Complement peptide receptors

Overview

Complement peptide receptors are activated by the endogenous ~75 amino-acid anaphylatoxin polypeptides C3a and C5a, generated upon stimulation of the complement cascade. C3a and C5a exert their functions through binding to their receptors (C3aR, C5aR1 and C5aR2), causing cell recruitment and triggering cellular degranulation that contributes to local inflammation.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Species
Receptor
Family
Assays
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Respiratory
à la carte
Reference agonist:
C3a
EC50:
3.7 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Hematology
Respiratory
Musculoskeletal
à la carte
Reference agonist:
C5a
EC50:
220 pM
Human
Assay modes:
-
Panels:
-
Reference agonist:
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
C3a
EC50:
2.3 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
C5a
EC50:
590 pM