated in liver in the inflammatory state induced by lipopolysaccharide (LPS) administration [18].
  • Through a high capacity screening followed by chemical optimization, we identified a novel non-peptide C5a receptor antagonist, N-[(4-dimethylaminophenyl)methyl]-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1- carboxamide hydrochloride (W-54011) [19].

Physical interactions of C5r1

  • However, little is known about the role of the C5a/C5aR complex in liver and its involvement during a proliferative process [16].

Regulatory relationships of C5r1


Other interactions of C5r1

  • Here, we show that transient expression of C3aR and C5aR occurs in cerebellar granule neurons in vivo with a maximal density in 12-day-old rat, suggesting a role of these receptors during development of the cerebellum [9].
  • In contrast, LPS failed to induce C5aR directly in cultured HC in-vitro but induced C5aR in HC in vivo and in co-cultures of HC and KC which release IL-6 upon stimulation with LPS [20].
  • These data suggest that complement-mediated inflammation can be modulated at the C5a receptor level, independent of proinflammatory TNF-alpha production, and prevent acute local and remote organ injury [22].

Analytical, diagnostic and therapeutic context of C5r1


  1. Experimental diffuse axonal injury induces enhanced neuronal C5a receptor mRNA expression in rats. Stahel, P.F., Kossmann, T., Morganti-Kossmann, M.C., Hans, V.H., Barnum, S.R. Brain Res. Mol. Brain Res. (1997) [Pubmed]
  2. A new small molecule C5a receptor antagonist inhibits the reverse-passive Arthus reaction and endotoxic shock in rats. Strachan, A.J., Woodruff, T.M., Haaima, G., Fairlie, D.P., Taylor, S.M. J. Immunol. (2000) [Pubmed]
  3. A small molecule C5a receptor antagonist protects kidneys from ischemia/reperfusion injury in rats. Arumugam, T.V., Shiels, I.A., Strachan, A.J., Abbenante, G., Fairlie, D.P., Taylor, S.M. Kidney Int. (2003) [Pubmed]
  4. Characterisation of C5a receptor agonists from phage display libraries. Cain, S.A., Higginbottom, A., Monk, P.N. Biochem. Pharmacol. (2003) [Pubmed]
  5. Kinetics of anaphylatoxin C5a receptor expression during experimental allergic encephalomyelitis. Nataf, S., Davoust, N., Barnum, S.R. J. Neuroimmunol. (1998) [Pubmed]
  6. Therapeutic activity of C5a receptor antagonists in a rat model of neurodegeneration. Woodruff, T.M., Crane, J.W., Proctor, L.M., Buller, K.M., Shek, A.B., de Vos, K., Pollitt, S., Williams, H.M., Shiels, I.A., Monk, P.N., Taylor, S.M. FASEB J. (2006) [Pubmed]
  7. Complement C5a receptor-mediated signaling may be involved in neurodegeneration in Alzheimer's disease. Farkas, I., Takahashi, M., Fukuda, A., Yamamoto, N., Akatsu, H., Baranyi, L., Tateyama, H., Yamamoto, T., Okada, N., Okada, H. J. Immunol. (2003) [Pubmed]
  8. Induction of anaphylatoxin C5a receptors in rat hepatocytes by lipopolysaccharide in vivo: mediation by interleukin-6 from Kupffer cells. Koleva, M., Schlaf, G., Landmann, R., Götze, O., Jungermann, K., Schieferdecker, H.L. Gastroenterology (2002) [Pubmed]
  9. Characterization of C3a and C5a receptors in rat cerebellar granule neurons during maturation. Neuroprotective effect of C5a against apoptotic cell death. Bénard, M., Gonzalez, B.J., Schouft, M.T., Falluel-Morel, A., Vaudry, D., Chan, P., Vaudry, H., Fontaine, M. J. Biol. Chem. (2004) [Pubmed]
  10. Analysis of the tissue distribution of the rat C5a receptor and inhibition of C5a-mediated effects through the use of two MoAbs. Rothermel, E., Götze, O., Zahn, S., Schlaf, G. Scand. J. Immunol. (2000) [Pubmed]
  11. Contribution of anaphylatoxin C5a to late airway responses after repeated exposure of antigen to allergic rats. Abe, M., Shibata, K., Akatsu, H., Shimizu, N., Sakata, N., Katsuragi, T., Okada, H. J. Immunol. (2001) [Pubmed]
  12. Molecular cloning and expression of the functional rat C5a receptor. Rothermel, E., Zwirner, J., Vogt, T., Rabini, S., Götze, O. Mol. Immunol. (1997) [Pubmed]
  13. Ligand-induced phosphorylation of anaphylatoxin receptors C3aR and C5aR is mediated by "G protein-coupled receptor kinases. Langkabel, P., Zwirner, J., Oppermann, M. Eur. J. Immunol. (1999) [Pubmed]
  14. Cloning and functional expression of the canine anaphylatoxin C5a receptor. Evidence for high interspecies variability. Perret, J.J., Raspe, E., Vassart, G., Parmentier, M. Biochem. J. (1992) [Pubmed]
  15. Anaphylatoxin C5a receptor mRNA is strongly expressed in Kupffer and stellate cells and weakly in sinusoidal endothelial cells but not in hepatocytes of normal rat liver. Schieferdecker, H.L., Rothermel, E., Timmermann, A., Götze, O., Jungermann, K. FEBS Lett. (1997) [Pubmed]
  16. Expression of a functional C5a receptor in regenerating hepatocytes and its involvement in a proliferative signaling pathway in rat. Daveau, M., Benard, M., Scotte, M., Schouft, M.T., Hiron, M., Francois, A., Salier, J.P., Fontaine, M. J. Immunol. (2004) [Pubmed]
  17. Expression and function of the C5a receptor in rat alveolar epithelial cells. Riedemann, N.C., Guo, R.F., Sarma, V.J., Laudes, I.J., Huber-Lang, M., Warner, R.L., Albrecht, E.A., Speyer, C.L., Ward, P.A. J. Immunol. (2002) [Pubmed]
  18. Distribution of rat C5a anaphylatoxin receptor. Akatsu, H., Abe, M., Miwa, T., Tateyama, H., Maeda, S., Okada, N., Kojima, K., Okada, H. Microbiol. Immunol. (2002) [Pubmed]
  19. Identification of a potent and orally active non-peptide C5a receptor antagonist. Sumichika, H., Sakata, K., Sato, N., Takeshita, S., Ishibuchi, S., Nakamura, M., Kamahori, T., Ehara, S., Itoh, K., Ohtsuka, T., Ohbora, T., Mishina, T., Komatsu, H., Naka, Y. J. Biol. Chem. (2002) [Pubmed]
  20. Expression and induction of anaphylatoxin C5a receptors in the rat liver. Schlaf, G., Schmitz, M., Rothermel, E., Jungermann, K., Schieferdecker, H.L., Götze, O. Histol. Histopathol. (2003) [Pubmed]
  21. IFN-gamma inhibits inflammatory cell recruitment and the evolution of bacterial cell wall-induced arthritis. Wahl, S.M., Allen, J.B., Ohura, K., Chenoweth, D.E., Hand, A.R. J. Immunol. (1991) [Pubmed]
  22. Complement C5a receptor antagonist attenuates multiple organ injury in a model of ruptured abdominal aortic aneurysm. Harkin, D.W., Romaschin, A., Taylor, S.M., Rubin, B.B., Lindsay, T.F. J. Vasc. Surg. (2004) [Pubmed]
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