Anaphylatoxin GPCR Family Subtypes and Products

What Are Anaphylatoxin Receptors?

Anaphylatoxin receptors are a family of G protein-coupled receptors (GPCRs) that consists of C3a, C5a, and C5L2 receptors. Anaphylatoxins, also known as complement peptides, serve a major role in inflammation, and are targets for anti-inflammatory treatments. There are currently no satisfactory antagonists for the three mammalian complement peptides.

Anaphylatoxin Receptor Information

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C3a receptor (C3a anaphylatoxin chemotactic receptor) is a receptor for the chemotactic and inflammatory peptide anaphylatoxin C3a. The receptor is widely expressed in many hematopoietic cell lines, throughout the CNS and other tissues, and the expression level in glial cells increases during CNS inflammation. It stimulates chemotaxis, granule enzyme release and superoxide anion production, mediates the pathogenesis of demyelinating disease by directly or indirectly chemoattracting encephalitogenic cells to the CNS. Administration of small molecule inhibitors of C3a receptor inhibits airway responses.

C5a receptor (C5a anaphylatoxin chemotactic receptor, or CD88 antigen, C5R1) is a receptor for chemotactic and inflammatory peptide anaphylatoxin C5a. C5a is a classic, potent inflammatory mediator, and the C5R1 receptor stimulates chemotaxis, granule enzyme release and superoxide anion production. C5a receptor antagonists, such as AcPhe[Orn-Pro-D-cyclohexylalanine-Trp-Arg], show therapeutic effects in various inflammatory disease models. C5a receptor may also be involved in neurodegeneration and Alzheimer’s disease.

Anaphylatoxin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes