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Gene Review

Cckar  -  cholecystokinin A receptor

Mus musculus

Synonyms: AW106902, CCK-A receptor, CCK-AR, CCK1-R, Cholecystokinin receptor type A, ...
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Disease relevance of Cckar


Psychiatry related information on Cckar

  • Thus, this increased frequency in open-arm entries for CCK-AR(-/-) mice was interpreted to be due to an increase in locomotor activity, rather than to a reduction in anxiety [6].
  • Furthermore, PP secretion in response to CCK-8 showed a similarity with that of insulin in terms of dose- and time-response characteristics as well as sensitivity to CCKA-receptor antagonism [7].

High impact information on Cckar

  • Together, these findings indicate that cholecystokinin-induced inhibition of food intake is mediated by the cholecystokinin-A receptor [8].
  • The cholecystokinin-A receptor mediates inhibition of food intake yet is not essential for the maintenance of body weight [8].
  • We concluded that helices VI and III of the CCK1R are functionally linked through the CCK1R agonist binding site and that positioning of the C-terminal ends of peptidic agonists toward Phe(330) of helix VI is responsible for extent of phospholipase C activation through Galpha(q) coupling [9].
  • Computational simulations predicted that residue 121 affected orientation of the C-terminal end of CCK, thus suggesting that the molecular complex with a reduced inositol phosphate production observed with the mutated CCK1R resembles that resulting from binding of JMV 180 to the WT-CCK1R [9].
  • A chimeric protein consisting of the cholecystokinin receptor type A (CCKAR) and the green fluorescent protein (GFP) was used for studying receptor localization, internalization, and recycling in live cells in real time in four different cell lines [10].

Chemical compound and disease context of Cckar


Biological context of Cckar


Anatomical context of Cckar

  • Cckar is widely expressed in the gastrointestinal system (pancreas, gallbladder, intestine, colon and stomach), as well as in brain and kidney [13].
  • D2R expression in the nucleus accumbens was significantly lower in the CCK-BR(-/-) mice and was significantly higher in CCK-AR(-/-) mice than in wild-type mice [17].
  • AIMS: To determine pancreatic functions in a CCK-A receptor deficient mouse mutant generated by gene targeting in embryonic stem cells [18].
  • In addition to ICC, circular smooth muscle cells at the tip of the comma-shaped sphincter muscle, but not elsewhere, also exhibited strong, membrane-bound CCKAR immunoreactivity [19].
  • In the rat, cells that display strong CCKAR immunoreactivity and fit the morphological description of interstitial cells of Cajal (ICC) were found in the distal sphincter muscle and in the circular muscle of the proximal duodenum [19].

Associations of Cckar with chemical compounds

  • Differences in ethanol ingestion between cholecystokinin-A receptor deficient and -B receptor deficient mice [17].
  • Based on the evidence of interaction between CCK and dopamine, we had found previously that the CCK-AR gene -81A/G polymorphism was associated with alcohol dependence [17].
  • CONCLUSION: The CCK-A receptor is important for pancreatic exocrine secretion, but not essential for maintaining glucose concentration and pancreatic growth in mice [18].
  • Since asperlicin, a selective CCK-A receptor antagonist, may be regarded as a conformationally constrained 2-substituted-3-phenyl-4(3H)-quinazolinone, the progenitor of compound 3 (compound 2, 2-[2-(1H-indol-3-yl)ethyl]-3-phenyl-4(3H)- quinazolinone) might therefore represent a conformationally flexible pharmacophore of the natural product [20].
  • In contrast, the selective CCKA receptor antagonist, devazepide, was inactive [21].

Regulatory relationships of Cckar


Other interactions of Cckar

  • Pretreatment with L364,714, the CCK1 receptor specific antagonist did not block COX-2 induction by gastrin [23].
  • We demonstrate that although CCK-AR(-/-) mice show a similar dysregulation in meal size as OLETF rats, they do not have an elevation in DMH NPY mRNA expression levels [3].
  • The present results demonstrate that the response of the gastric vagal afferent activity in CCK-A receptor deficient OLETF rats was more sensitive to intravenous administration of IL-1beta than was in control LETO rats [24].
  • The effect of CGRP on food intake was not antagonized by the cholecystokinin A receptor antagonist, L364,718 [25].

