CCK<sub>1</sub> receptor | Cholecystokinin receptors | IUPHAR/BPS Guide to PHARMACOLOGY

CCK1 receptor

Target id: 76

Nomenclature: CCK1 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 CCK1 receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 428 4p15.1-p15.2 CCKAR cholecystokinin A receptor 10,56
Mouse 7 436 5 C1 Cckar cholecystokinin A receptor 26,52
Rat 7 444 14q11 Cckar cholecystokinin A receptor 51,59
Previous and Unofficial Names
CCK1-R | cholecystokinin receptor type A | cholecystokinin-1 receptor
Database Links
Specialist databases
GPCRDB cckar_human (Hs), cckar_mouse (Mm), cckar_rat (Rn)
Other databases
CATH/Gene3D
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).
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
CCK-33 {Sp: Human} Rn Full agonist 9.3 pKd 20
pKd 9.3 [20]
ARL-15849 Rn Full agonist 10.5 pKi 49
pKi 10.5 [49]
PD136450 Rn Full agonist 5.9 pKi 5
pKi 5.9 [5]
SR146131 Hs Full agonist 9.3 pIC50 4
pIC50 9.3 [4]
CCK-58 {Sp: Dog} Mm Full agonist 9.2 pIC50 41
pIC50 9.2 [41]
[125I]DTyr-Gly-[(Nle28,31)CCK-26-33 Hs Full agonist 9.0 pIC50 40
pIC50 9.0 (IC50 1x10-9 M) [40]
CCK-8 {Sp: Human, Mouse, Rat} Rn Full agonist 7.2 – 9.9 pIC50 19
pIC50 9.9 [19]
pIC50 7.2 [19]
A-71623 Rn Full agonist 8.4 pIC50 3
pIC50 8.4 (IC50 3.98x10-9 M) [3]
JMV180 Hs Full agonist 8.3 pIC50 25
pIC50 8.3 (IC50 5.44x10-9 M) [25]
GW-5823 Hs Full agonist 7.6 pIC50 18
pIC50 7.6 (IC50 2.51x10-8 M) [18]
CE-326597 Hs Agonist 7.5 pIC50 13
pIC50 7.5 (IC50 3.17x10-8 M) [13]
Glaxo-11p Hs Full agonist 7.2 pIC50 2
pIC50 7.2 [2]
pentagastrin Rn Full agonist 6.2 pIC50 19
pIC50 6.2 [19]
gastrin-17 {Sp: Human} Rn Full agonist 6.1 pIC50 19
pIC50 6.1 [19]
CCK-4 {Sp: Human} Rn Full agonist 5.3 pIC50 19
pIC50 5.3 [19]
rebamipide Rn Full agonist 4.4 pIC50 33
pIC50 4.4 [33]
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
[3H]devazepide Hs Antagonist 9.7 pKd 8
pKd 9.7 (Kd 2x10-10 M) [8]
TP-680 Rn Antagonist 8.9 pKi 1
pKi 8.9 [1]
JNJ-17156516 Hs Antagonist 8.0 pKi 36
pKi 8.0 [36]
dexloxiglumide Hs Antagonist 7.5 pKi 36
pKi 7.5 [36]
YM-022 Rn Antagonist 6.8 pKi 37
pKi 6.8 [37]
L-740093 Rn Antagonist 5.8 pKi 39
pKi 5.8 [39]
CI-1015 Rn Antagonist 5.3 pKi 55
pKi 5.3 [55]
devazepide Rn Antagonist 9.7 pIC50 19
pIC50 9.7 (IC50 1.9x10-10 M) [19]
lintitript Rn Antagonist 9.7 pIC50 17
pIC50 9.7 [17]
T-0632 Rn Antagonist 9.6 pIC50 53
pIC50 9.6 (IC50 2.5x10-10 M) [53]
pranazepide Rn Antagonist 9.4 pIC50 21
pIC50 9.4 [21]
IQM-97423 Rn Antagonist 9.0 pIC50 27
pIC50 9.0 [27]
PD-140548 Rn Antagonist 8.6 pIC50 50
pIC50 8.6 (IC50 2.5x10-9 M) [50]
lintitript Hs Antagonist 8.3 pIC50 16
pIC50 8.3 (IC50 5x10-9 M) [16]
SC-50998 Rn Antagonist 7.8 pIC50 15
pIC50 7.8 [15]
lorglumide Rn Antagonist 6.7 – 8.2 pIC50 19,22
pIC50 6.7 – 8.2 (IC50 1.99x10-7 – 6.31x10-9 M) [19,22]
YF-476 Rn Antagonist 6.9 pIC50 47
pIC50 6.9 [47]
VL-0395 Rn Antagonist 6.7 pIC50 57
pIC50 6.7 [57]
L-365260 Rn Antagonist 6.6 pIC50 19
pIC50 6.6 [19]
loxiglumide Rn Antagonist 6.5 pIC50 48
pIC50 6.5 [48]
L-736380 Rn Antagonist 6.4 pIC50 7
