Recombinant Rat Gastrin/cholecystokinin type B receptor (Cckbr)

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Description

Production Methods

Recombinant rat Cckbr is typically produced using heterologous expression systems:

  • Mammalian cells (e.g., COS-7, CHO): Enable proper post-translational modifications and ligand-binding functionality .

  • Baculovirus/insect cell systems: Used for large-scale production in structural studies .

Example Protocol

  1. Cloning of rat Cckbr cDNA into expression vectors .

  2. Transfection into host cells and selection via antibiotic resistance .

  3. Affinity purification using tags (e.g., FLAG, His-tag) .

Functional Roles

Gastrointestinal Tract

  • Regulates gastric acid secretion and intestinal sodium absorption .

  • Mechanism: Activates phospholipase C (PLC) via Gq, increasing intracellular Ca²⁺ and inositol trisphosphate (IP₃) .

Central Nervous System

  • Modulates dopamine release in the striatum and nucleus accumbens .

  • Key pathways:

    • Inhibits dopamine via GABAergic interneurons in the anterior nucleus accumbens .

    • Enhances ERK1/2 signaling through PKC-dependent Shc phosphorylation .

Ligand Interactions

Binding Affinities

LigandReceptor StateKd (nM)Source
GastrinHigh-affinity0.1–0.3
CCK-8 (sulfated)Low-affinity2–5
L-365,260 (antagonist)Inactive0.13

Notable Ligands

  • Agonists: Gastrin-17, CCK-4, BBL-454 .

  • Antagonists: YF476, PD-135,158 (used in cancer and anxiety studies) .

Research Applications

Disease Models

  • Colorectal cancer: Misspliced Cckbr variants correlate with tumor invasiveness .

  • Parkinson’s disease: CCKBR antagonism enhances L-DOPA efficacy in dopamine-depleted models .

Therapeutic Targeting

  • Small-molecule antagonists: Reduce acid secretion in peptic ulcers .

  • Inverse agonists (e.g., L-740,093): Investigated for anxiety disorders .

Challenges and Future Directions

  • Structural heterogeneity: Conformational flexibility complicates drug design .

  • Species-specific differences: Rat Cckbr’s higher gastrin affinity vs. human orthologs necessitates cautious extrapolation .

Product Specs

Form
Lyophilized powder
Note: We will prioritize shipping the format that we have in stock. However, if you have a specific requirement for the format, please indicate your preference when placing the order. We will fulfill your request if possible.
Lead Time
Delivery time may vary depending on the purchase method or location. Please contact your local distributor for specific delivery time information.
Note: All of our proteins are shipped with standard blue ice packs by default. If you require dry ice shipping, please notify us in advance as additional fees will apply.
Notes
Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
Reconstitution
We recommend centrifuging the vial briefly before opening to ensure the contents settle at the bottom. Reconstitute the protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. We suggest adding 5-50% glycerol (final concentration) and aliquoting for long-term storage at -20°C/-80°C. Our standard final glycerol concentration is 50%. This can be used as a reference.
Shelf Life
The shelf life is influenced by multiple factors, including storage conditions, buffer components, storage temperature and the inherent stability of the protein itself.
Generally, liquid forms have a shelf life of 6 months at -20°C/-80°C. Lyophilized forms have a shelf life of 12 months at -20°C/-80°C.
Storage Condition
Store at -20°C/-80°C upon receipt. Aliquoting is necessary for multiple uses. Avoid repeated freeze-thaw cycles.
Tag Info
Tag type will be determined during the manufacturing process.
The tag type will be decided during the production process. If you have a specific tag type in mind, please inform us and we will prioritize developing the specified tag.
Synonyms
Cckbr; Gastrin/cholecystokinin type B receptor; CCK-B receptor; CCK-BR; Cholecystokinin-2 receptor; CCK2-R
Buffer Before Lyophilization
Tris/PBS-based buffer, 6% Trehalose.
Datasheet
Please contact us to get it.
Expression Region
1-452
Protein Length
full length protein
Species
Rattus norvegicus (Rat)
Target Names
Target Protein Sequence
MELLKLNRSVQGPGPGSGSSLCRPGVSLLNSSSAGNLSCDPPRIRGTGTRELEMAIRITL YAVIFLMSVGGNVLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF IFGTVICKAISYLMGVSVSVSTLNLVAIALERYSAICRPLQARVWQTRSHAARVILATWL LSGLLMVPYPVYTMVQPVGPRVLQCMHRWPSARVQQTWSVLLLLLLFFIPGVVIAVAYGL ISRELYLGLHFDGENDSETQSRARNQGGLPGGAAPGPVHQNGGCRPVTSVAGEDSDGCCV QLPRSRLEMTTLTTPTPGPVPGPRPNQAKLLAKKRVVRMLLVIVLLFFLCWLPVYSVNTW RAFDGPGAQRALSGAPISFIHLLSYVSACVNPLVYCFMHRRFRQACLDTCARCCPRPPRA RPQPLPDEDPPTPSIASLSRLSYTTISTLGPG
Uniprot No.

