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Cholecystokinin receptors
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	CCK1
	CCK2

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CCK₁

Previous and Unofficial Names CCKA CCK-A Structural Information class A G protein-coupled receptor Species TM AA Chromosomal Location Gene Name Reference Human 7 428 4p15.1-p15.2 CCKAR 3-4 Rat 7 444 14q11 Cckar 1-2 Mouse 7 436 5 C1 Cckar 5-6

Contents: Previous and Unofficial Names Structural Information Database Links Agonists Antagonists Transduction Mechanisms Tissue Distribution Functional Assays Physiological Functions Physiological Consequences of Altering Gene Expression

Database Links
ChEMBL Target	10472 (Hs), 10466 (Mm), 12824 (Rn)
Ensembl	ENSG00000163394 (Hs), ENSMUSG00000029193 (Mm), ENSRNOG00000043124 (Rn)
Entrez Gene	886 (Hs), 12425 (Mm), 24889 (Rn)
GeneCards	CCKAR (Hs)
HomoloGene	37337 (Hs)
OMIM	118444 (Hs)
PharmGKB Gene	PA26142 (Hs)
Protein Ontology (PRO)	PRO:000001216 (Hs)
RefSeq Nucleotide	NM_000730 (Hs), NM_009827 (Mm), NM_012688 (Rn)
RefSeq Protein	NP_000721 (Hs), NP_033957 (Mm), NP_036820 (Rn)
UniGene Hs.	129 (Hs)
UniProt	P32238 (Hs), O08786 (Mm), P30551 (Rn)
Wikipedia	CCK1

Search for 3D structures on the PDB
Search using keywords: Cholecystokinin receptors CCK1	Search using accession numbers: P30551 || P32238 || O08786

Agonists
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Affinity Units Reference CCK-33 Rn Full agonist 9.3 pKd 32 ARL-15849 Rn Full agonist 10.5 pKi 31 PD136450 Rn Full agonist 5.9 pKi 37 CCK-8 (sulphated) Rn Full agonist 9.9 pIC50 33 SR146131 Hs Full agonist 9.3 pIC50 38 CCK-58 Mm Full agonist 9.2 pIC50 34 A-71623 Rn Full agonist 8.4 pIC50 30 GW-5823 Hs Full agonist 7.6 pIC50 35 CCK-8 (sulphated) Rn Full agonist 7.2 pIC50 33 Glaxo-11p Hs Full agonist 7.2 pIC50 36 pentagastrin Rn Full agonist 6.2 pIC50 33 gastrin Rn Full agonist 6.1 pIC50 33 CCK-4 Rn Full agonist 5.3 pIC50 33 rebamipide Rn Full agonist 4.4 pIC50 39
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 IQM-95333 Rn Antagonist 9.2 pKi 42 TP-680 Rn Antagonist 8.9 pKi 49 JNJ-17156516 Hs Antagonist 8.0 pKi 44 dexloxiglumide Hs Antagonist 7.5 pKi 44 YM-022 Rn Antagonist 6.8 pKi 52 L-740093 Rn Antagonist 5.8 pKi 46 CI-1015 Rn Antagonist 5.3 pKi 40 L-364718 Rn Antagonist 9.7 pIC50 33 lintitript Rn Antagonist 9.7 pIC50 28 T-0632 Rn Antagonist 9.6 pIC50 48 FK-480 Rn Antagonist 9.4 pIC50 41 IQM-97423 Rn Antagonist 9.0 pIC50 43 SC-50998 Rn Antagonist 7.8 pIC50 47 lorglumide Rn Antagonist 6.7 – 8.2 pIC50 33,53 YF-476 Rn Antagonist 6.9 pIC50 51 VL-0395 Rn Antagonist 6.7 pIC50 50 L-365260 Rn Antagonist 6.6 pIC50 33 loxiglumide Rn Antagonist 6.5 pIC50 54 L-736380 Rn Antagonist 6.4 pIC50 45 PD-135158 Rn Antagonist 5.9 pIC50 33 CI-988 Rn Antagonist 5.6 pIC50 33 proglumide Rn Antagonist 2.2 pIC50 55
View species-specific antagonist tables

Primary Transduction Mechanisms
Transducer	Effector/Response
Gq/G11 family	Phospholipase C stimulation
References:  3-4

Secondary Transduction Mechanisms
Transducer	Effector/Response
Gs family	Adenylate cyclase stimulation
References:  7

Tissue Distribution
Stomach. Species:  Human Technique:  RT-PCR, autoradiography, immunohistochemistry. References:  14-15
Exocrine pancreas. Species:  Human Technique:  RT-PCR. References:  16
Endocrine pancreas. Species:  Human Technique:  Immunohistochemistry. References:  17
Gallbladder. Species:  Human Technique:  Radioligand binding. References:  18
Bowel. Species:  Human Technique:  Autoradiography. References:  19-20
Adrenal gland. Species:  Human Technique:  RT-PCR, autoradiography. References:  21
Blood cells. Species:  Human Technique:  RT-PCR. References:  22
Kidney. Species:  Human Technique:  RT-PCR. References:  23
Vagal afferent fibres. Species:  Human Technique:  RT-PCR, in situ hybridisation, radioligand binding. References:  24-25

Functional Assays
COS cells transiently transfected with human CCK1 receptor cDNA. Species:  Human Tissue:  COS cells. Response measured:  Intracellular Ca2+ (Fura-2 AM). References:  3
COS cells transiently transfected with human CCK1 receptor cDNA. Species:  Human Tissue:  COS cells. Response measured:  IP3 production. References:  4

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:  26
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:  27
CCK acts at CCK1 receptors to stimulate gallbladder contraction. Species:  Rat Tissue:  Gallbladder. References:  28
CCK acts at CCK1 receptors to decrease feeding for the rat. Species:  Rat Tissue:  Intestine. References:  29

Physiological Consequences of Altering Gene Expression
CCK1 receptor-deficient rats showed impaired learning and memory. Species:  Rat Tissue:  Technique:  Receptor-deficient strain (OLETF). References:  13
CCK1 receptor-deficient mice showed severely impaired intestinal feedback in response to lipid. Species:  Mouse Tissue:  Technique:  Gene targeting in embryonic stem cells. References:  8
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:  9
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:  10
CCK1 receptor-deficient rats showed altered extracellular dopamine concentration in the brain. Species:  Rat Tissue:  Technique:  Receptor-deficient strain (OLETF). References:  11
CCK1 receptor-deficient rats showed increased gastric acid secretion. Species:  Rat Tissue:  Technique:  Receptor-deficient strain (OLETF). References:  12

To cite this receptor data page, please use the following:

Quan Chen, Fan Gao, Laurence J. Miller.
Cholecystokinin receptors: CCK₁. Last modified on 2010-06-30. Accessed on 2010-09-09. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=76.

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