CCK<sub>2</sub> receptor | Cholecystokinin receptors | IUPHAR/BPS Guide to PHARMACOLOGY

CCK2 receptor

Target id: 77

Nomenclature: CCK2 receptor

Family: Cholecystokinin receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for CCK2 receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 447 11p15.4 CCKBR cholecystokinin B receptor 25,33,40,54
Mouse 7 453 7 E3 Cckbr cholecystokinin B receptor 59
Rat 7 452 1q33 Cckbr cholecystokinin B receptor 60
Previous and Unofficial Names
CCK2 receptor | CCK-B receptor | cholecystokinin-2 receptor | CHOLREC | gastrin/cholecystokinin type B receptor | CCK-B/gastrin receptor
Database Links
Specialist databases
GPCRDB gasr_human (Hs), gasr_mouse (Mm), gasr_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
CCK-4 {Sp: Human}
CCK-33 {Sp: Human}
CCK-8 {Sp: Human, Mouse, Rat}
CCK-33 {Sp: Mouse} , CCK-33 {Sp: Rat}
gastrin-17 {Sp: Human} , gastrin-17 {Sp: Mouse} , gastrin-17 {Sp: Rat}
Comments: CCK-58 is an endogenous peptide fragment from the cholecystokinin precursor protein, but there is no affinity data available for this ligand at cholecystokinin receptors. For the rodent homologues of this peptide please see the following ligand entries: CCK-58 (mouse) and CCK-58 (rat). Gastrin-34 is one of the main forms of secreted gastrin present in the blood but there is no activity data for its interactions with this receptor. For the rodent homologues of this peptide please see gastrin-34 (mouse) and gastrin-34 (rat). Desulfated gastrin-14 (minigastrin) is an endogenous antagonist of cholecystokinin and radiolabelled analogues of this peptide are used as probes for this receptor. The gastrin precursor peptide is also cleaved into larger peptides gastrin-52 and gastrin-71.
Potency order of endogenous ligands (Human)
CCK-8 (CCK, P06307) ≥ gastrin-17 (GAST, P01350), desulfated cholecystokinin-8, CCK-4 (CCK, P06307)

