• Source: Cholecystokinin A receptor

The Cholecystokinin A receptor is a human protein, also known as CCKAR or CCK1, with CCK1 now being the IUPHAR-recommended name.




Function


This gene encodes a G-protein coupled receptor that binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine.
The extracellular, N-terminal, domain of this protein adopts a tertiary structure consisting of a few helical turns and a disulfide-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding hormonal ligand.




Selective Ligands






= Agonists

=
Cholecystokinin
CCK-4
SR-146,131
A-71623 - modified tetrapeptide, potent and selective CCKA agonist, IC50 3.7nM, 1200x selectivity over CCKB, CAS# 130408-77-4




= Antagonists

=
Proglumide
Lorglumide
Devazepide
Dexloxiglumide
Asperlicin
SR-27897
IQM-95333
JNJ-17156516




See also


Cholecystokinin receptor
Cholecystokinin antagonist




References






External links


"Cholecystokinin Receptors: CCK1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2012-10-23. Retrieved 2008-12-04.




Further reading



This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Kata Kunci Pencarian:

• Reseptor kolesistokinin B
• Gastrin
• Cholecystokinin receptor
• Cholecystokinin A receptor
• Cholecystokinin
• Cholecystokinin B receptor
• Neurotransmitter
• Orexin
• Rhodopsin-like receptors
• Acetylcholine receptor
• Bombesin
• Beta-2 adrenergic receptor