CGRP receptor | Calcitonin receptors | IUPHAR/BPS Guide to PHARMACOLOGY

CGRP receptor

Target id: 48

Nomenclature: CGRP receptor

Family: Calcitonin receptors

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   GtoImmuPdb view: OFF :     Currently no data for CGRP receptor in GtoImmuPdb

Quaternary Structure: Subunits
RAMP1 (Accessory protein)
calcitonin receptor-like receptor
Previous and Unofficial Names
CGRP1
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  CGRP receptor ectodomain in complex with RAMP1
PDB Id:  3N7P
Resolution:  2.8Å
Species:  Human
References:  47
Image of receptor 3D structure from RCSB PDB
Description:  CGRP receptor ectodomain in complex with antagonist
PDB Id:  3N7S
Ligand:  olcegepant
Resolution:  2.1Å
Species:  Human
References:  47
Image of receptor 3D structure from RCSB PDB
Description:  CGRP receptor ectodomain in complex with antagonist, ligand MK-0974
PDB Id:  3N7R
Ligand:  telcagepant
Resolution:  2.9Å
Species:  Human
References:  47
Image of receptor 3D structure from RCSB PDB
Description:  CGRP receptor ectodomain in complex with CGRP27–37 [Asp31, Pro34, Phe35]
PDB Id:  4RWG
Resolution:  2.44Å
Species:  Human
References:  8
Natural/Endogenous Ligands
adrenomedullin {Sp: Human} , adrenomedullin {Sp: Mouse} , adrenomedullin {Sp: Rat}
adrenomedullin 2/intermedin {Sp: Human} , adrenomedullin 2/intermedin {Sp: Mouse} , adrenomedullin 2/intermedin {Sp: Rat}
α-CGRP {Sp: Human}
β-CGRP {Sp: Human} , β-CGRP {Sp: Mouse}
α-CGRP {Sp: Mouse, Rat}
β-CGRP {Sp: Rat}
Comments: α-CGRP and β-CGRP are the principal endogenous agonists
Potency order of endogenous ligands (Human)
α-CGRP (CALCA, P06881) > adrenomedullin (ADM, P35318) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) > amylin (IAPP, P10997) ≥ calcitonin (salmon)

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Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[Cys(Et)2,7]α-CGRP (human) Hs Full agonist 10.5 pKi 39
pKi 10.5 [39]
β-CGRP {Sp: Human} Hs Full agonist 9.9 – 11.0 pKi 1,34
pKi 9.9 – 11.0 [1,34]
α-CGRP {Sp: Human} Hs Full agonist 9.7 – 10.0 pKi 1,34
pKi 9.7 – 10.0 [1,34]
adrenomedullin {Sp: Human} Hs Full agonist 8.1 pKi 1,34
pKi 8.1 [1,34]
[Cys(ACM)2,7]CGRP Hs Partial agonist 8.0 pKi 1
pKi 8.0 [1]
adrenomedullin 2/intermedin {Sp: Human} Hs Full agonist 7.5 – 9.1 pEC50 24
pEC50 7.5 – 9.1 [24]
β-CGRP {Sp: Rat} Rn Full agonist 8.2 – 9.3 pIC50 3,9,26,40
pIC50 8.2 – 9.3 [3,9,26,40]
α-CGRP {Sp: Mouse, Rat} Rn Full agonist 8.2 – 8.9 pIC50 3,9,26,40
pIC50 8.2 – 8.9 [3,9,26,40]
α-CGRP {Sp: Mouse, Rat} Mm Full agonist 8.2 pIC50 25
pIC50 8.2 [25]
adrenomedullin {Sp: Rat} Rn Full agonist 6.8 – 8.8 pIC50 26,40
pIC50 6.8 – 8.8 [26,40]
adrenomedullin {Sp: Rat} Mm Full agonist 7.6 pIC50 25
pIC50 7.6 [25]
[125I]αCGRP (mouse, rat) Hs Full agonist - -
View species-specific agonist tables
Agonist Comments
Reference [26] uses the rat calcitonin receptor-like receptor but mouse RAMP1.
Reference [9] uses the rat calcitonin receptor-like receptor but human RAMP1.