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]PBC-264 Rn Full agonist 9.7 pKd 18
pKd 9.7 (Kd 2x10-10 M) [18]
RB-400 Rn Full agonist 9.1 pKi 5
pKi 9.1 (Ki 7.9x10-10 M) [5]
BBL-454 Rn Full agonist 8.6 pKi 5
pKi 8.6 [5]
BC-254 Rn Full agonist 7.4 pKi 18
pKi 7.4 [18]
ARL-15849 Rn Full agonist 6.6 pKi 51
pKi 6.6 [51]
CCK-8 {Sp: Human, Mouse, Rat} Hs Full agonist 9.9 – 10.0 pIC50 25,33
pIC50 9.9 – 10.0 [25,33]
CCK-58 {Sp: Dog} Mm Full agonist 9.5 pIC50 43
pIC50 9.5 [43]
BC-264 Rn Full agonist 9.5 pIC50 5
pIC50 9.5 [5]
pentagastrin Mm Full agonist 9.1 pIC50 23
pIC50 9.1 [23]
PBC-264 Rn Full agonist 9.1 pIC50 26
pIC50 9.1 (IC50 8.6x10-10 M) [26]
[125I]gastrin Hs Full agonist 9.0 pIC50
pIC50 9.0 (IC50 1x10-9 M)
[3H]gastrin Hs Full agonist 9.0 pIC50
pIC50 9.0 (IC50 1x10-9 M)
[125I]DTyr-Gly-[(Nle28,31)CCK-26-33 Hs Full agonist 9.0 pIC50 41
pIC50 9.0 (IC50 1x10-9 M) [41]
CCK-33 {Sp: Human} Hs Full agonist 8.8 pIC50 25
pIC50 8.8 [25]
desulfated cholecystokinin-8 Hs Full agonist 8.3 – 8.7 pIC50 33
pIC50 8.3 – 8.7 [33]
JMV310 Rn Full agonist 8.4 pIC50 46
pIC50 8.4 [46]
gastrin-17 {Sp: Human} Mm Full agonist 8.3 pIC50 23
pIC50 8.3 [23]
CCK-4 {Sp: Human} Hs Full agonist 7.5 pIC50 25
pIC50 7.5 [25]
A-71378 Hs Full agonist 6.5 pIC50 17
pIC50 6.5 [17]
desulfated gastrin-14 {Sp: Human} Hs Agonist - -
gastrin-34 {Sp: Human} Hs Agonist - -
gastrin-71 {Sp: Human} Hs Agonist - -
desulfated gastrin-17 {Sp: Human} Hs Agonist - -
desulfated gastrin-34 {Sp: Human} Hs Agonist - -
desulfated gastrin-71 {Sp: Human} Hs Agonist - -
gastrin-14 {Sp: Human} Hs Agonist - -
View species-specific agonist tables
Agonist Comments
pIC50 values represent inhibition of binding of [125I]CCK.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]PD142308 Cp Antagonist 9.6 pKd 22
pKd 9.6 (Kd 2.5x10-10 M) [22]
[3H]JB-93182 Rn Antagonist 9.5 pKd 19
pKd 9.5 [19]
[3H]L365260 Hs Antagonist 8.2 – 8.5 pKd 39
pKd 8.2 – 8.5 (Kd 5.7x10-9 – 2.9x10-9 M) [39]
[3H]PD140376 Cp Antagonist 9.7 – 10.0 pKi 24
pKi 9.7 – 10.0 (Ki 2x10-10 – 1x10-10 M) [24]
YF-476 Hs Antagonist 9.6 pKi 39
pKi 9.6 [39]
Z-360 Hs Antagonist 9.3 pKi 28
pKi 9.3 [28]
[125I]-BDZ2 Hs Antagonist 8.4 pKi 1
pKi 8.4 (Ki 3.98x10-9 M) [1]
AG-041R Hs Antagonist 8.3 pKi 39
pKi 8.3 [39]
RP-69758 Rn Antagonist 8.0 pKi 6
pKi 8.0 [6]
TP-680 Rn Antagonist 5.7 pKi 2
pKi 5.7 [2]
PD-149164 Mm Antagonist 10.1 pIC50 4
pIC50 10.1 [4]
PD-135666 Mm Antagonist 9.8 pIC50 52
pIC50 9.8 [52]
YF-476 Hs Antagonist 9.7 pIC50 9,55
pIC50 9.7 [9,55]
GV150013 Hs Antagonist 9.4 pIC50 58
pIC50 9.4 (IC50 3.9x10-10 M) [58]
L-740093 Hs Antagonist 9.2 pIC50 39
pIC50 9.2 (IC50 6.3x10-10 M) [39]
YM-022 Hs Antagonist 9.2 pIC50 39
pIC50 9.2 (IC50 6.3x10-10 M) [39]
CI-988 Hs Antagonist 9.1 pIC50 17
pIC50 9.1 [17]
PD-135158 Hs Antagonist 8.9 pIC50 17
pIC50 8.9 [17]
CI-988 Mm Antagonist 8.8 pIC50 23
pIC50 8.8 [23]
itriglumide Rn Antagonist 8.6 pIC50 35
pIC50 8.6 [35]
CI-1015 Mm Antagonist 8.5 pIC50 57
pIC50 8.5 [57]
JNJ-26070109 Hs Antagonist 8.5 pIC50 37
pIC50 8.5 [37]
L-365260 Hs Antagonist 8.4 pIC50 33
pIC50 8.4 (IC50 3.98x10-9 M) [33]
RP73870 Rn Antagonist 8.0 pIC50 34
pIC50 8.0 (IC50 9.8x10-9 M) [34]
LY262691 Rn Antagonist 7.5 pIC50 42
pIC50 7.5 (IC50 3.1x10-8 M) [42]
LY-288513 Hs Antagonist 7.0 pIC50 17
pIC50 7.0 [17]
devazepide Hs Antagonist 6.8 pIC50 33
pIC50 6.8 [33]
tetronothiodin Hs Antagonist 6.7 pIC50 30
pIC50 6.7 [30]
PD-140548 Rn Antagonist 6.6 pIC50 8
pIC50 6.6 [8]
GW-5823 Hs Antagonist 6.0 pIC50 21
pIC50 6.0 [21]
lorglumide Hs Antagonist 5.5 pIC50 17
pIC50 5.5 [17]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  33
Tissue Distribution
Stomach.
Species:  Human
Technique:  RT-PCR, autoradiography, immunohistochemistry.
References:  29,45,48
Exocrine pancreas.
Species:  Human
Technique:  RT-PCR, Northern blot, radioligand binding.
References:  13,27,40,56
Endocrine pancreas.
Species:  Human
Technique:  In situ hybridization, receptor autoradiography, immunohistochemistry.
References:  44,47
Adrenal gland.
Species:  Human
Technique:  RT-PCR.
References:  36
Blood cells.
Species:  Human
Technique:  RT-PCR.
References:  14,49
Adipocytes.
Species:  Rat
Technique:  RT-PCR, radioligand binding.
References:  3
Expression Datasets

