Page last updated: 2024-10-24

cholecystokinin receptor activity

Definition

Target type: molecularfunction

Combining with cholecystokinin and transmitting the signal across the membrane by activating an associated G-protein to initiate a change in cell activity. Cholecystokinin can act as a neuropeptide or as a gastrointestinal hormone. [GOC:signaling, PMID:9835394]

Cholecystokinin receptor activity refers to the biological process by which a cell responds to the presence of cholecystokinin (CCK). CCK is a hormone and neurotransmitter that plays a crucial role in digestion, appetite regulation, and pancreatic function. CCK receptors, specifically CCK receptor type A (CCKAR-A) and CCK receptor type B (CCKAR-B), are G protein-coupled receptors (GPCRs) located on the cell surface. Upon binding of CCK to its receptor, a series of events are triggered, leading to downstream signaling pathways.

When CCK binds to CCKAR-A, it activates a signaling cascade that ultimately results in the release of digestive enzymes from the pancreas and the contraction of the gallbladder, facilitating the release of bile. CCKAR-A activation also plays a role in satiety and appetite regulation by signaling to the brain, reducing food intake.

CCKAR-B, on the other hand, is mainly found in the brain and peripheral tissues. Its activation is involved in the regulation of anxiety, pain perception, and neuronal development.

The molecular function of cholecystokinin receptor activity, therefore, involves the complex interaction of CCK with its receptors, activating signaling pathways that mediate a wide range of physiological processes, including digestion, appetite regulation, and neuronal function.'
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Proteins (2)

ProteinDefinitionTaxonomy
Gastrin/cholecystokinin type B receptorA cholecystokinin receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32239]Homo sapiens (human)
Cholecystokinin receptor type AA cholecystokinin receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32238]Homo sapiens (human)

Compounds (33)

CompoundDefinitionClassesRoles
5-methoxytryptamine5-methoxytryptamine : A member of the class of tryptamines that is the methyl ether derivative of serotonin.

5-Methoxytryptamine: Serotonin derivative proposed as potentiator for hypnotics and sedatives.
aromatic ether;
primary amino compound;
tryptamines
5-hydroxytryptamine 2A receptor agonist;
5-hydroxytryptamine 2B receptor agonist;
5-hydroxytryptamine 2C receptor agonist;
antioxidant;
cardioprotective agent;
human metabolite;
mouse metabolite;
neuroprotective agent;
radiation protective agent;
serotonergic agonist
propranololpropranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.

Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
naphthalenes;
propanolamine;
secondary amine
anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
indopanalpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position.

indopan: RN given refers to parent cpd without isomeric designation
tryptamines
paclitaxelTaxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).taxane diterpenoid;
tetracyclic diterpenoid
antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
5-methoxy-alpha-methyltryptamine5-methoxy-alpha-methyltryptamine: RN given refers to parent cpd without isomeric designationtryptamines
loxiglumideloxiglumide: cholecystokinin receptor antagonist; RN refers to (+-)-isomer; structure in first sourceorganic molecular entity
spiroglumidespiroglumide: a CCK receptor antagonist; antigastrin; structure given in first source
Pyrrolidine-1-carbonitrilepyrrolidines
enkephalin, d-penicillamine (2,5)-DPDPE : A heterodetic cyclic peptide that is a cyclic enkephalin analogue, having D-penicillaminyl residues located at positions 2 and 5, which form the heterocycle via a disulfide bond.

Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.
heterodetic cyclic peptidedelta-opioid receptor agonist
ci 988PD 134308: selective cholecystokinin type B receptor antagonist; inhibits growth of LoVo, a human colon cancer cell line; structure given in first source
a 71623A 71623: structure given in first source; a cholecystokinin-A receptor agonist
sr 27897SR 27897: structure given in first source; a CCK(A) receptor antagonistindolyl carboxylic acid
l 740093L 740093: a CCK-B receptor antagonist; structure in first source
cholecystokinin 9cholecystokinin 9: nonapeptide
devazepidedevazepide : An indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.

Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
1,4-benzodiazepinone;
indolecarboxamide
antineoplastic agent;
apoptosis inducer;
cholecystokinin antagonist;
gastrointestinal drug
tetragastrintetragastrin : A tetrapeptide composed of L-tryptophan, L-methione, L-aspartic acid and L-phenylalaninamide residues joined in sequence.

Tetragastrin: L-Tryptophyl-L-methionyl-L-aspartyl-L-phenylalaninamide. The C-terminal tetrapeptide of gastrin. It is the smallest peptide fragment of gastrin which has the same physiological and pharmacological activity as gastrin.
peptidyl amide;
tetrapeptide
anxiogenic;
human metabolite
asperlicinasperlicin: cholecystokinin antagonist; isolated from Aspergillus alliaceus; structure given in first source
cholecystokinin (26-33)cholecystokinin (26-33): cholecystokinin receptor antagonists
cholecystokinin (27-33), tert-butyloxycarbonyl-nle(28,31)-cholecystokinin (27-33), tert-butyloxycarbonyl-Nle(28,31)-: cholecystokinin agonist
2-(2-(5-bromo-1h-indol-3-yl)ethyl)-3-(1-methylethoxyphenyl)-4-(3h)-quinazolinone2-(2-(5-bromo-1H-indol-3-yl)ethyl)-3-(1-methylethoxyphenyl)-4-(3H)-quinazolinone: CCK2 receptor antagonistquinazolines
l 365260L 365260: a CCK-B antagonist; structure given in first source; potent & selective CCK-B & gastrin receptor ligand; L 365260 and L 365346 are (R)- and (S)-stereoisomers, respectivelybenzodiazepine
enkephalin, ala(2)-mephe(4)-gly(5)-peptide
sincalideSincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.oligopeptide
pentagastrinPentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.organic molecular entity
yf 476YF 476: gastrin and CCK-B receptor antagonist; structure in first source
l 365260
mart-1 antigenMART-1 Antigen: A melanosome-specific protein that plays a role in the expression, stability, trafficking, and processing of GP100 MELANOMA ANTIGEN, which is critical to the formation of Stage II MELANOSOMES. The protein is used as an antigen marker for MELANOMA cells.
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride
naluzotannaluzotan: an antidepressant and anti-anxiety agent; structure in first source
butyloxycarbonyl-tryptophyl-methionyl-aspartyl-phenylalaninamide
a 803467A 803467: an Nav1.8 sodium channel blocker; structure in first source
gastrin 17gastrin-17 : One of the primary forms of gastrin that is a 17-membered peptide consisting of Glp, Gly, Pro, Trp, Leu, Glu, Glu, Glu, Glu, Glu, Ala, Tyr, Gly, Trp, Met, Asp and Phe-NH2 residues joined in sequence.gastrinantineoplastic agent
nitd 609NITD 609: an antimalarial and coccidiostat; structure in first source