[Cys(ACM)2,7]-CGRP and [Cys(Et)2,7]-CGRP were introduced as selective CGRP2 agonists. This receptor phenotype is now considered to be a mixture of AM and AMY receptors [18]. [Cys(ACM)2,7]-CGRP is a partial agonist and the efficacy of [Cys(Et)2,7]-CGRP is very system dependent at CGRP and AMY receptors [5,19,39]. It is therefore recommended that these peptides are used with caution.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
olcegepant Hs Antagonist 10.7 – 11.0 pKi 13,20,22,27,32
pKi 10.7 – 11.0 (Ki 2x10-11 – 1x10-11 M) [13,20,22,27,32]
atogepant Hs Antagonist 10.8 pKi 7
pKi 10.8 (Ki 1.5x10-11 M) [7]
Description: In a recombinant receptor binding assay, antagonising 125I-CGRP binding.
compound 49 [PMID: 24405707] Hs Antagonist 10.5 pKi 27
pKi 10.5 (Ki 3x10-11 M) [27]
Description: Binding assay with cell membranes treated with 125I-CGRP.
α-CGRP-(8-37) (human) Hs Antagonist 9.2 – 9.6 pKi 1,34
pKi 9.2 – 9.6 [1,34]
telcagepant Hs Antagonist 9.1 pKi 44
pKi 9.1 [44]
α-CGRP-(8-37) (rat) Rn Antagonist 8.2 – 8.9 pIC50 3,9,26,40
pIC50 8.2 – 8.9 [3,9,26,40]
View species-specific antagonist tables
Antagonist Comments
BIBN4096BS (and MK-0974) shows at least an order of magnitude selectivity for primate over non-primate receptors. The pharmacology of these compounds have recently been reviewed [37]. This affinity is conferred by a tryptophan at position 74 of human RAMP1 [32]. A variety of other non-peptide antagonists have been described, but their pharmacology has not been widely explored [32]. In functional assays the pA2 for CGRP 8-37 shows a wide spread of values from around 7 to nearly 9, depending on the system being analysed [16,21]. Thus it is difficult to use it to classify receptors.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
erenumab Hs Antagonist 10.7 pKi 45
pKi 10.7 (Ki 2x10-11 M) [45]
Description: Displacement binding of [(125)I]-CGRP at the human CGRP receptor
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  1,34
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
Gq/G11 family
Phospholipase C stimulation
Potassium channel
Comments:  CGRP can also activate a phosphatidylinositol 3-(OH) kinase dependent pathway and increase cGMP [41].
References:  2,31
Tissue Distribution
Lung, non-pregnant and pregnant uterus, placenta.
Species:  Human
Technique:  Northern blotting.
References:  49
Spleen > liver, lung > spinal cord, whole brain > heart, kidney.
Note: CGRP receptor distribution can only be mapped reliably with [125I]-CGRP, as the calcitonin receptor-like receptor and the RAMPs form components of other receptors. Even radioligand binding is not without its problems as iodinated CGRP has appreciable affinity for amylin receptors.
Species:  Rat
Technique:  Radioligand binding.
References:  38
Functional Assays
Measurement of cAMP in SK-N-MC cells endogenously expressing a CGRP receptor.
Species:  Human
Tissue:  SK-N-MC cells.
Response measured:  cAMP production.
References:  15
Measurement of blood vessel diameter.
Species:  Human
Tissue:  Isolated cranial arteries.
Response measured:  Smooth muscle relaxation.
References:  15
Measurement of cAMP levels in Drosophila Schneider 2 cells transfected with the rat calcitonin receptor-like receptor and RAMP1.
Species:  Rat
Tissue:  Drosophila Schneider 2 cells.
Response measured:  cAMP accumulation.
References:  3
Measurement of cAMP levels in COS-7 cells transfected with the mouse calcitonin receptor-like receptor and mouse RAMP1.
Species:  Mouse
Tissue:  COS-7 cells.
Response measured:  cAMP accumulation.
References:  25
Measurement of cAMP levels in COS-7 cells transfected with the human calcitonin receptor-like receptor and human RAMP1.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  cAMP accumulation.
