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CaS receptor

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Target not currently curated in GtoImmuPdb

Target id: 54

Nomenclature: CaS receptor

Family: Calcium-sensing receptor

Contents:

Gene and Protein Information Click here for help
class C G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 1078 3q13.33-q21.1 CASR calcium sensing receptor 77
Mouse 7 1079 16 25.57 cM Casr calcium-sensing receptor 55
Rat 7 1079 11q22 Casr calcium-sensing receptor 96
Previous and Unofficial Names Click here for help
CaR | GPRC2A | extracellular calcium-sensing receptor | divalent cation-sensing receptor | calcium-sensing receptor
Database Links Click here for help
Specialist databases
GPCRdb casr_human (Hs), casr_mouse (Mm), casr_rat (Rn)
Other databases
Alphafold P41180 (Hs), Q9QY96 (Mm), P48442 (Rn)
ChEMBL Target CHEMBL1878 (Hs), CHEMBL4105868 (Mm), CHEMBL2516 (Rn)
DrugBank Target P41180 (Hs)
Ensembl Gene ENSG00000036828 (Hs), ENSMUSG00000051980 (Mm), ENSRNOG00000002265 (Rn)
Entrez Gene 846 (Hs), 12374 (Mm), 24247 (Rn)
Human Protein Atlas ENSG00000036828 (Hs)
KEGG Gene hsa:846 (Hs), mmu:12374 (Mm), rno:24247 (Rn)
OMIM 601199 (Hs)
Orphanet ORPHA119185 (Hs)
Pharos P41180 (Hs)
RefSeq Nucleotide NM_000388 (Hs), NM_013803 (Mm), NM_016996 (Rn)
RefSeq Protein NP_000379 (Hs), NP_038831 (Mm), NP_058692 (Rn)
SynPHARM 2181 (in complex with Ca2+)
UniProtKB P41180 (Hs), Q9QY96 (Mm), P48442 (Rn)
Wikipedia CASR (Hs)
Natural/Endogenous Ligands Click here for help
Ca2+
L-tryptophan
Mg2+
spermine
Amino-acid rank order of potency
L-phenylalanine, L-tryptophan, L-histidine > L-alanine > L-serine, L-proline, L-glutamic acid > L-aspartic acid (not L-lysine, L-arginine, L-leucine and L-isoleucine)  [31]
Cation rank order of potency
Gd3+ > Ca2+ > Mg2+  [14]
Glutamyl peptide rank order of potency
S-methylglutathione ≈ γGlu-Val-Gly > glutathione > γGlu-Cys  [10,86,116]
Polyamine rank order of potency
spermine > spermidine > putrescine  [93]

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
neomycin Small molecule or natural product Approved drug Ligand has a PDB structure Rn Full agonist 4.0 pKd 96
⤷ pKd 4.0 [96]
spermine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 3.5 pKd 93
⤷ pKd 3.5 [93]
Ca2+ Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 2.5 pKd 91
⤷ pKd 2.5 [91]
Ca2+ Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 2.5 pKd 96
⤷ pKd 2.5 [96]
Ca2+ Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 2.4 pKd 77
⤷ pKd 2.4 [77]
Mg2+ Click here for species-specific activity table Ligand is endogenous in the given species Rn Partial agonist 2.4 pKd 12,96
⤷ pKd 2.4 [12,96]
View species-specific agonist tables
Agonist Comments
Etelcalcetide is a novel peptide agonist of the receptor [115]. Other aminoglycosides show agonist activity [96].

Bovine data is available on a number of other ligands including: polyarginine (and other polycations) (pKd 7) ([15]), Gd3+ and other lanthanides (pKd 4.3-4.9) ([13-14]), neomycin (and other aminoglycosides) (pKd 6.9).
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
2-methyl-3-phenethyl-3H-pyrimidin-4-one Small molecule or natural product Hs Antagonist 7.0 pIC50 108
⤷ pIC50 7.0 [108]
compound (S)-3h [PMID: 15686947] Small molecule or natural product Hs Antagonist 6.9 pIC50 127
⤷ pIC50 6.9 [127]
compound 17 [PMID: 15300839] Small molecule or natural product Rn Antagonist 5.3 pIC50 57
⤷ pIC50 5.3 [57]
1-arylmethylpyrrolidin-2-yl ethanol amine Small molecule or natural product Rn Antagonist 4.3 pIC50 45
⤷ pIC50 4.3 [45]
View species-specific antagonist tables
Antagonist Comments
There have been few, if any, studies evaluating whether these are competitive or noncompetitive antagonists. The binding site for polycationic (type 1) CaR agonists, such as calcium or gadolinium, are almost certainly in a different location from that of these antagonists, with the former being predominantly in the amino-terminal extracellular domain and the latter in the transmembrane domains. However, the binding site for the calcimimetic (type 2) CaR activators, at a minimum, overlaps with that of the antagonists [16,50].