Analytical, diagnostic and therapeutic context of Cckar


  1. Lack of cholecystokinin-A receptor enhanced gallstone formation: a study in CCK-A receptor gene knockout mice. Sato, N., Miyasaka, K., Suzuki, S., Kanai, S., Ohta, M., Kawanami, T., Yoshida, Y., Takiguchi, S., Noda, T., Takata, Y., Funakoshi, A. Dig. Dis. Sci. (2003) [Pubmed]
  2. Targeted disruption of the murine cholecystokinin-1 receptor promotes intestinal cholesterol absorption and susceptibility to cholesterol cholelithiasis. Wang, D.Q., Schmitz, F., Kopin, A.S., Carey, M.C. J. Clin. Invest. (2004) [Pubmed]
  3. Differential roles for cholecystokinin a receptors in energy balance in rats and mice. Bi, S., Scott, K.A., Kopin, A.S., Moran, T.H. Endocrinology (2004) [Pubmed]
  4. Association of cholecystokinin A receptor gene polymorphism with cholelithiasis and the molecular mechanisms of this polymorphism. Miyasaka, K., Takata, Y., Funakoshi, A. J. Gastroenterol. (2002) [Pubmed]
  5. Suppression of pancreatic tumor progression by systemic delivery of a pancreatic-cancer-specific promoter driven Bik mutant. Li, Z., Ding, Q., Li, Y., Miller, S.A., Abbruzzese, J.L., Hung, M.C. Cancer Lett. (2006) [Pubmed]
  6. Anxiety-related behaviors in cholecystokinin-A, B, and AB receptor gene knockout mice in the plus-maze. Miyasaka, K., Kobayashi, S., Ohta, M., Kanai, S., Yoshida, Y., Nagata, A., Matsui, T., Noda, T., Takiguchi, S., Takata, Y., Kawanami, T., Funakoshi, A. Neurosci. Lett. (2002) [Pubmed]
  7. Effects of cholecystokinin and glucagon-like peptide 1 on the secretion of pancreatic polypeptide in mice. Ahrén, B., Gingerich, R.L., Havel, P.J. Regul. Pept. (1995) [Pubmed]
  8. The cholecystokinin-A receptor mediates inhibition of food intake yet is not essential for the maintenance of body weight. Kopin, A.S., Mathes, W.F., McBride, E.W., Nguyen, M., Al-Haider, W., Schmitz, F., Bonner-Weir, S., Kanarek, R., Beinborn, M. J. Clin. Invest. (1999) [Pubmed]
  9. Molecular mechanism underlying partial and full agonism mediated by the human cholecystokinin-1 receptor. Archer-Lahlou, E., Escrieut, C., Clerc, P., Martinez, J., Moroder, L., Logsdon, C., Kopin, A., Seva, C., Dufresne, M., Pradayrol, L., Maigret, B., Fourmy, D. J. Biol. Chem. (2005) [Pubmed]
  10. Visualization of G protein-coupled receptor trafficking with the aid of the green fluorescent protein. Endocytosis and recycling of cholecystokinin receptor type A. Tarasova, N.I., Stauber, R.H., Choi, J.K., Hudson, E.A., Czerwinski, G., Miller, J.L., Pavlakis, G.N., Michejda, C.J., Wank, S.A. J. Biol. Chem. (1997) [Pubmed]
  11. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. Bignon, E., Bachy, A., Boigegrain, R., Brodin, R., Cottineau, M., Gully, D., Herbert, J.M., Keane, P., Labie, C., Molimard, J.C., Olliero, D., Oury-Donat, F., Petereau, C., Prabonnaud, V., Rockstroh, M.P., Schaeffer, P., Servant, O., Thurneyssen, O., Soubrié, P., Pascal, M., Maffrand, J.P., Le Fur, G. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  12. Therapeutic effects of loxiglumide on experimental acute pancreatitis using various models. Satake, K., Kimura, K., Saito, T. Digestion (1999) [Pubmed]
  13. Molecular structure of the mouse CCK-A receptor gene. Lacourse, K.A., Lay, J.M., Swanberg, L.J., Jenkins, C., Samuelson, L.C. Biochem. Biophys. Res. Commun. (1997) [Pubmed]