Target Background

Function
The Gastrin/cholecystokinin type B receptor (CCKBR) serves as a receptor for gastrin and cholecystokinin. CCK-B receptors are widely distributed throughout the central nervous system where they modulate various functions including anxiety, analgesia, arousal, and neuroleptic activity. This receptor exerts its effects through association with G proteins, which activate a phosphatidylinositol-calcium second messenger system.
Gene References Into Functions
  1. CCK-B receptors mediate acetylcholine release through cell bodies of cholinergic interneurons in the corpus striatum. PMID: 22981453
  2. CCK1 and CCK2 receptors are expressed on pancreatic stellate cells and induce collagen production PMID: 20843811
  3. Pancreatic islet CCK1/2 receptors initiate somatostatin secretion through constitutive secretion controlled at the level of protein synthesis. PMID: 19959964
  4. CCK(B) receptor mediates synergistic stimulation of DNA synthesis and cyclin expression PMID: 11748587
  5. Research indicates that CCKB, but not CCKA receptors are involved in anxiety, as determined by microinjection of cholecystokinin agonists. PMID: 12373548
  6. Genetic variations in CCK2 receptor in PVG hooded and Sprague-Dawley rats and its mRNA expression on cat exposure PMID: 12708535
  7. CCK-AR and CCK-BR gene were present in pulmonary vascular endothelial cells, macrophages, bronchial epithelial cells and alveolar epithelial cells, which play an important role in mediating the regulatory actions of CCK-8 on these cells. PMID: 12800239
  8. Gastrin increased PGE2 secretion in Swiss 3T3 cells expressing the CCK2 receptor PMID: 12891702
  9. Studies have identified CCK-A and CCK-B receptor mRNAs in the rat retina and demonstrated their functional role in stimulating tyrosine phosphorylation pathways. PMID: 14698681
  10. Insulin can negatively control pancreatic somatostatin mRNA and hormone content and positively control CCK(B)R mRNA; the CCK(B)R protein appears to be delayed. PMID: 15161757
  11. Analysis of interspecies polymorphism in the human and rat cholecystokinin receptor-2 and its effect on the cholecystokinin binding site PMID: 15817487
  12. Research findings support the view that dorsolateral periaqueductal gray CCK(2) receptors modulate panic-related behaviors. PMID: 16168394
  13. Under 'basal' conditions, a portion of the glandular protein synthesis, as well as the whole increase in synthesis in response to administration of pentagastrin, engaged both types of CCK receptors. PMID: 16556659
  14. CCK(2) receptors located in the peraqueductal gray are involved in the regulation of panic-related behaviors and may mediate the effect of cholecystokinin-4 on panic. PMID: 17498673
  15. Functional postsynaptic G-protein-coupled CCK B receptors are prevalent in neonatal rodent spinal cord. PMID: 17581850
  16. CCK modulates glutamate-GABA mechanisms by acting on CCK-2 receptors via volume transmission occurring at basolateral amygdaloid nucleus and/or by synaptic or perisynaptic volume transmission in rostrolateral main and paracapsular intercalated islands. PMID: 18088282
  17. Findings indicate that CCK, acting via CCK(B) receptors, produces a long-lasting excitation of layer 6b neocortical neurons, and this action may play a crucial role in modulation of corticothalamic circuit activity. PMID: 19497313

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Database Links
Protein Families
G-protein coupled receptor 1 family
Subcellular Location
Cell membrane; Multi-pass membrane protein.
Tissue Specificity
Parietal cells, pancreas, brain and various neoplastic tissues.

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