Pathophysiologic concentrations of extracellular phosphate and sulphate may elicit non-competitive antagonism of CaS [18].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
NPS 2143 Small molecule or natural product Ligand has a PDB structure Hs Negative 6.2 – 6.7 pKB 34,65-66
⤷ pKB 6.2 – 6.7 [34,65-66]
Description: Ca2+i release
tecalcet Small molecule or natural product Ligand has a PDB structure Hs Positive 6.2 – 6.6 pKB 32,34
⤷ pKB 6.2 – 6.6 [32,34]
Description: Ca2+i release
AC265347 Small molecule or natural product Hs Positive 6.3 – 6.4 pKB 32,65
⤷ pKB 6.3 – 6.4 [32,65]
Description: Ca2+i release
calindol Small molecule or natural product Hs Positive 6.3 pKB 32
⤷ pKB 6.3 [32]
Description: Ca2+i release
cinacalcet Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Positive 5.9 – 6.6 pKB 32,34,65-66
⤷ pKB 5.9 – 6.6 [32,34,65-66]
Description: Ca2+i release
tecalcet Small molecule or natural product Ligand has a PDB structure Hs Positive 6.5 pKd 82
⤷ pKd 6.5 [82]
calindol Small molecule or natural product Hs Positive 6.0 – 6.5 pKd 56,89
⤷ pKd 6.0 – 6.5 [56,89]
L-tryptophan Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Positive 2.6 – 4.4 pKd 30-31
⤷ pKd 2.6 – 4.4 [30-31]
AC265347 Small molecule or natural product Hs Positive 7.6 – 8.1 pEC50 68
⤷ pEC50 7.6 – 8.1 [68]
cinacalcet Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Positive 7.3 pEC50 80
⤷ pEC50 7.3 (EC50 5.1x10-8 M) [80]
evocalcet Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Positive 7.0 pEC50 75
⤷ pEC50 7.0 (EC50 9.3x10-8 M) [75]
etelcalcetide Peptide Approved drug Hs Positive 4.6 pEC50 115
⤷ pEC50 4.6 (EC50 2.5x10-5 M) [115]
Description: Measuring ligand induced IP1 accumulation.
ATF936 Small molecule or natural product Hs Negative 8.9 pIC50 120
⤷ pIC50 8.9 [120]
Description: Inhibition of 2.5 mM Ca2+-mediated Ca2+i release
AXT914 Small molecule or natural product Hs Negative 8.9 pIC50 119
⤷ pIC50 8.9 (IC50 1.4x10-9 M) [119]
upacicalcet Small molecule or natural product Approved drug Hs Positive 8.1 pIC50 106
⤷ pIC50 8.1 (IC50 8.2x10-9 M) [106]
Description: Competition binding assay, dispalcement of [3H]-upacicalcet from hCaSR by unlabelled upacicalcet
encaleret Small molecule or natural product Hs Negative 7.9 pIC50 110
⤷ pIC50 7.9 [110]
Description: Inhibition of 5 mM Ca2+-mediated luciferase reporter activity
(R)-2h [PMID:19625189] Small molecule or natural product Hs Negative 7.4 pIC50 37
⤷ pIC50 7.4 (IC50 4.1x10-8 M) [37]
NPS 2143 Small molecule or natural product Ligand has a PDB structure Hs Negative 7.1 – 7.4 pIC50 79,127
⤷ pIC50 7.1 – 7.4 [79,127]
compound 18c [PMID:19143533] Small molecule or natural product Hs Negative 7.1 pIC50 126
⤷ pIC50 7.1 (IC50 7.6x10-8 M) [126]
Description: Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.
SB-423562 Small molecule or natural product Hs Negative 7.1 pIC50 62
⤷ pIC50 7.1 [62]
ronacaleret Small molecule or natural product Hs Negative 6.5 – 6.8 pIC50 5
⤷ pIC50 6.5 – 6.8 [5]
calhex 231 Small molecule or natural product Hs Negative 6.4 pIC50 90
⤷ pIC50 6.4 [90]
Description: Inhibition of 9mM Ca2+o-mediated IP accumulation
Allosteric Modulator Comments
Note that aromatic amino acids and calcimimetics are ineffective in the absence of Ca2+. N1-Arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines [33] and cinacalcet [78,107] are also allosteric regulators, but do not have associated affinity values. Activity is also shown by other aromatic amino acids e.g. L-Phe, L-Tyr, L-His. NPS 89636 and AXT-914 have been shown to be negative allosteric modulators of this receptor, although affinity data and a chemical structures are unavailable [38,67].