pIC50 6.4 [7]
PD-135158 Rn Antagonist 5.9 pIC50 19
pIC50 5.9 [19]
CI-988 Rn Antagonist 5.6 pIC50 19
pIC50 5.6 [19]
proglumide Rn Antagonist 2.2 pIC50 29
pIC50 2.2 [29]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  10,56
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  30
Tissue Distribution
Kidney.
Species:  Human
Technique:  RT-PCR.
References:  32
Blood cells.
Species:  Human
Technique:  RT-PCR.
References:  46
Adrenal gland.
Species:  Human
Technique:  RT-PCR, autoradiography.
References:  31
Stomach.
Species:  Human
Technique:  RT-PCR, autoradiography, immunohistochemistry.
References:  43,45
Exocrine pancreas.
Species:  Human
Technique:  RT-PCR.
References:  23
Endocrine pancreas.
Species:  Human
Technique:  Immunohistochemistry.
References:  35
Gallbladder.
Species:  Human
Technique:  Radioligand binding.
References:  54
Bowel.
Species:  Human
Technique:  Autoradiography.
References:  42,44
Vagal afferent fibres.
Species:  Human
Technique:  RT-PCR, in situ hybridisation, radioligand binding.
References:  6,34
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 CCK1 receptor cDNA.
Species:  Human
Tissue:  COS cells.
Response measured:  IP3 production.
References:  10
COS cells transiently transfected with human CCK1 receptor cDNA.
Species:  Human
Tissue:  COS cells.
Response measured:  Intracellular Ca2+ (Fura-2 AM).
References:  56
Physiological Functions
CCK-8 (sulphated) and CCK-8 (desulphated) produced an increase in the amplitude of EMG and a decrease in mean respiratory interval.
Species:  Rat
Tissue:  Nuclei of the solitary tract, ventral respiratory group and Kolliker-Fuse nucleus.
References:  12
CCK acts at CCK1 receptors on acinar cells in the pancreas to stimulate the secretion of the digestive enzyme pancreatic amylase.
Species:  Rat
Tissue:  Pancreatic acini.
References:  28
CCK acts at CCK1 receptors to decrease feeding for the rat.
Species:  Rat
Tissue:  Intestine.
References:  11
Physiological Consequences of Altering Gene Expression
CCK1 receptor-deficient rats showed increased gastric acid secretion.
Species:  Rat
Tissue: 
Technique:  Receptor-deficient strain (OLETF).
References:  24
CCK1 receptor-deficient rats showed impaired learning and memory.
Species:  Rat
Tissue: 
Technique:  Receptor-deficient strain (OLETF).
References:  38
CCK1 receptor-deficient rats showed altered extracellular dopamine concentration in the brain.
Species:  Rat
Tissue: 
Technique:  Receptor-deficient strain (OLETF).
References:  14
CCK1 receptor-deficient mice showed severely impaired intestinal feedback in response to lipid.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  60
CCK1 receptor-deficient mice showed increased intestinal cholesterol absorption and susceptibility to cholesterol cholelithiasis.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  58
CCK1 receptor-deficient rats showed reduced CCK-induced Fos expression in the hindbrain, nodose ganglia and enteric neurones.
Species:  Rat
Tissue: 
Technique:  Receptor-deficient strain (OLETF).
