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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| Protein | Definition | Taxonomy |
|---|---|---|
| Gastrin/cholecystokinin type B receptor | A cholecystokinin receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32239] | Homo sapiens (human) |
| Cholecystokinin receptor type A | A cholecystokinin receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32238] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 5-methoxytryptamine | 5-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 |
| propranolol | propranolol : 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 |
| indopan | alpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position. indopan: RN given refers to parent cpd without isomeric designation | tryptamines | |
| paclitaxel | Taxus: 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-methyltryptamine | 5-methoxy-alpha-methyltryptamine: RN given refers to parent cpd without isomeric designation | tryptamines | |
| loxiglumide | loxiglumide: cholecystokinin receptor antagonist; RN refers to (+-)-isomer; structure in first source | organic molecular entity | |
| spiroglumide | spiroglumide: a CCK receptor antagonist; antigastrin; structure given in first source | ||
| Pyrrolidine-1-carbonitrile | pyrrolidines | ||
| 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 peptide | delta-opioid receptor agonist |
| ci 988 | PD 134308: selective cholecystokinin type B receptor antagonist; inhibits growth of LoVo, a human colon cancer cell line; structure given in first source | ||
| a 71623 | A 71623: structure given in first source; a cholecystokinin-A receptor agonist | ||
| sr 27897 | SR 27897: structure given in first source; a CCK(A) receptor antagonist | indolyl carboxylic acid | |
| l 740093 | L 740093: a CCK-B receptor antagonist; structure in first source | ||
| cholecystokinin 9 | cholecystokinin 9: nonapeptide | ||
| devazepide | devazepide : 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 |
| tetragastrin | tetragastrin : 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 |
| asperlicin | asperlicin: 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)-quinazolinone | 2-(2-(5-bromo-1H-indol-3-yl)ethyl)-3-(1-methylethoxyphenyl)-4-(3H)-quinazolinone: CCK2 receptor antagonist | quinazolines | |
| l 365260 | L 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, respectively | benzodiazepine | |
| enkephalin, ala(2)-mephe(4)-gly(5)- | peptide | ||
| sincalide | Sincalide: 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 | |
| pentagastrin | Pentagastrin: 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 476 | YF 476: gastrin and CCK-B receptor antagonist; structure in first source | ||
| l 365260 | |||
| mart-1 antigen | MART-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 | |||
| naluzotan | naluzotan: an antidepressant and anti-anxiety agent; structure in first source | ||
| butyloxycarbonyl-tryptophyl-methionyl-aspartyl-phenylalaninamide | |||
| a 803467 | A 803467: an Nav1.8 sodium channel blocker; structure in first source | ||
| gastrin 17 | gastrin-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. | gastrin | antineoplastic agent |
| nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source |