Additional functional readouts of receptor activity:

tecalcet: functional pKB 5.6 - 6.2 for ERK1/2 phosphorylation (pERK1/2) [32,34], functional pKB 6.8 for inositol phosphate (IP) accumulation [32], functional pKB 9.4 for membrane ruffling [34], pEC50 6.3 for potentiation of 0.5 mM Ca2+-mediated Ca2+i release [82], pEC50 6.5 for potentiation of 2 mM Ca2+-mediated inositol phosphate (IP) accumulation [89].

calindol: functional pKB 5.2 for pERK1/2 [32], functional pKB 6.4 for IP accumulation [32], pEC50 6.5 for potentiation of 2 mM Ca2+-mediated IP accumulation [89].

AC265347: functional pKB 6.3 - 6.7 for pERK1/2 [32,65], functional pKB 8.0 for IP accumulation [32], pEC50 7.6 for potentiation of 1.6 mM Ca2+-mediated cellular proliferation, and pEC50 8.1 for potentiation of 1.6 mM Ca2+-mediated IP accumulation [68].

cinacalcet: functional pKB 5.9 - 6.7 for pERK1/2 [32,34,65-66], functional pKB 6.1 for IP accumulation [32], functional pKB 8.1 for membrane ruffling [34], pEC50 7.3 for potentiation of 0.5 mM Ca2+-mediated Ca2+i release [80].