References:  9
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
B6.129S4-Cckar Cckbr
MGI:99478  MGI:99479  MP:0004924 abnormal behavior PMID: 12459512 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0004773 abnormal bile composition PMID: 15314689 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0005365 abnormal bile salt homeostasis PMID: 15314689 
Cckartm1Kym Cckartm1Kym/Cckartm1Kym
B6.129S4-Cckar
MGI:99478  MP:0001777 abnormal body temperature regulation PMID: 15178543 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae * C57BL/6J
MGI:99478  MGI:99479  MP:0001777 abnormal body temperature regulation PMID: 15178543 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0005278 abnormal cholesterol homeostasis PMID: 15314689 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv * 129S1/Sv * 129X1/SvJ
MGI:99478  MP:0005449 abnormal food intake PMID: 9927499 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:99478  MP:0000783 abnormal forebrain morphology PMID: 15152034 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:99478  MP:0006009 abnormal neuronal migration PMID: 15152034 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv * 129S1/Sv * 129X1/SvJ
MGI:99478  MP:0006092 abnormal olfactory neuron morphology PMID: 18305161 
Cckartm1Kym Cckartm1Kym/Cckartm1Kym
involves: 129S4/SvJae * C57BL/6J
MGI:99478  MP:0002694 abnormal pancreas secretion PMID: 11893936 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv * 129S1/Sv * 129X1/SvJ
MGI:99478  MP:0004275 abnormal postnatal subventricular zone morphology PMID: 18305161 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv * 129S1/Sv * 129X1/SvJ
MGI:99478  MP:0004279 abnormal rostral migratory stream morphology PMID: 18305161 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0006002 abnormal small intestinal transit time PMID: 15314689 
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 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv * 129S1/Sv * 129X1/SvJ
MGI:99478  MP:0004981 decreased neuronal precursor cell number PMID: 18305161 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0009854 delayed gastric emptying PMID: 15168241 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0009343 dilated gallbladder PMID: 15314689 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv * 129S1/Sv * 129X1/SvJ
MGI:99478  MP:0002830 gallstones PMID: 9927499 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0002830 gallstones PMID: 15314689 
Cckartm1Kym Cckartm1Kym/Cckartm1Kym
B6.129S4-Cckar
MGI:99478  MP:0001399 hyperactivity PMID: 12459512 
Cckartm1Kpn Cckartm1Kpn/Cckartm1Kpn
involves: 129S/SvEv
MGI:99478  MP:0002646 increased cholesterol absorption PMID: 15314689 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0003909 increased eating behavior 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 
Cckartm1Kym|Cckbrtm1Tom Cckartm1Kym/Cckartm1Kym,Cckbrtm1Tom/Cckbrtm1Tom
involves: 129S4/SvJae
MGI:99478  MGI:99479  MP:0009108 increased pancreas weight PMID: 11925470 

