Cholecystokinin GPCR Family Subtypes and Products

What Are Cholecystokinin Receptors?

Cholecystokinin receptors are a family of G protein-coupled receptors consisting of CCK₁ and CCK₂ receptors. CCK₁ receptors are found in the pancreas, gastrointestinal tract, gallbladder, and specific areas of the brain, while CCK₂ receptors are found throughout the brain and in the oxyntic mucosa in the stomach. Cholecystokinin plays a major role in maintaining nutritional homeostasis through its involvement in processes such as gastric emptying, gallbladder contraction, and pancreatic exocrine secretion. Antagonists for CCK receptors are being evaluated for their potential as therapeutic drugs for appetite control, gastrointestinal dysmotility states, anxiety, depression, and drug dependency.

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Cholecystokinin Receptor Information

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CCK1

CCK2

Cholecystokinin (CCK) is a regulatory peptide hormone with many functions in the gastrointestinal tract and brain. CCK1 (also known as CCKA) receptors are present in the gall bladder, gastric smooth muscle cells and mucosa, myenteric neurons, and brain. CCK regulates gastric acid secretion, gastric emptying and gall bladder motility in the gastrointestinal tract. Clinical studies show that CCK1 may also be involved in many types of diseases, such as pancreatic disorders, motility disorders, tumor growth and regulation of satiety.

Cholecystokinin B receptor (CCKBR/CCK2R) is a 447-amino acid 7 transmembrane protein. The cholecystokinin (CCK) family of peptides and their receptors are widely distributed throughout the central nervous system and gastrointestinal tract. CCKBR is a type B (gastrin) receptor that has high affinity for both sulfated and nonsulfated CCK analogs found principally in the CNS and select areas of the gastrointestinal tract. Type B receptors regulate anxiety, arousal, neuroleptic activity and opiate-induced analgesia. Outside of the CNS they regulate gastric acid secretion and may play a role in gastrointestinal motility and growth of normal and neoplastic gastrointestinal tissue. Northern hybridization shows CCKBR expressed in the stomach, pancreas, brain and gallbladder.

Cholecystokinin Cell Lines

Receptor Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Cholecystokinin	CCK1	human	CHO-K1	C1038-1a	DC1038-1a	MC1038-1a
	CCK1	human	HEK293T	C1038	DC1038	MC1038
	CCK2	human	HEK293T	H1039	DH1039	MH1039