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Non-peptide CCK B receptor antagonists such as L-365,260, L-369,293, YF-476, RP-69758, LY-288,513, PD-145,942 and the CCK B receptor inverse agonist L-740,093 have since been developed, [3] and while all of the drugs developed so far have suffered from limited bioavailability or other issues which have hindered their clinical development ...
CCK is found extensively throughout the central nervous system, with high concentrations found in the limbic system. [31] CCK is synthesized as a 115 amino acid preprohormone, that is then converted into multiple isoforms. [31] The predominant form of CCK in the central nervous system is the sulfated octapeptide, CCK-8S. [31]
Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin. [1] There are two different subtypes CCK A and CCK B which are ~50% homologous: [2] Various cholecystokinin antagonists have been developed and are used in research, although the only drug of this class that has been widely marketed to date is ...
A CDK (cyclin-dependent kinase) inhibitor is any chemical that inhibits the function of CDKs. They are used to treat cancers by preventing overproliferation of cancer cells . The US FDA approved the first drug of this type, palbociclib (Ibrance), [ 1 ] a CDK4 / 6 inhibitor, in February 2015, for use in postmenopausal women with breast cancer ...
CI-988 (PD-134,308) is a drug which acts as a cholecystokinin antagonist, selective for the CCK B subtype. In animal studies it showed anxiolytic effects [1] [2] and potentiated the analgesic action of both morphine [3] and endogenous opioid peptides, [4] [5] as well as preventing the development of tolerance to opioids [6] [7] and reducing symptoms of withdrawal.
CCK then acts on the gallbladder to release bile and on the pancreas to release digestive enzymes, which help to further break down the food. This coordinated response helps to ensure efficient digestion and absorption of nutrients. Another function is to act as a competitive inhibitor of trypsin, which is a protease that can activate other ...
Sincalide is a cholecystokinetic drug administered by injection to aid in diagnosing disorders of the gallbladder and pancreas. It is the 8-amino acid C-terminal fragment of cholecystokinin, and also known as CCK-8. Common adverse effects following administration include abdominal discomfort and nausea.
886 12425 Ensembl ENSG00000163394 ENSMUSG00000029193 UniProt P32238 O08786 RefSeq (mRNA) NM_000730 NM_009827 NM_001347354 RefSeq (protein) NP_000721 NP_001334283 NP_033957 Location (UCSC) Chr 4: 26.48 – 26.49 Mb Chr 5: 53.86 – 53.87 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Protein domain Cholecystokinin A receptor, N-terminal domain molecular complex of cholecystokinin-8 ...