References:  5
Physiological Functions
Vasodilation.
Species:  Human
Tissue:  Isolated cerebral arteries.
References:  15
Antiproliferative effect.
Species:  Rat
Tissue:  Cultured vascular smooth muscle cells.
References:  29
Positive inotropic effects on the heart.
Species:  Human
Tissue:  Isolated myocardial trabeculae from the right atrium and left ventricle of the heart.
References:  43
Inhibition of food intake.
Species:  Rat
Tissue:  In vivo.
References:  46
Suppression of angiotensin-II-stimulated aldosterone production.
Species:  Rat
Tissue:  Zona glomerulosa cells of the adrenal gland.
References:  4
Inhibition of galanin-stimulated contraction.
Species:  Rat
Tissue:  Isolated non-pregnant uterus.
References:  49
Vasodilation.
Species:  Rat
Tissue:  Isolated perfused kidney.
References:  23
Inhibition of gastric emptying.
Species:  Rat
Tissue:  In vivo.
References:  33
Positive inotropic and chronotropic effects on the heart.
Species:  Rat
Tissue:  Isolated ventricular cardiomyocytes.
References:  6
Vasodilation.
Species:  Human
Tissue:  Small arteries from thymus.
References:  11
Thermal hyperalgesia.
Species:  Mouse
Tissue:  Skin.
References:  36
Thermal hyperalgesia.
Species:  Mouse
Tissue:  Spinal cord.
References:  36
Vasodilation.
Species:  Rat
Tissue:  Mesenteric vascular bed and cerebral blood vessels.
References:  17,51
Endothelium-independent vasodilation.
Species:  Human
Tissue:  Middle meningeal arteries.
References:  14
Mechanical nociception
Species:  Rat
Tissue:  Bone joints.
References:  10
Physiological Consequences of Altering Gene Expression
Protection against diet-induced obesity.
Species:  Mouse
Tissue: 
Technique:  CGRP knockout mouse
References:  50
TRPV1 channel mobilisation and nociception.
Species:  Mouse
Tissue: 
Technique:  knockout
References:  12
Antisense oligonucleotides against RAMP1 increase pulmonary artery pressure.
Species:  Rat
Tissue: 
Technique:  Antisense oligonucleotide.
References:  42
In mice engineered for neural over-expression of human RAMP1, plasma extravasation in response to CGRP, a marker of neurogenic inflammation, was enhanced.
Species:  Mouse
Tissue: 
Technique:  Gene overexpression.
References:  53
Promotion of energy expenditure
Species:  Mouse
Tissue:  Central nervous system (RAMP1 overexpression)
Technique: 
References:  52
In a conditional RAMP1-/-mouse model, αCGRP-mediated reductions in blood pressure were lost and there were disturbances in pro-inflammatory cytokine production.
Species:  Mouse
Tissue: 
Technique:  Knockout.
References:  28,35,48
Impaired wound healing in RAMP-/- mice is associated with reduced expression of VEFG-A, -B and –C.
Species:  Mouse
Tissue: 
Technique:  Knockout
References:  30

References

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51. Wang Z, Martorell BC, Wälchli T, Vogel O, Fischer J, Born W, Vogel J. (2015) Calcitonin gene-related peptide (CGRP) receptors are important to maintain cerebrovascular reactivity in chronic hypertension. PLoS ONE, 10 (4): e0123697. [PMID:25860809]

52. Zhang Z, Liu X, Morgan DA, Kuburas A, Thedens DR, Russo AF, Rahmouni K. (2011) Neuronal receptor activity-modifying protein 1 promotes energy expenditure in mice. Diabetes, 60 (4): 1063-71. [PMID:21357463]

53. Zhang Z, Winborn CS, Marquez de Prado B, Russo AF. (2007) Sensitization of calcitonin gene-related peptide receptors by receptor activity-modifying protein-1 in the trigeminal ganglion. J Neurosci, 27: 2693-2703. [PMID:17344407]

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How to cite this page

Debbie Hay, David R. Poyner.
Calcitonin receptors: CGRP receptor. Last modified on 19/02/2018. Accessed on 18/10/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=48.