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Cholecystokinin GPCR Assays

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Background of Cholecystokinin (CCK)

CCK was originally found to be involved in gallbladder contraction and pancreatic secretion. Later, studies showed that CCK may be the most abundant neuropeptide in the mammalian central nervous system (CNS). Furthermore, there is evidence that reveals that CCK is also involved in the secretion and motility of the gastrointestinal tract. To date, two CCK receptors have been identified that mediate CCK: CCK1 receptors and CCK2 receptors.

Distribution and Function of CCK Receptors

CCK is released from gastroenteroendocrine cells in the upper small intestine in further response to dietary substances and binds to existing receptors to modulate various gastrointestinal target tissues. Notably, CCK1 and CCK2 receptors are closely associated with various disease pathologies, such as metabolic and gastrointestinal diseases.

Mechanism of CCK Receptors

The two receptor types differ in their relative affinities for natural ligands and their molecular structures. However, CCK receptors are involved in multiple pathways to exert their functions.

Receptor Gene Mechanism Agonists Antagonists
CCK1 Receptors CCKAR
  • The CCK1 receptor activates adenylyl cyclase, leading to increased cyclic AMP.
  • The CCK1 receptor activates the cGMP pathway.
  • A-71623
  • A-70874
  • Devazepide
  • Loxiglumide
  • SR 27897
  • CR-1505
  • T-0632
CCK2 Receptors CCKBR
  • The CCK2 receptor activates the PI3K pathway.
  • CCK2 receptor activates the MAPK cascade.
  • Gastrin I
  • BC 264
  • BC 254
  • BC 197
  • CI 988
  • L-365,260
  • LY 225910
  • LY 288513
  • YM 022

Assay List of Cholecystokinin Receptors

Creative Biolabs can provide a range of assays of cholecystokinin receptors. You can choose the assay in the list or contact us for more information:

CCKAR CCKBR
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX381 Magic™ Human CCKAR In Vitro cAMP Assay 1321N1 cAMP Assay
Calcium Flux Assay
S01YF-0722-KX96 Magic™ Human CCKAR In Vitro Calcium Assay, HEK293 HEK293 Calcium Flux Assay
S01YF-1122-KX380 Magic™ Human CCKAR In Vitro Calcium Flux Assay 1321N1 Calcium Flux Assay
IP1 Assay
S01YF-0722-KX14 Magic™ Human CCKAR In Vitro Agonist & Antagonist IP1 Assay, CHO CHO IP1 Assay
S01YF-1122-KX382 Magic™ Human CCKAR In Vitro IP1 Assay 1321N1 IP1 Assay
Radioligand Binding Assay
S01YF-1122-KX383 Magic™ Human CCKAR In Vitro Radioligand Binding Assay 1321N1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX97 Magic™ Human CCKBR In Vitro Calcium Assay, HEK293 HEK293 Calcium Flux Assay
S01YF-1122-KX384 Magic™ Human CCKBR In Vitro Calcium Flux Assay 1321N1 Calcium Flux Assay

Published Data

Paper Title Cholecystokinin (CCK) and its receptors (CCK1 and CCK2) in chickens: functional analysis and tissue expression
Journal Poultry Science
Published 2022
Abstract CCK is mainly distributed in the gastrointestinal tract and CNS and participates in a series of physiological responses through the activation of its receptors (CCK1 and CCK2). In contrast to mammals, the CCK gene and its receptors have been cloned in various birds. However, there are still large gaps in the knowledge of their functions and tissue expression. In this study, the researchers examined the expression of CCK and its two receptors in chicken tissues. In addition, the function of these two receptors was investigated. Combined with differences in the tissue distribution of CCK and its receptors, this study provides new insights into the physiological functions of CCK/CCKRs in birds.
Result Using three cell-based luciferase reporter systems and western blotting, this study demonstrated that cCCK-8S can efficiently activate cCCK1, while cCCK-8S and cCCK-4 are effective in activating cCCK2. RNA-seq data revealed that cCCK is abundantly expressed in the testis, ileum and brain, midbrain, cerebellum, hindbrain, and hypothalamus. Immunofluorescence results further confirmed that CCK is abundant in the hypothalamus. Furthermore, cCCK1 is highly expressed in the pancreas and expressed in various intestinal regions and the pituitary gland, whereas cCCK2 expression is mainly restricted to the brain. This article revealed the different specificities of the CCK receptor for various CCK peptides. Combined with the differences in tissue distribution of CCK and its receptors, this study provides a new basis for understanding the physiological function of CCK/CCKRs in birds.

RNA-seq data showing the expression of CCK (A), CCK1 (B), and CCK2 (C) in adult chicken tissues.Fig.1. RNA-seq data showing the expression of CCK (A), CCK1 (B), and CCK2 (C) in adult chicken tissues. (Wan, 2022)

Reference

  1. Wan, Y.; et al. Cholecystokinin (CCK) and its receptors (CCK₁ and CCK₂) in chickens: functional analysis and tissue expression. Poultry Science. 2022; 13: 3352.
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