References

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1. 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]

2. Aquino CJ, Armour DR, Berman JM, Birkemo LS, Carr RA, Croom DK, Dezube M, Dougherty RW, Ervin GN, Grizzle MK, Head JE, Hirst GC, James MK, Johnson MF, Miller LJ, Queen KL, Rimele TJ, Smith DN, Sugg EE. (1996) Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger". J Med Chem, 39: 562-569. [PMID:8558528]

3. Asin KE, Bednarz L, Nikkel AL, Gore PA, Montana WE, Cullen MJ, Shiosaki K, Craig R, Nadzan AM. (1992) Behavioral effects of A71623, a highly selective CCK-A agonist tetrapeptide. Am J Physiol, 263: R125-R135. [PMID:1636779]

4. Bignon E, Bachy A, Boigegrain R, Brodin R, Cottineau M, Gully D, Herbert JM, Keane P, Labie C, Molimard JC, Olliero D, Oury-Donat F, Petereau C, Prabonnaud V, Rockstroh MP, Schaeffer P, Servant O, Thurneyssen O, Soubrie P, Pascal M, Maffrand JP, Le Fur G. (1999) SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther, 289: 742-751. [PMID:10215648]

5. Blevins GT, van de Westerlo EM, Yule DI, Williams JA. (1994) Characterization of cholecystokininA receptor agonist activity by a family of cholecystokininB receptor antagonists. J Pharmacol Exp Ther, 269: 911-916. [PMID:7516969]

6. Broberger C, Holmberg K, Shi TJ, Dockray G, Hökfelt T. (2001) Expression and regulation of cholecystokinin and cholecystokinin receptors in rat nodose and dorsal root ganglia. Brain Res, 903: 128-140. [PMID:11382396]

7. Castro JL, Ball RG, Broughton HB, Russell MG, Rathbone D, Watt AP, Baker R, Chapman KL, Fletcher AE, Patel S, Smith AJ, Marshall GR, Ryecroft W, Matassa VG. (1996) Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas. J Med Chem, 39: 842-849. [PMID:8632408]

8. Chang RS, Lotti VJ, Chen TB, Kunkel KA. (1986) Characterization of the binding of [3H]-(+/-)-L-364,718: a new potent, nonpeptide cholecystokinin antagonist radioligand selective for peripheral receptors. Mol. Pharmacol., 30 (3): 212-7. [PMID:3018478]

9. Covasa M, Ritter RC. (2005) Reduced CCK-induced Fos expression in the hindbrain, nodose ganglia, and enteric neurons of rats lacking CCK-1 receptors. Brain Res, 1051: 155-163. [PMID:16005445]

10. de Weerth A, Pisegna JR, Huppi K, Wank SA. (1993) Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor. Biochem Biophys Res Commun, 194: 811-818. [PMID:8343165]

11. Dourish CT, Ruckert AC, Tattersall FD, Iversen SD. (1989) Evidence that decreased feeding induced by systemic injection of cholecystokinin is mediated by CCK-A receptors. Eur J Pharmacol, 173: 233-234. [PMID:2625140]

12. Ellenberger HH, Smith FM. (1999) Sulfated cholecystokinin octapeptide in the rat: pontomedullary distribution and modulation of the respiratory pattern. Can J Physiol Pharmacol, 77: 490-504. [PMID:10535709]

13. Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM et al.. (2010) Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity. Bioorg. Med. Chem. Lett., 20 (22): 6797-801. [PMID:20851601]

14. Feifel D, Shilling PD, Kuczenski R, Segal DS. (2003) Altered extracellular dopamine concentration in the brains of cholecystokinin-A receptor deficient rats. Neurosci Lett, 348: 147-150. [PMID:12932815]

15. Flynn DL, Villamil CI, Becker DP, Gullikson GW, Moummi C, Yang D. (1992) 1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists. Bioorg Med Chem Lett, 2(10): 1251-1256.

16. Gouldson P, Legoux P, Carillon C, Delpech B, Le Fur G, Ferrara P, Shire D. (2000) The agonist SR 146131 and the antagonist SR 27897 occupy different sites on the human CCK(1) receptor. Eur. J. Pharmacol., 400 (2-3): 185-94. [PMID:10988332]

17. Gully D, Fréhel D, Marcy C, Spinazzé A, Lespy L, Neliat G, Maffrand JP, Le Fur G. (1993) Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. Eur J Pharmacol, 232: 13-19. [PMID:7681406]

18. Henke BR, Aquino CJ, Birkemo LS, Croom DK, Dougherty RW, Ervin GN, Grizzle MK, Hirst GC, James MK, Johnson MF, Queen KL, Sherrill RG, Sugg EE, Suh EM, Szewczyk JW, Unwalla RJ, Yingling J, Willson TM. (1997) Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists. J Med Chem, 40: 2706-2725. [PMID:9276016]

