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) |