NPS 2143: functional pKB 6.2 - 6.7 for pERK1/2 [34,65-66], functional pKB 7.8 for membrane ruffling [34], pIC50 7.4 for inhibition of 1.75mM Ca2+-mediated Ca2+i release [79].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family
Gq/G11 family
G12/G13 family 		Adenylyl cyclase inhibition
Phospholipase C stimulation
Phospholipase D stimulation
Comments:  In [53], activation of PLD by the CaR takes place through a direct mechanism involving G12/G13. In some cases, inhibition of adenylate cyclase appears to be indirect, occurring by a calcium sensing receptor-mediated increase in the cytosolic calcium concentration, which then inhibits a calcium-sensitive isoform of adenylate cyclase, see below [35].
References:  19,27,53,58,81
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family
G protein (identity unknown) 		Adenylyl cyclase stimulation
Potassium channel
Phospholipase A2 stimulation
Phospholipase D stimulation
Other - See Comments
Comments:  In addition to the transducers and effectors noted above, the calcium sensing receptor also activates a nonselective cation channel [130], MAPK pathways, e.g. ERK1/2 [48,59,73], p38 MAPK [69], JNK [23], PI-3K [111], PI-4K [52], Rho [92] and the epidermal growth factor receptor [70].
References:  25,35,48,58-59,73,129-130
Tissue Distribution Click here for help
Colon cancer cells, Caco-2.
Species:  Human
Technique:  RT-PCR, immunocytochemistry and Western blotting.
References:  64
Osteosarcoma cell line, MG-63.
Species:  Human
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  123
Osteoblastic cells, SaOS-2.
Species:  Human
Technique:  Western blotting.
References:  20
Embryonic astrocytes, astrocytomas and meningiomas.
Species:  Human
Technique:  Northern blotting, RT-PCR and Western blotting.
References:  22
C-cells.
Species:  Human
Technique:  in situ hybridization.
References:  42
Parathyroid.
Species:  Human
Technique:  Northern blotting.
References:  77
Placental villi (cytotrophoblasts and synctiotrophoblasts), trophoblast columns.
Species:  Human
Technique:  Northern blotting, RT-PCR, in situ hybridisation and immunocytochemistry.
References:  8
Pituitary.
Species:  Human
Technique:  Northern blotting.
References:  71
Lens epithelial cells.
Species:  Human
Technique:  Northern blotting, RT-PCR and immunocytochemistry.
References:  26
Keratinocytes.
Species:  Human
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  40
Minor salivary gland.
Species:  Human
Technique:  Northern blotting.
References:  49
Prostate cancer cells, PC-3 and LnCaP.
Species:  Human
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  128
Ovarian surface cells.
Species:  Human
Technique:  Northern and Western blotting.
References:  72
Promyelocytic leukemia cells, HL-60.
Species:  Human
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  125
Myeloma cells, U266, IM-9 and RPM18226.
Species:  Human
Technique:  RT-PCR, immunocytochemistry and Western blotting.
References:  124
Medullary thyroid cancer, normal and adenomatous parathyroid, normal and adenomatous pituitary.
Species:  Human
Technique:  RT-PCR.
References:  71
Thyroid c-cells.
Species:  Human
Technique:  RT-PCR.
References:  44
Monocytes.
Species:  Human
Technique:  Northern blotting.
References:  87
Gastrinoma cells.
Species:  Human
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  54
Gastric mucosal epithelial cells.
Species:  Human
Technique:  Immunocytochemistry and Western blotting.
References:  100
Breast cancer cell lines, MCF-7 and MDA-MB-231.
Species:  Human
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  104
Pancreatic islet and insulinoma cells.
Species:  Human
Technique:  RT-PCR.
References:  54,101
Pancreatic islet and insulinoma cells
Species:  Human
Technique:  immunocytochemistry.
References:  60
Pancreatic acinar and duct cells.
Pancreatic cancer cells, Capan-1.
Species:  Human
Technique:  RT-PCR and immunocytochemistry.
References:  101
Breast ductal cells.
Species:  Human
Technique:  Northern blotting, RT-PCR and immunocytochemistry.
References:  28
Colon.
Species:  Human
Technique:  RT-PCR, immunocytochemistry and Western blotting.
References:  109
Skin.
Species:  Mouse
Technique:  RT-PCR and immunocytochemistry.
References:  61
Kidney.
Species:  Mouse
Technique:  Immunocytochemistry and Western blotting.
References:  51
Mesangial cells.
Species:  Mouse
Technique:  RT-PCR, immunocytochemistry and Western blotting.
References:  63
Monocytic cell line, J774.
Species:  Mouse
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  39
Parathyroid.
Species:  Mouse
Technique:  immunocytochemistry.
References:  51
Breast.
Species:  Mouse
Technique:  RNAse protection and immunocytochemistry.
References:  113
Osteoblasts, osteoclasts, osteocytes and chondrocytes.
Species:  Mouse
Technique:  In situ hybridisation and immunocytochemistry.
References:  20
Osteoblastic cell line, MC3T3-E1.