19. Hughes J, Boden P, Costall B, Domeney A, Kelly E, Horwell DC, Hunter JC, Pinnock RD, Woodruff GN. (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A, 87: 6728-6732. [PMID:1975695]

20. Innis RB, Snyder SH. (1980) Distinct cholecystokinin receptors in brain and pancreas. Proc Natl Acad Sci U S A, 77: 6917-6921. [PMID:6256771]

21. Ito H, Sogabe H, Nakarai T, Sato Y, Tomoi M, Kadowaki M, Matsuo M, Tokoro K, Yoshida K. (1994) Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide. J Pharmacol Exp Ther, 268: 571-575. [PMID:7509389]

22. Iwamoto Y, Yamamoto R, Kuzuya T. (1987) CR-1409: a potent inhibitor of cholecystokinin-stimulated amylase release and cholecystokinin binding in rat pancreatic acini. Pancreas, 2: 85-90. [PMID:2437574]

23. Ji B, Bi Y, Simeone D, Mortensen RM, Logsdon CD. (2001) Human pancreatic acinar cells lack functional responses to cholecystokinin and gastrin. Gastroenterology, 121: 1380-1390. [PMID:11729117]

24. Kanagawa K, Nakamura H, Murata I, Yosikawa I, Otsuki M. (2002) Increased gastric acid secretion in cholecystokinin-1 receptor-deficient Otsuka Long-Evans Tokushima fatty rats. Scand J Gastroenterol, 37: 9-16. [PMID:11843043]

25. Kennedy K, Escrieut C, Dufresne M, Clerc P, Vaysse N, Fourmy D. (1995) Identification of a region of the N-terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK. Biochem. Biophys. Res. Commun., 213 (3): 845-52. [PMID:7654246]

26. Lacourse KA, Lay JM, Swanberg LJ, Jenkins C, Samuelson LC. (1997) Molecular structure of the mouse CCK-A receptor gene. Biochem Biophys Res Commun, 236: 630-635. [PMID:9245702]

27. Latorre M, Bartolomé-Nebreda JM, García-López MT, González-Muñiz R, Herranz R, Del Río J, Cenarruzabeitia E. (2004) Pharmacological study of IQM-97,423, a potent and selective CCK1 receptor antagonist with protective effect in experimental acute pancreatitis. Pharmacology, 72: 68-76. [PMID:15331911]

28. Liddle RA, Goldfine ID, Williams JA. (1984) Bioassay of plasma cholecystokinin in rats: effects of food, trypsin inhibitor, and alcohol. Gastroenterology, 87: 542-549. [PMID:6204904]

29. Makovec F, Bani M, Cereda R, Chisté R, Pacini MA, Revel L, Rovati LA, Rovati LC, Setnikar I. (1987) Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung, 37: 1265-1268. [PMID:3440035]

30. Marino CR, Leach SD, Schaefer JF, Miller LJ, Gorelick FS. (1993) Characterization of cAMP-dependent protein kinase activation by CCK in rat pancreas. FEBS Lett, 316: 48-52. [PMID:7678554]

31. Mazzocchi G, Malendowicz LK, Aragona F, Spinazzi R, Nussdorfer GG. (2004) Cholecystokinin (CCK) stimulates aldosterone secretion from human adrenocortical cells via CCK2 receptors coupled to the adenylate cyclase/protein kinase A signaling cascade. J Clin Endocrinol Metab, 89: 1277-1284. [PMID:15001623]

32. Monstein HJ, Nylander AG, Salehi A, Chen D, Lundquist I, Håkanson R. (1996) Cholecystokinin-A and cholecystokinin-B/gastrin receptor mRNA expression in the gastrointestinal tract and pancreas of the rat and man. A polymerase chain reaction study. Scand J Gastroenterol, 31: 383-390. [PMID:8726308]

33. Moon SJ, An JM, Kim J, Lee SI, Ahn W, Kim KH, Seo JT. (2004) Pharmacological characterization of rebamipide: its cholecystokinin CCK1 receptor binding profile and effects on Ca2+ mobilization and amylase release in rat pancreatic acinar cells. Eur J Pharmacol, 505: 61-66. [PMID:15556137]

