AntagonistsProtein-coupled receptorsPeptidesCCK8Somatostatin receptorHigh affinityAgonistsSerotoninRatsOctapeptideTyrosine kinase receptorAffinityCCK2Urotensin-II recepLigandBlockadeRadionuclide therapyCharacterizationPancreaticHumansSignaling pathwaySubunitSubtypeCellsSatietyAngiotensinVitroBindMembranesEffectsMotilitySelectiveHumanMechanismsResponsesExpressionEvidenceTissueIntake
Antagonists2
- There are two different subtypes CCKA and CCKB which are ~50% homologous: 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 the anti-ulcer drug proglumide. (wikipedia.org)
- They represent a convenient target for studying cholecystokinin -B/ gastrin (CCK(2)) receptor antagonists in vivo. (curehunter.com)
Protein-coupled receptors3
- Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin. (wikipedia.org)
- G protein-coupled receptors in gastrointestinal physiology. (wikipedia.org)
- Though researchers' attention and this Viewpoint focus on a few famous ion channels that are considered the usual suspects as MS mechanosensors, we also discuss some of the more unusual suspects, such as G-protein coupled receptors. (stanford.edu)
Peptides2
- A broad spectrum of radiolabeled peptides with high affinity for receptors expressed on tumor cells is currently under preclinical and clinical investigation for scintigraphic imaging and radionuclide therapy. (nih.gov)
- Purpose: Radiolabelled cholecystokinin (CCK) and gastrin-derived peptides potentially can be used for peptide receptor radionuclide therapy (PRRT). (utmb.edu)
CCK84
- The present paper evaluates two (99m)Tc-labeled forms of the C-terminal octapeptide of cholecystokinin (CCK8): sulfated (s)CCK8, with high affinity for CCK1 and CCK2 receptors, and nonsulfated (ns)CCK8, with high affinity for CCK2 receptors but low affinity for CCK1 receptors. (nih.gov)
- In conclusion, these data show that CCK8 analogues can be efficiently labeled with (99m)Tc using s-HYNIC as chelator and nicotinic acid/tricine as coligand system without compromising receptor binding. (nih.gov)
- Receptor fragment approach to the binding between CCK8 peptide and cholecystokinin receptors: a fluorescence study on type B receptor fragment CCK(B)-R (352-379). (uni-bielefeld.de)
- As this receptor is expressed on colorectal and pancreatic tumours, but not in normal tissue, these tumours are potentially new targets for PRRT with CCK8 and gastrin analogs. (utmb.edu)
Somatostatin receptor1
- Of particular clinical relevance is the independence of CCK-2/gastrin-R status on the degree of tumor differentiation in human MTCs ( 5 , 6 ), whereas, in advanced and clinically aggressive forms of the disease, somatostatin receptor expression is lacking ( 7 , 8 ). (snmjournals.org)
High affinity3
- Cholecystokinin (CCK) is a peptide hormone that has a variety of physiologically important functions in the gastrointestinal tract, in which distinct high affinity receptors have been identified. (elsevierpure.com)
- As nonsulfated gastrin derivatives were shown to be more suitable for tumor targeting by virtue of their CCK-2 receptor selectivity, high affinity, and favorable in vivo profile ( 20 ), Behr et al. (snmjournals.org)
- Met-195 of the cholecystokinin-A receptor interacts with the sulfated tyrosine of cholecystokinin and is crucial for receptor transition to high affinity state. (anaspec.com)
Agonists1
- Cholecystokinin B (CCK B ) agonists increase "anxiety" in laboratory animals and induce "panic" in humans. (jneurosci.org)
Serotonin2
- Electrolytic lesions of the LPBN display increased water intake in response to central and peripheral injection of ANG II, the blockade of serotonin and cholecystokinin receptors of the LPBN increased water and sodium intake, suggested that exist an area that control inhibition of sodium appetite. (fapesp.br)
- Positron emission tomography (PET) scanning has demonstrated increased flow in the right parahippocampal region and reduced serotonin type 1A receptor binding in the anterior and posterior cingulate and raphe of patients with panic disorder. (medscape.com)
Rats3
- Although some of these analogs originally showed promising results in rats ( 18 ), none displayed convincing accumulation in the strongly receptor-positive stomach or detected small lesions in MTC patients ( 19 ). (snmjournals.org)
- Cholecystokinin and satiety in rats and rhesus monkeys. (ssib.org)
- Previous studies evaluated the effects of GABA receptors of LPBN on water and sodium intake in satiated and depleted-sodium rats. (fapesp.br)
Octapeptide2