Species:  Mouse
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  122
Bone marrow stromal cell line, ST-2.
Species:  Mouse
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  121
Pituitary cell line, AtT-20.
Species:  Mouse
Technique:  Northern blotting, RT-PCR and immunocytochemistry.
References:  39
C-cells.
Species:  Rat
Technique:  immunocytochemistry.
References:  42
Kidney.
Species:  Rat
Technique:  immunocytochemistry.
References:  74,97
Kidney inner medullary collecting duct.
Species:  Rat
Technique:  Western blotting.
References:  105
Kidney.
Species:  Rat
Technique:  immunocytochemistry.
References:  74
Osteoblast, osteocyte and osteoclast.
Species:  Rat
Technique:  immunocytochemistry.
References:  38
Pancreas, adrenal medulla, testis, multiple brain regions.
Species:  Rat
Technique:  immunocytochemistry.
References:  74
Small and large intestine.
Species:  Rat
Technique:  immunocytochemistry.
References:  21,74
Kidney proximal tubule.
Species:  Rat
Technique:  immunocytochemistry.
References:  97
Stomach.
Species:  Rat
Technique:  immunocytochemistry.
References:  29,74
Parathyroid and kidney.
Species:  Rat
Technique:  Ribonuclease protection assay.
References:  11
Liver.
Species:  Rat
Technique:  Immunocytochemistry and Western blotting.
References:  17
Heart.
Species:  Rat
Technique:  Western blotting.
References:  74
Osteoblasts, osteoclasts and osteocytes.
Species:  Rat
Technique:  RT-PCR.
References:  38
Osteoblasts, osteoclasts, osteocytes and chondrocytes.
Species:  Rat
Technique:  immunocytochemistry.
References:  20
Thyroid c-cells.
Species:  Rat
Technique:  Northern blotting, in situ hybridisation and immunocytochemistry.
References:  44
Fibroblasts.
Species:  Rat
Technique:  Northern and Western blotting.
References:  73
Oligodendrocytes.
Species:  Rat
Technique:  RT-PCR, immunocytochemistry and Western blotting.
References:  26
Microglia.
Species:  Rat
Technique:  Northern blotting, RT-PCR, immunocytochemistry and Western blotting.
References:  25
Sensory nerve.
Species:  Rat
Technique:  Western blotting.
References:  118
Testicular cancer cell-line H-500.
Species:  Rat
Technique:  RT-PCR, Western blot, immunocytochemistry.
References:  102
Fibroblasts.
Species:  Rat
Technique:  Northern blot.
References:  73
C-cells.
Species:  Rat
Technique:  Northern blot.
References:  42,44
Stomach.
Species:  Rat
Technique:  Northern blot.
References:  29
Small and large intestine.
Species:  Rat
Technique:  Northern blot.
References:  21
Oligodendrocytes.
Species:  Rat
Technique:  Northern blot and RT-PCR.
References:  24
Oligodendrocytes.
Species:  Rat
Technique:  Northern blot and RT-PCR.
References:  24
Microglia.
Species:  Rat
Technique:  Northern blot, RT-PCR and immunocytochemistry.
References:  25
Testicular cancer cell (H-500).
Species:  Rat
Technique:  Northern blot and RT-PCR.
References:  102
Medullary thyroid cancer cell line (rMTC44-2).
Species:  Rat
Technique:  RT-PCR.
References:  44
Heart.
Species:  Rat
Technique:  RT-PCR.
References:  117
Osteoblast, osteocyte and osteoclast.
Species:  Rat
Technique:  RT-PCR.
References:  38
Multiple brain regions.
Species:  Rat
Technique:  in situ hybridization.
References:  99
Osteoblast, osteocyte, osteocyte and chondrocyte.
Species:  Rat
Technique:  in situ hybridization.
References:  20
Kidney.
Species:  Rat
Technique:  Northern blot and RT-PCR.
References:  95,97
Tissue Distribution Comments
A variety of techniques--Northern blotting, RT-PCR, immunocytochemistry and Western blotting--were used to identify the calcium sensing receptor in the receptor distribution studies. Lack of availability of some human tissues, such as kidney, have so far precluded a comprehensive tissue survery for expression of the human calcium sensing receptor in humans.
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Effects of agonists/allosteric regulators on human calcium sensing receptor-transfected HEK 293 cells.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in cytosolic calcium concentration, inhibition of adenylate cyclase, stimulation of inositol phosphate generation, activation of MAPK.
References:  4,19,59
Effects of agonists/allosteric regulators on rat calcium sensing receptor-transfected CHO cells.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of inositol phosphate generation, inhibition of adenylate cyclase.
References:  57,90
Measurement of cytosolic calcium concentration, adenylate cyclase activity, inositol phosphate generatation and activity of MAPK.
Species:  Mouse
Tissue:  AtT-20 cells.
Response measured:  Increase in intracellular Ca2+, inhibition of adenylate cyclase, stimulation of inositol phosphate generation, activation of MAPK.
References:  39
Functional Assay Comments
In addition to these two calcium sensing receptor transfected cell systems, measurement of the same responses AtT-20 cells [57] have also proven to be useful test systems.