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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
COS cells transiently transfected with human CCK2 receptor cDNA.
Species:  Human
Tissue:  COS cells.
Response measured:  Intracellular Ca2+ (Fura-2 AM).
References:  33
COS cells transiently transfected with human CCK2 receptor cDNA.
Species:  Human
Tissue:  COS cells.
Response measured:  IP3 production.
References:  33
CHO cells stably transfected with human CCK2 receptor cDNA.
Species:  Human
Tissue:  CHO cells.
Response measured:  Intracellular Ca2+ (Fura-2 AM).
References:  25
CHO cells stably transfected with human CCK2 receptor cDNA.
Species:  Human
Tissue:  CHO cells.
Response measured:  IP3 production.
References:  25
Physiological Functions
The transfer of rats from a familiar to a novel environment prolongs the increase of extracellular dopamine efflux induced by CCK-8 in the posterior nucleus accumbens.
Species:  Rat
Tissue:  Nucleus accumbens.
References:  31
Rat hippocampal neurones are critically involved in physiological improvement of memory processes induced by CCK2 receptor stimulation.
Species:  Rat
Tissue:  Hippocampal neurones.
References:  50
CCK in the perfusion medium produced a concentration-dependent increase in firing rate of neurones located in ventromedial nuclei of rat hypothalamic slices.
Species:  Rat
Tissue:  Ventromedial nuclei of rat hypothalamus.
References:  7
CCK2 receptor agonists affect nociception and behaviour in rodents.
Species:  Mouse
Tissue:  In vivo (brain).
References:  15
CCK2 receptor antagonist produced an anxiolytic-like action in rats.
Species:  Rat
Tissue:  In vivo (brain).
References:  57
Physiological Consequences of Altering Gene Expression
CCK2 receptor-deficient mice showed an impairment of performance in spontaneous alternation behaviour, supporting the physiological role of CCK2 receptors in attention and/or memory processes.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  16
CCK2 receptor-deficient mice showed a remarkable atrophy of the gastric mucosa.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  38
CCK2 receptor-deficient mice showed a marked increase in basal gastric pH and in plasma gastrin concentration. In the stomach of mutant mice, parietal and enterochromaffin-like cells were decreased. In the antrum, somatostatin cell density decreases and the gastrin cell number increases.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  32
CCK2 receptor-deficient mice showed altered differentiation of gastric ECL cells.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  11
CCK2 receptor-deficient mice showed hyperphagia and increased fat deposition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  12
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0004924 abnormal behavior PMID: 15325774 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0004924 abnormal behavior PMID: 11682252 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckar Cckbr
MGI:99478  MGI:99479  MP:0004924 abnormal behavior PMID: 12459512 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0002128 abnormal blood circulation PMID: 15355324 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99478  MGI:99479  MP:0001777 abnormal body temperature regulation PMID: 15178543 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0004152 abnormal circulating iron level PMID: 18755804 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0001663 abnormal digestive system physiology PMID: 8876222 
Cckbrtm1Kpn Cckbrtm1Kpn/Cckbrtm1Kpn
involves: 129S2/SvPas
MGI:99479  MP:0004141 abnormal enteroendocrine cell morphology PMID: 8978369 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0002910 abnormal excitatory postsynaptic currents PMID: 20392936 
Cckbrtm1Kpn Cckbrtm1Kpn/Cckbrtm1Kpn
involves: 129S2/SvPas
MGI:99479  MP:0003892 abnormal gastric gland PMID: 8978369 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0005209 abnormal gastric mucosa morphology PMID: 8876222 
Cckbrtm1Kpn Cckbrtm1Kpn/Cckbrtm1Kpn
involves: 129S2/SvPas
MGI:99479  MP:0004139 abnormal gastric parietal cell morphology PMID: 8978369 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0002736 abnormal nociception after inflammation PMID: 15355324 
Cckbrtm1Kpn Cckbrtm1Kpn/Cckbrtm1Kpn
involves: 129S2/SvPas
MGI:99479  MP:0005218 abnormal pancreatic delta cell morphology PMID: 8978369 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6
MGI:99479  MP:0008872 abnormal physiological response to xenobiotic PMID: 11403953 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0000470 abnormal stomach morphology PMID: 8876222 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0001364 decreased anxiety-related response PMID: 15325774 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0001364 decreased anxiety-related response PMID: 15013032 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0001262 decreased body weight PMID: 15325774 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99478  MGI:99479  MP:0001262 decreased body weight PMID: 15178543 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0001262 decreased body weight PMID: 11925470  15168241 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckar Cckbr
MGI:99478  MGI:99479  MP:0001262 decreased body weight PMID: 12459512 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0001442 decreased grooming behavior PMID: 15325774 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0008734 decreased susceptibility to endotoxin shock PMID: 16857893 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99479  MP:0009854 delayed gastric emptying PMID: 15168241 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0009854 delayed gastric emptying PMID: 15168241 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6
MGI:99479  MP:0009749 enhanced behavioral response to addictive substance PMID: 11403953 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6
MGI:99479  MP:0009753 enhanced behavioral response to morphine PMID: 11403953 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0001399 hyperactivity PMID: 11682252  16857893 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6
MGI:99479  MP:0001399 hyperactivity PMID: 11403953 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0005498 hyporesponsive to tactile stimuli PMID: 15355324 
Cckbr+|Cckbrtm1Tom Cckbrtm1Tom/Cckbr+
B6.129S4-Cckbr
MGI:99479  MP:0005498 hyporesponsive to tactile stimuli PMID: 15355324 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6
MGI:99479  MP:0009758 impaired behavioral response to cocaine PMID: 11403953 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0001405 impaired coordination PMID: 11682252 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0003829 impaired febrile response PMID: 16857893 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckbr
MGI:99479  MP:0001363 increased anxiety-related response PMID: 12459512 
Cckbrtm1Kpn Cckbrtm1Kpn/Cckbrtm1Kpn
involves: 129S2/SvPas
MGI:99479  MP:0004731 increased circulating gastrin level PMID: 8978369 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0004731 increased circulating gastrin level PMID: 18755804  8876222 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99479  MP:0004731 increased circulating gastrin level PMID: 15168241 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0003911 increased drinking behavior PMID: 16857893 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0003909 increased eating behavior PMID: 16857893 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99479  MP:0003909 increased eating behavior PMID: 11925470 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0003909 increased eating behavior PMID: 11925470 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99479  MP:0004889 increased energy expenditure PMID: 11925470 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0004889 increased energy expenditure PMID: 11925470 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0003917 increased kidney weight PMID: 11925470 
Cckbrtm1Tom Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99479  MP:0008807 increased liver iron level PMID: 18755804 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0009108 increased pancreas weight PMID: 11925470 
Cckbrtm1Kpn Cckbrtm1Kpn/Cckbrtm1Kpn
involves: 129S2/SvPas
MGI:99479  MP:0008006 increased stomach pH PMID: 8978369 
Biologically Significant Variants
Type:  Splice variant
Species:  Human
Description:  A splice variant of the CCK2 receptor was identified which differed from the predominant CCK2 receptor isoform by the presence of intron 4. This variant was identified in human pancreatic cancer specimens and plays a crucial role in the growth of pancreatic cancer.
References:  53
Type:  Splice variant
Species:  Human
Description:  A splice variant of the CCK2 receptor was identified with additional amino acids (GGAGP) in exon 4 by screening a human EMBL phage library.
References:  54
Type:  Splice variant
Species:  Human
Description:  A splice variant of the CCK2 receptor identified in intron 4 is expressed in colorectal cancers but not in the normal colonic mucosa adjacent to the cancer. This variant receptor is constitutively active in tumour cells, and increases Src-dependent HIF-1α expression and tumour growth.
References:  10,20