- The effects of the cholecystokinin (CCK)-receptor antagonist proglumide, the protease inhibitor gabexate, and the hormones secretin and cholecystokinin-octapeptide (CCK-8) were studied in a model of acute hemorrhagic pancreatitis induced by feeding mice a choline-deficient, ethionine-supplemented (CDE) diet. (duke.edu)
- C-terminal sulfated and amidated octapeptide Cholecystokinin (sulfated CCK-8) has the full biological action of the full-length 33-amino acid long Cholecystokinin (CCK). (anaspec.com)
Tyrosine kinase receptor2
- The levels of tyrosine kinase receptor (c-kit) and CCK-A receptors in CBD tissues and isolated CBD cells were quantified using the double immunofluorescence labeling technique . (bvsalud.org)
- Insulin is an anabolic hormone that promotes glucose uptake, glycogenesis, lipogenesis, and protein synthesis of skeletal muscle and fat tissue through the tyrosine kinase receptor pathway. (medscape.com)
Affinity1
- Materials and methods: The receptor binding affinity of [ 111 In]DOTA-sCCK8 and [ 111 In]DOTA-MG0 for the CCK2R and CCK2i4svR was determined using stably transfected HEK293 cell lines, expressing either CCK2R or CCK2i4svR. (utmb.edu)
CCK21
- Further evidence for a C-terminal structural motif in CCK2 receptor active peptide hormones. (uni-bielefeld.de)
Urotensin-II recep1
- Solution structure of urotensin-II receptor extracellular loop III and characterization of its interaction with urotensin-II. (uni-bielefeld.de)
Ligand1
- When the ability of CR2093 to bind to EGF receptors was assessed in a ligand binding assay, it was found that the antagonist displaced up to 23% of labeled EGF. (dundee.ac.uk)
Blockade4
- Long-lasting cholecystokinin(2) receptor blockade after a single subcutaneous injection of YF476 or YM022. (curehunter.com)
- We conclude that a single subcutaneous injection of 300 micromol kg(-1) YF476 causes blockade of CCK(2) receptors in the stomach of the rat for 8 weeks thus providing a convenient method for studies of the consequences of long-term CCK(2) receptor inhibition. (curehunter.com)
- Scholars@Duke publication: Beneficial effects of cholecystokinin-receptor blockade and inhibition of proteolytic enzyme activity in experimental acute hemorrhagic pancreatitis in mice. (duke.edu)
- Blockade of CCK receptors and early inhibition of protease activity may be beneficial in severe acute pancreatitis. (duke.edu)
Radionuclide therapy1
- The advent of radiolabeled somatostatin analogs in the targeted imaging and radionuclide therapy of tumors overexpressing somatostatin receptors has paved the way for other radiopeptides to target alternative cancer-associated peptide receptor systems ( 1 - 4 ). (snmjournals.org)
Characterization1
- Ito, M., Functional characterization of a human brain cholecystokinin-B receptor. (riken.jp)
Pancreatic3
- We describe here the purification of the digitonin-solubilized rat pancreatic receptor as an initial step in the determination of its primary structure. (elsevierpure.com)
- Constitutive expression of this receptor has been demonstrated in human colorectal cancer and in pancreatic cancer, but not in normal tissue. (utmb.edu)
- AR42J, a rat pancreatic cell line expressing receptors for both gastrin and epidermal growth factor (EGF), has been used to examine the effect of the gastrin receptor antagonist CR2093 on basal, gastrin-17 (G17), EGF and transforming growth factor (TGF)-alpha stimulated growth in vitro. (dundee.ac.uk)
Humans2
- Although accumulation in some nontarget organs was also higher with (99m)Tc-sCCK8, this may not reflect the human situation due to a different receptor expression pattern in humans as compared to mice. (nih.gov)
- Therefore, further studies are warranted to investigate the possible use of (99m)Tc-sCCK8 for scintigraphic imaging of CCK receptor-positive tumors in humans. (nih.gov)
Signaling pathway1
- Taniguchi, T., Cholecystokinin-B/gastrin receptor signaling pathway involves tyrosine phosphorylations of p125FAK and p42MAP. (riken.jp)
Subunit1
- Validated multiple differentially expressed genes (DEGs), such as glycine receptor subunit 2 and cholecystokinin, at the transcript and/or protein levels, supporting the relevance of these genes to CDKL5-regulated excitability. (cureepilepsy.org)
Subtype2
- The aim of this study was to evaluate 3 new 99m Tc-labeled minigastrin analogs modified with open chain tetraamines at the N-terminus for their suitability in the CCK-2/gastrin-R-targeted imaging of tumors (CCK-2/gastrin-R = cholecystokinin subtype 2/gastrin receptor). (snmjournals.org)
- 90%) and high-density expression of CCK-2/gastrin-R (CCK-2/gastrin-R = cholecystokinin subtype 2/gastrin receptor) in human medullary thyroid cancer (MTC), already suspected by the highly sensitive pentagastrin diagnostic test ( 5 - 7 ). (snmjournals.org)