Physiological Functions Click here for help
Inhibition of PTH secretion and parathyroid cellular proliferation.
Species:  Human
Tissue:  Parathyroid glands or cells.
References:  78,82
Inhibition of PTH secretion and parathyroid cellular proliferation.
Species:  Rat
Tissue:  Parathyroid glands or cells.
References:  114
Inhibition of PTH-stimulated phosphate excretion in the proximal tubule.
Species:  Mouse
Tissue:  Microdissected in vitro tubule preparations.
References:  3
Inhibition of vasopressin-stimulated reabsorption of water in the renal inner medullary collecting duct.
Species:  Rat
Tissue:  Microdissected in vitro tubule preparations.
References:  105
Stimulation of PTHrP secretion in vitro.
Species:  Human
Tissue:  Prostate cell line.
References:  103
Stimulation of calcitonin secretion from thyroidal C-cells.
Species:  Rat
Tissue:  C-cell cell line rMTC44-2.
References:  44
Stimulation of calcitonin secretion from thyroidal C-cells.
Species:  Human
Tissue:  C-cell cell lines.
References:  42
Promotion of differentiation of keratinocytes.
Species:  Mouse
Tissue:  Primary cultures of keratinocytes, intact mouse epidermis in vivo.
References:  61,83,112
Stimulation of secretion of ACTH.
Species:  Mouse
Tissue:  Studies using the murine AtT-20 cell line.
References:  41
Stimulation of secretion of ACTH.
Species:  Human
Tissue:  In vivo.
References:  47
Inhibition of PTH secretion and parathyroid cellular proliferation.
Species:  Mouse
Tissue:  Parathyroid glands or cells.
References:  51
Inhibition of renal tubular reabsorption of calcium and magnesium in the renal thick ascending limb.
Species:  Mouse
Tissue:  Microdissected in vitro tubule preparations.
References:  7,36,76
Stimulation of PTHrP secretion in vitro.
Species:  Human
Tissue:  Breast and prostate cancer cell lines.
References:  103-104
Stimulation of PTHrP secretion in vitro.
Species:  Rat
Tissue:  Testicular cancer cells line H-500.
References:  102
Stimulation of calcitonin secretion from thyroidal C-cells.
Species:  Mouse
Tissue:  In vivo.
References:  43
Inhibition of PTHrP secretion in vitro and in vivo.
Species:  Mouse
Tissue:  Breast epithelial cells.
References:  113
Regulation of hematopoietic cell retention in bone marrow.
Species:  Mouse
Tissue:  Hematopoietic stem cells.
References:  1
Inhibition of colonic fluid secretion.
Species:  Rat
Tissue:  Perfused colon crypts.
References:  46
Stimulation of expression of cyclooxygenase COX-2.
Species:  Human
Tissue:  Jaw cyst fibroblasts.
References:  85
Regulation of secretion of BMP-2 and Noggin.
Species:  Human
Tissue:  18Co colonic myofibroblasts.
References:  88
Regulation in intracellular pH.
Species:  Mouse
Tissue:  In vitro perfused cells of the medullary thick ascending limb.
References:  2
Regulation of expression/secretion of chemokines (CXCL-9, CXCL-10 and MCP-3).
Species:  Mouse
Tissue:  GnRH neurons.
References:  6
Stimulation of gastric acid secretion.
Species:  Mouse
Tissue:  Gastric glands in vitro.
References:  94
Inhibition of proliferation of colonic crypt cells.
Species:  Human
Tissue:  Colon cancer cell line.
References:  64
Stimulation of non-selective cation channel.
Species:  Rat
Tissue:  Hippocampal neurons.
References:  130
Modulation of chondrocyte differentiation.
Species:  Mouse
Tissue:  Cultured chondrocyte cells.
References:  98
Physiological Consequences of Altering Gene Expression Click here for help
Absent expression of calcium-sensing receptor in calcium receptor knockout mice removes the tonic inhibitory action of extracellular calcium on PTH secretion and parathyroid cellular proliferation and impairs keratinocyte differentiation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  51,61,83
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002896 abnormal bone mineralization PMID: 11517179 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000678 abnormal parathyroid gland morphology PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002980 abnormal postural reflex PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0001504 abnormal posture PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0001438 aphagia PMID: 7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0003195 calcinosis PMID: 15347804 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0001304 cataracts PMID: 15347804 
Casr+|CasrNuf CasrNuf/Casr+
either: (involves: 102/Ei * 102/H * C3H/He) or (involves: 102/Ei * C3H/He * C3H/HeH)		 MGI:1351351  MP:0001304 cataracts PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0001265 decreased body size PMID: 11517179 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0001262 decreased body weight PMID: 11517179 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000063 decreased bone density PMID: 7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0002905 decreased circulating parathyroid hormone level PMID: 15347804 