  14. Energy metabolism and turnover are increased in mice lacking the cholecystokinin-B receptor. Miyasaka, K., Ichikawa, M., Ohta, M., Kanai, S., Yoshida, Y., Masuda, M., Nagata, A., Matsui, T., Noda, T., Takiguchi, S., Takata, Y., Kawanami, T., Funakoshi, A. J. Nutr. (2002) [Pubmed]
  15. Localization of the murine cholecystokinin A and B receptor genes. Samuelson, L.C., Isakoff, M.S., Lacourse, K.A. Mamm. Genome (1995) [Pubmed]
  16. Targeted disruption of the murine CCK1 receptor gene reduces intestinal lipid-induced feedback inhibition of gastric function. Whited, K.L., Thao, D., Lloyd, K.C., Kopin, A.S., Raybould, H.E. Am. J. Physiol. Gastrointest. Liver Physiol. (2006) [Pubmed]
  17. Differences in ethanol ingestion between cholecystokinin-A receptor deficient and -B receptor deficient mice. Miyasaka, K., Hosoya, H., Takano, S., Ohta, M., Sekime, A., Kanai, S., Matsui, T., Funakoshi, A. Alcohol Alcohol. (2005) [Pubmed]
  18. Role of CCK-A receptor for pancreatic function in mice: a study in CCK-A receptor knockout mice. Takiguchi, S., Suzuki, S., Sato, Y., Kanai, S., Miyasaka, K., Jimi, A., Shinozaki, H., Takata, Y., Funakoshi, A., Kono, A., Minowa, O., Kobayashi, T., Noda, T. Pancreas (2002) [Pubmed]
  19. Immunohistochemical identification of cholecystokinin A receptors on interstitial cells of Cajal, smooth muscle, and enteric neurons in rat pylorus. Patterson, L.M., Zheng, H., Ward, S.M., Berthoud, H.R. Cell Tissue Res. (2001) [Pubmed]
  20. Synthesis and X-ray crystallographic analysis of quinazolinone cholecystokinin/gastrin receptor ligands. Yu, M.J., McCowan, J.R., Mason, N.R., Deeter, J.B., Mendelsohn, L.G. J. Med. Chem. (1992) [Pubmed]
  21. The behavioural properties of CI-988, a selective cholecystokininB receptor antagonist. Singh, L., Field, M.J., Hughes, J., Menzies, R., Oles, R.J., Vass, C.A., Woodruff, G.N. Br. J. Pharmacol. (1991) [Pubmed]
  22. Hypolocomotion induced by peripheral or central injection of CCK in the mouse is blocked by the CCKA receptor antagonist devazepide but not by the CCKB receptor antagonist L-365,260. O'Neill, M.F., Dourish, C.T., Iversen, S.D. Eur. J. Pharmacol. (1991) [Pubmed]
  23. Gastrin and EGF synergistically induce cyclooxygenase-2 expression in Swiss 3T3 fibroblasts that express the CCK2 receptor. Slice, L.W., Hodikian, R., Zhukova, E. J. Cell. Physiol. (2003) [Pubmed]
  24. Effects of systemic injection of interleukin-1beta on gastric vagal afferent activity in rats lacking type A cholecystokinin receptors. Kurosawa, M., Bucinskaite, V., Miyasaka, K., Funakoshi, A., Lundeberg, T. Neurosci. Lett. (2000) [Pubmed]
  25. Peripherally administered calcitonin gene-related peptide decreases food intake in mice. Morley, J.E., Farr, S.A., Flood, J.F. Peptides (1996) [Pubmed]
  26. Different effects of oral administration of synthetic trypsin inhibitor on the pancreas between cholecystokinin-A receptor gene knockout mice and wild type mice. Sato, N., Suzuki, S., Kanai, S., Ohta, M., Jimi, A., Noda, T., Takiguchi, S., Funakoshi, A., Miyasaka, K. Jpn. J. Pharmacol. (2002) [Pubmed]
  27. Treatment for hyperglycemia promotes pancreatic regeneration in rats without CCK-1 receptor gene expression. Yamamoto, M., Jia, D.M., Fukumitsu, K., Otsuki, M. Pancreas (2003) [Pubmed]
  28. The development of a sensitive and specific enzyme immunoassay for FK480, a novel cholecystokinin type-A receptor antagonist, in human plasma. Nozaki, K., Suzuki, S., Maeda, F., Takagaki, S., Suzuki, A., Hata, T. Journal of pharmaceutical and biomedical analysis. (1998) [Pubmed]
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