Cells3
- Expression and functional study of cholecystokinin-A receptors on the interstitial Cajal-like cells of the guinea pig common bile duct. (bvsalud.org)
- Animal steroid hormones initiate signaling by passive diffusion into cells and binding to their nuclear receptors to regulate gene expression. (biologists.com)
- In Vitro: NPS 2143 blocks increases in cytoplasmic Ca2+ concentrations with IC50 of 43 nM elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. (atminhibitor.com)
Satiety1
- Cholecystokinin may be the mediator of satiety. (bvsalud.org)
Angiotensin1
- These studies showed that GABA receptors activation induced water and NaCl intake, responses that was reduced by previous injections of angiotensin antagonist losartan(the AT1 receptor antagonist). (fapesp.br)
Vitro1
- U-67827E and CCK had identical in vitro potencies as demonstrated by their ability to induce pyloric contractions or competitively inhibit [ 125 I]CCK-8 binding to type A and B CCK receptors. (johnshopkins.edu)
Bind1
- Certain disorders can block this step (eg, renal disease can inhibit production of the active form of vitamin D ). Antibodies to the circulating hormone or its receptor can block the ability of the hormone to bind to its receptor. (msdmanuals.com)
Membranes2
- The final preparation of the purified receptor had a specific content of 8,055 pmol/mg, which represented a 9,051-fold purification from intact membranes. (elsevierpure.com)
- Elution of radioactive peaks from each chromatographic column was coincident with [ 3 H]364,718 binding activity and resulted in a labeled polypeptide having the same electrophoretic mobility as receptor derived from freshly labeled membranes and purified from untreated membranes. (elsevierpure.com)
Effects1
- The question raised is which central CCK B receptors mediate these effects. (jneurosci.org)
Motility2
- To elucidate the expression profile and significance of cholecystokinin -A (CCK-A) receptors in ICLCs in the common bile duct (CBD), as well as the role of CCK in regulating CBD motility through CCK-A receptors on CBD ICLCs. (bvsalud.org)
- CCK-A receptors are highly expressed on CBD ICLCs, and CCK may regulate CBD motility through the CCK-A receptors on ICLCs. (bvsalud.org)
Selective2
- Finally, intra-amygdala infusion of the CCK B receptor-selective antagonist PD-135158 (10 μg) blocked the potentiation of startle produced by i.c.v. infusions of pentagastrin, suggesting that i.c.v. infusions of pentagastrin potentiate startle responses via activation of amygdala CCK B receptors. (jneurosci.org)
- Description: NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM. (atminhibitor.com)
Human2
- Intermolecular interactions between the neurotensin and the third extracellular loop of human neurotensin 1 receptor. (uni-bielefeld.de)
- The Human cholecystokinin-B/gastrin receptor was provided by the RIKEN BRC through the National BioResource Project of the MEXT, Japan (cat. (riken.jp)
Mechanisms3
- Here, we investigate the role CCK B receptor-mediated mechanisms in the amygdala in the potentiation of startle. (jneurosci.org)
- These results show that amygdala CCK B receptor-mediated mechanisms are involved in the potentiation of acoustic startle responses. (jneurosci.org)
- It can also inhibit type 1 growth factor-stimulated growth, but although this action may in part be related to the antagonist's ability to inhibit binding to the EGF receptor, other mechanisms may be involved. (dundee.ac.uk)
Responses1
- First, intra-amygdala infusions of the CCK B receptor agonist pentagastrin (0, 0.01, 0.1, 1, and 10 n m ) produced a dose-related potentiation of acoustic startle responses. (jneurosci.org)
Expression1
- Immunofluorescence showed co-expression of c-kit and CCK-A receptors in the CBD muscularis layer. (bvsalud.org)
Evidence1
- Evidence for cholecystokinin as a major factor in the development of acute pancreatitis. (duke.edu)
Tissue2
- Description: This is Double-antibody Sandwich Chemiluminescent immunoassay for detection of Dog Cholecystokinin A Receptor (CCKAR) in Tissue homogenates and other biological fluids. (orbitalbiosciences.com)
- Description: A sandwich quantitative ELISA assay kit for detection of Rat Cholecystokinin A Receptor (CCKAR) in samples from tissue homogenates or other biological fluids. (orbitalbiosciences.com)
Intake1
- The relative ability of a norleucine substituted cholecystokinin (CCK) analogue, U-67827E, to interact with CCK receptors and to inhibit food intake was examined across a variety of paradigms. (johnshopkins.edu)