Casr+|CasrNuf CasrNuf/Casr+
either: (involves: 102/Ei * 102/H * C3H/He) or (involves: 102/Ei * C3H/He * C3H/HeH)		 MGI:1351351  MP:0002905 decreased circulating parathyroid hormone level PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0001429 dehydration PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000060 delayed bone ossification PMID: 11517179 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0003112 enlarged parathyroid gland PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000194 hypercalcemia PMID: 7493018 
Casr+|Casrtm1Ces Casrtm1Ces/Casr+
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000194 hypercalcemia PMID: 7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0001566 hyperphosphatemia PMID: 15347804 
Casr+|CasrNuf CasrNuf/Casr+
either: (involves: 102/Ei * 102/H * C3H/He) or (involves: 102/Ei * C3H/He * C3H/HeH)		 MGI:1351351  MP:0001566 hyperphosphatemia PMID: 15347804 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0000195 hypocalcemia PMID: 15347804 
Casr+|CasrNuf CasrNuf/Casr+
either: (involves: 102/Ei * 102/H * C3H/He) or (involves: 102/Ei * C3H/He * C3H/HeH)		 MGI:1351351  MP:0000195 hypocalcemia PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002986 hypocalciuria PMID: 7493018 
Casr+|Casrtm1Ces Casrtm1Ces/Casr+
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002986 hypocalciuria PMID: 7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0002986 hypocalciuria PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000198 hypophosphatemia PMID: 11517179 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0002902 hypophosphaturia PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0010092 increased circulating magnesium level PMID: 7493018 
Casr+|Casrtm1Ces Casrtm1Ces/Casr+
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0010092 increased circulating magnesium level PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002904 increased circulating parathyroid hormone level PMID: 7493018 
Casr+|Casrtm1Ces Casrtm1Ces/Casr+
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002904 increased circulating parathyroid hormone level PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002608 increased hematocrit PMID: 7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0001846 increased inflammatory response PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0003408 increased width of hypertrophic chondrocyte zone PMID: 11517179 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0000069 kyphoscoliosis PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0005202 lethargy PMID: 7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0003199 muscle calcification PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0003114 pigmented parathyroid gland PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0001732 postnatal growth retardation PMID: 7493018 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0002082 postnatal lethality PMID: 11517179  7493018 
CasrNuf CasrNuf/CasrNuf
involves: 102/Ei * C3H/He		 MGI:1351351  MP:0002083 premature death PMID: 15347804 
Casrtm1Ces Casrtm1Ces/Casrtm1Ces
involves: 129X1/SvJ * Black Swiss		 MGI:1351351  MP:0003116 rickets PMID: 11517179 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Epilepsy, idiopathic generalized, susceptibility to, 8; EIG8
Synonyms: Idiopathic generalized epilepsy [Disease Ontology: DOID:1827]
Disease Ontology: DOID:1827
OMIM: 612899
Disease:  Familial hypocalciuric hypercalcemia type 1
OMIM: 145980
Orphanet: ORPHA93372
Disease:  Familial isolated hypoparathyroidism due to impaired PTH secretion
Orphanet: ORPHA189466
Disease:  Hypocalcemia, autosomal dominant, with Bartter syndrome
Synonyms: Autosomal dominant hypocalcemia [Orphanet: ORPHA428]
Bartter syndrome with hypocalcemia [Orphanet: ORPHA263417]
OMIM: 601198
Orphanet: ORPHA428, ORPHA263417
Disease:  Neonatal severe primary hyperparathyroidism
OMIM: 239200
Orphanet: ORPHA417
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Mouse
Description:  Calcium-sensing receptor expressed in differentiating keratinocytes that lacks exon 5 and has been suggested to exert a dominant negative action on the full length receptor, although some other data suggest that it may harbor some intrinsic biological activity.
References:  61,83-84
Type:  Splice variant
Species:  Human
Description:  Calcium sensing receptor expressed in placental cytotrophoblasts and parathyroid gland that lacks exon 3. Its function is unknown.
References:  9

References

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59. Kifor O, MacLeod RJ, Diaz R, Bai M, Yamaguchi T, Yao T, Kifor I, Brown EM. (2001) Regulation of MAP kinase by calcium-sensing receptor in bovine parathyroid and CaR-transfected HEK293 cells. Am J Physiol Renal Physiol, 280: F291-F302. [PMID:11208605]

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