34. Moriarty P, Dimaline R, Thompson DG, Dockray GJ. (1997) Characterization of cholecystokininA and cholecystokininB receptors expressed by vagal afferent neurons. Neuroscience, 79: 905-913. [PMID:9219953]

35. Morisset J, Julien S, Lainé J. (2003) Localization of cholecystokinin receptor subtypes in the endocine pancreas. J Histochem Cytochem, 51: 1501-1513. [PMID:14566022]

36. Morton MF, Barrett TD, Yan W, Freedman JM, Lagaud G, Prendergast CE, Moreno V, Pyati J, Figueroa K, Li L, Wu X, Rizzolio M, Breitenbucher JG, McClure K, Shankley NP. (2007) 3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl) -1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide. J Pharmacol Exp Ther, 323: 562-569. [PMID:17684117]

37. Nishida A, Miyata K, Tsutsumi R, Yuki H, Akuzawa S, Kobayashi A, Kamato T, Ito H, Yamano M, Katuyama Y. (1994) Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3- (3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther, 269: 725-731. [PMID:7910212]

38. Nomoto S, Miyake M, Ohta M, Funakoshi A, Miyasaka K. (1999) Impaired learning and memory in OLETF rats without cholecystokinin (CCK)-A receptor. Physiol Behav, 66: 869-872. [PMID:10405116]

39. Patel S, Smith AJ, Chapman KL, Fletcher AE, Kemp JA, Marshall GR, Hargreaves RJ, Ryecroft W, Iversen LL, Iversen SD. (1994) Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo. Mol Pharmacol, 46: 943-948. [PMID:7969084]

40. Powers SP, Pinon DI, Miller LJ. (1988) Use of N,O-bis-Fmoc-D-Tyr-ONSu for introduction of an oxidative iodination site into cholecystokinin family peptides. Int. J. Pept. Protein Res., 31 (5): 429-34. [PMID:3410633]

41. Reeve JR, McVey DC, Bunnett NW, Solomon TE, Keire DA, Ho FJ, Davis MT, Lee TD, Shively JE, Vigna SR. (2002) Differences in receptor binding and stability to enzymatic digestion between CCK-8 and CCK-58. Pancreas, 25: e50-e55. [PMID:12370550]

42. Rettenbacher M, Reubi JC. (2001) Localization and characterization of neuropeptide receptors in human colon. Naunyn Schmiedebergs Arch Pharmacol, 364: 291-304. [PMID:11683516]

43. Reubi JC, Waser B, Läderach U, Stettler C, Friess H, Halter F, Schmassmann A. (1997) Localization of cholecystokinin A and cholecystokinin B-gastrin receptors in the human stomach. Gastroenterology, 112: 1197-1205. [PMID:9098003]

44. Reubi JC, Waser B, Schmassmann A, Laissue JA. (1999) Receptor autoradiographic evaluation of cholecystokinin, neurotensin, somatostatin and vasoactive intestinal peptide receptors in gastro-intestinal adenocarcinoma samples: where are they really located?. Int J Cancer, 81: 376-386. [PMID:10209952]

45. Schmitz F, Göke MN, Otte JM, Schrader H, Reimann B, Kruse ML, Siegel EG, Peters J, Herzig KH, Fölsch UR, Schmidt WE. (2001) Cellular expression of CCK-A and CCK-B/gastrin receptors in human gastric mucosa. Regulatory Peptides, 102: 101-110. [PMID:11730982]

46. Schmitz F, Schrader H, Otte JM, Schmitz H, Stuber E, Herzig KH, Schmidt WE. (2001) Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells. Regulatory Peptides, 101: 25-33. [PMID:11495676]

47. Semple G, Ryder H, Rooker DP, Batt AR, Kendrick DA, Szelke M, Ohta M, Satoh M, Nishida A, Akuzawa S, Miyata K. (1997) (3R)-N-(1-(tert-butylcarbonylmethyl) -2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4 -benzodiazepin-3-yl)-N' -(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. J Med Chem, 40: 331-341. [PMID:9022799]

