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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
Nomenclature calcitonin receptor‐like receptor CGRP receptor AM1 receptor AM2 receptor
HGNC, UniProt CALCRL, Q16602
Subunits calcitonin receptor‐like receptor, RAMP1 (Accessory protein) calcitonin receptor‐like receptor, RAMP2 (Accessory protein) calcitonin receptor‐like receptor, RAMP3 (Accessory protein)
Rank order of potency α‐CGRP (CALCA, P06881) >adrenomedullin (ADM, P35318) ≥adrenomedullin 2/intermedin (ADM2, Q7Z4H4) >amylin (IAPP, P10997) ≥calcitonin (salmon) adrenomedullin (ADM, P35318) >adrenomedullin 2/intermedin (ADM2, Q7Z4H4) >α‐CGRP (CALCA, P06881), amylin (IAPP, P10997) >calcitonin (salmon) adrenomedullin (ADM, P35318) ≥adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥α‐CGRP (CALCA, P06881) >amylin (IAPP, P10997) >calcitonin (salmon)
Endogenous agonists β‐CGRP (CALCB, P10092) (pK i 9.9–11) [20, 1251], α‐CGRP (CALCA, P06881) (pK i 9.7–10) [20, 1251] adrenomedullin (ADM, P35318) (pK i 8.3–9.2) [20, 1251] adrenomedullin (ADM, P35318) (pK i 8.3–9) [20, 539]
Antagonists olcegepant (pK i 10.2–10.7) [435, 719, 720, 1194], telcagepant (pK i 9.1) [1633]
Selective antagonists AM‐(22‐52) (human) (pK i 7–7.8) [20, 720, 1251]
Labelled ligands [125I]αCGRP (human) (Agonist) (pK d 10), [125I]αCGRP (mouse, rat) (Agonist) [125I]AM (rat) (Agonist) (pK d 10–9) [125I]AM (rat) (Agonist) (pK d 9–10)