References

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1. Akgün E, Körner M, Gao F, Harikumar KG, Waser B, Reubi JC, Portoghese PS, Miller LJ. (2009) Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors. J. Med. Chem., 52 (7): 2138-47. [PMID:19271701]

2. Akiyama T, Tachibana I, Hirohata Y, Shirohara H, Yamamoto M, Otsuki M. (1996) Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol, 117: 1558-1564. [PMID:8730754]

3. Attoub S, Levasseur S, Buyse M, Goïot H, Laigneau JP, Moizo L, Hervatin F, Le Marchand-Brustel Y, Lewin JM, Bado A. (1999) Physiological role of cholecystokinin B/gastrin receptor in leptin secretion. Endocrinology, 140: 4406-4410. [PMID:10499492]

4. Augelli-Szafran CE, Horwell DC, Kneen C, Ortwine DF, Pritchard MC, Purchase TS, Roth BD, Trivedi BK, Hill D, Suman-Chauhan N, Webdale L. (1996) Cholecystokinin B antagonists. Synthesis and quantitative structure-activity relationships of a series of C-terminal analogues of CI-988. Bioorg Med Chem, 4: 1733-1745. [PMID:8931944]

5. Bellier B, Dugave C, Etivant F, Genet R, Gigoux V, Garbay C. (2004) Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties. Bioorg Med Chem Lett, 14: 369-372. [PMID:14698161]

6. Bertrand P, Böhme GA, Durieux C, Guyon C, Capet M, Jeantaud B, Boudeau P, Ducos B, Pendley CE, Martin GE. (1994) Pharmacological properties of ureido-acetamides, new potent and selective non-peptide CCKB/gastrin receptor antagonists. Eur J Pharmacol, 262: 233-245. [PMID:7813588]

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Quan Chen, Fan Gao, Laurence J. Miller.
Cholecystokinin receptors: CCK2 receptor. Last modified on 26/06/2018. Accessed on 13/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=77.