48. Setnikar I, Bani M, Cereda R, Chisté R, Makovec F, Pacini MA, Revel L, Rovati LC, Rovati LA. (1987) Pharmacological characterisation of a new potent and specific nonpolypeptidic cholecystokinin antagonist. Arzneimittelforschung, 37: 703-707. [PMID:3663268]

49. Simmons RD, Kaiser FC, Pierson ME, Rosamond JR. (1998) ARL 15849: a selective CCK-A agonist with anorectic activity in the rat and dog. Pharmacol Biochem Behav, 59: 439-444. [PMID:9476993]

50. Singh L, Field MJ, Hill DR, Horwell DC, McKnight AT, Roberts E, Tang KW, Woodruff GN. (1995) Peptoid CCK receptor antagonists: pharmacological evaluation of CCKA, CCKB and mixed CCKA/B receptor antagonists. Eur J Pharmacol, 286: 185-191. [PMID:8605955]

51. Takata Y, Takiguchi S, Funakoshi A, Kono A. (1995) Gene structure of rat cholecystokinin type-A receptor. Biochem Biophys Res Commun, 213: 958-966. [PMID:7654260]

52. Takata Y, Takiguchi S, Kataoka K, Funakoshi A, Miyasaka K, Kono A. (1997) Mouse cholecystokinin type-A receptor gene and its structural analysis. Gene, 187: 267-271. [PMID:9099891]

53. Taniguchi H, Yazaki N, Endo T, Nagasaki M. (1996) Pharmacological profile of T-0632, a novel potent and selective CCKA receptor antagonist, in vitro. Eur J Pharmacol, 304: 147-154. [PMID:8813597]

54. Tokunaga Y, Cox KL, Coleman R, Concepcion W, Nakazato P, Esquivel CO. (1993) Characterization of cholecystokinin receptors on the human gallbladder. Surgery, 113: 155-162. [PMID:7679224]

55. Trivedi BK, Padia JK, Holmes A, Rose S, Wright DS, Hinton JP, Pritchard MC, Eden JM, Kneen C, Webdale L, Suman-Chauhan N, Boden P, Singh L, Field MJ, Hill D. (1998) Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R) -tryptophan derivative (CI-1015) with an improved pharmacokinetic profile. J Med Chem, 41: 38-45. [PMID:9438020]

56. Ulrich CD, Ferber I, Holicky E, Hadac E, Buell G, Miller LJ. (1993) Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor. Biochem Biophys Res Commun, 193: 204-211. [PMID:8503909]

57. Varnavas A, Lassiani L, Valenta V, Berti F, Mennuni L, Makovec F. (2003) Anthranilic acid derivatives: a new class of non-peptide CCK1 receptor antagonists. Bioorg Med Chem, 11: 741-751. [PMID:12538004]

58. Wang DQ, Schmitz F, Kopin AS, Carey MC. (2004) Targeted disruption of the murine cholecystokinin-1 receptor promotes intestinal cholesterol absorption and susceptibility to cholesterol cholelithiasis. J Clin Invest, 114: 521-528. [PMID:15314689]

59. Wank SA, Harkins R, Jensen RT, Shapira H, de Weerth A, Slattery T. (1992) Purification, molecular cloning, and functional expression of the cholecystokinin receptor from rat pancreas. Proc Natl Acad Sci U S A, 89: 3125-3129. [PMID:1313582]

60. Whited KL, Thao D, Lloyd KC, Kopin AS, Raybould HE. (2006) Targeted disruption of the murine CCK1 receptor gene reduces intestinal lipid-induced feedback inhibition of gastric function. Am J Physiol Gastrointest Liver Physiol, 291: G156-G162. [PMID:16574983]

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Quan Chen, Fan Gao, Laurence J. Miller.
Cholecystokinin receptors: CCK1 receptor. Last modified on 26/06/2018. Accessed on 13/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=76.