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Gene Review

Cckar  -  cholecystokinin A receptor

Rattus norvegicus

Synonyms: CCK-A receptor, CCK-AR, CCK1-R, Cholecystokinin receptor type A, Cholecystokinin-1 receptor
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Disease relevance of Cckar


Psychiatry related information on Cckar


High impact information on Cckar


Chemical compound and disease context of Cckar


Biological context of Cckar


Anatomical context of Cckar


Associations of Cckar with chemical compounds

  • The cDNA sequence encodes a 452-amino acid protein that is 48% identical to the CCKA receptor and contains seven transmembrane domains characteristics of guanine nucleotide-binding regulatory protein-coupled receptors [23].
  • None of the three known phases of the febrile response of rats to LPS requires the CCK-A receptor [24].
  • Overexpression of messenger RNA for cholecystokinin-A receptor and novel expression of messenger RNA for gastrin (cholecystokinin-B) receptor in azaserine-induced rat pancreatic carcinoma [19].
  • Thus, devazepide, a selective CCK-A receptor antagonist, produced a dose-related inhibition of the CCK-8-stimulated rise in circulating beta-endorphin concentrations [25].
  • CCK-8-evoked cationic current was antagonized by lorglumide, a selective CCK-A receptor antagonist [26].

Physical interactions of Cckar

  • Thus, Lys120 outside the TM2 and Arg352 outside the TM6 of the CCK-AR are amino acids interacting with Tyr[SO(3)H]27 and Asp32 of the CCK peptide for binding [21].
  • In conclusion, our results demonstrate CCKA receptor activation causes rapid tyrosine phosphorylation of p130(Cas) through PLC-dependent and -independent mechanisms that require the participation of the small GTP-binding protein Rho and the integrity of the actin cytoskeleton, but not the microtubule network [27].
  • The high-affinity CCK-AR appears to be coupled to the Gbeta/cPLA2/arachidonic acid (AA) cascade in mediating Ca2+ oscillations [28].
  • The low-affinity CCK-AR is coupled to both the Galphaq/11/PLCbeta1/inositol 1,4,5-trisphosphate (IP3) to evoke intracellular Ca2+ release and the Src/PTK pathway to mediate extracellular Ca2+ influx [28].

Regulatory relationships of Cckar

  • We examined whether the CCK-A and CCK-B receptor genes are expressed in the islets and the role of CCK-A receptor in insulin secretion [29].
  • The CCKB selective agonist, pentagastrin, was inactive when applied at concentrations up to 10 microM. the CCKA receptor antagonist L-364,718 (1 to 100 nM) blocked the response to cholecystokinin [30].
  • These results indicate that CCK-8 stimulates pepsinogen secretion via CCK-2 receptors in CCK-1 receptor deficient OLETF rats and that the higher CCK-8-stimulated as well as basal pepsinogen secretion in OLETF rats might result from an elimination of tonic inhibition by somatostatin that is released from D cells through mainly CCK-1 receptors [31].
  • In contrast, all three stimuli are known to increase PLD activity readily in Chinese hamster ovary (CHO) cells expressing the rat pancreatic acinar cell CCKA receptor [32].
  • The specific gastrin antagonist L-365,260 inhibited the (partial) agonist activity of PD-136,450 in the stomach and the specific CCK-A receptor antagonist L-364,718 inhibited the agonist activity of PD-136,450 in the pancreas [33].

Other interactions of Cckar

  • In a previous study, we developed a new antagonist radioligand, 125I-Bolton-Hunter-labeled JMV-179, for the CCK-A receptor (CCK-AR), to analyze CCK antagonist binding sites in pancreatic plasma membranes [18].
  • To gain a better understanding of the roles of CCK-A and CCK-B receptors in spinal nociceptive transmission during inflammation, this study evaluated the effects of intrathecally administered FK480 (a CCK-A receptor antagonist) and YM022 (a CCK-B receptor antagonist) [34].
  • Increase in CYP1A1 and decrease in CCKAR expressions in vacuolated acinar cells may be involved in the pathogenesis of pancreatic lesions [22].
  • Also in the latter, in the vacuolated acinar cells, CYP1A1 was overexpressed, and statistically significant decreases in expressions of AhR, CCKAR, and amylase occurred [22].
  • Devazepide (3 mg x kg(-1)), a selective CCKA receptor antagonist, effectively attenuated the OT-induced inhibition of gastric emptying [35].

Analytical, diagnostic and therapeutic context of Cckar

  • Further to this, immunofluorecsence staining using anti-glucagon antibody was carried out after in situ hybridization using the CCK-AR cRNA probe in order to identify CCK-AR mRNA expressing cells [20].
  • Pancreatic CCK-1R protein was evaluated by immunoblot analysis and immunohistochemistry with a polyclonal antibody against rat CCK-1R protein [1].
  • Pancreatic CCK-1R mRNA was determined by Northern blot analysis [1].
  • METHODS: CCK-AR and CCK-BR mRNA expression and cellular distribution in the rat lung were detected by highly sensitive method of in situ reverse transcription-polymerase chain reaction (RT-PCR) and conventional in situ hybridization [36].
  • Pretreatment with the CCK-A receptor antagonist, lorglumide (1 microM), antagonized the effects of CCK-8s, whereas perfusion with the CCK-B preferring agonist CCK-8 nonsulfated (CCK-ns, 1 microM) did not affect the frequency of sEPSCs [37].


  1. Cholecystokinin-1 receptor protein up-regulation during pancreatic regeneration after acute haemorrhagic pancreatitis in rats. Yoshikawa, H., Nakamura, H., Tashiro, M., Yamaguchi, T., Taguchi, M., Fukumitsu, K., Otsuki, M. Eur. J. Clin. Invest. (2004) [Pubmed]
  2. Cholecystokinin receptor characterization and cholecystokinin-A receptor messenger RNA expression in transgenic mouse pancreatic carcinomas and dysplastic pancreas. Povoski, S.P., Zhou, W., Longnecker, D.S., Bell, R.H. Oncol. Res. (1994) [Pubmed]
  3. Increased spinal cholecystokinin activity after systemic resiniferatoxin: electrophysiological and in situ hybridization studies. Broberger, C., Farkas-Szallasi, T., Szallasi, A., Lundberg, J.M., Hökfelt, T., Wiesenfeld-Hallin, Z., Xu, X.J. Pain (2000) [Pubmed]
  4. Involvement of spinal cholecystokininB receptors in mediating neurotensin hyperalgesia from the medullary nucleus raphe magnus in the rat. Urban, M.O., Smith, D.J., Gebhart, G.F. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  5. L364,718 antagonizes the cholecystokinin-induced suppression of locomotor activity. Soar, J., Hewson, G., Leighton, G.E., Hill, R.G., Hughes, J. Pharmacol. Biochem. Behav. (1989) [Pubmed]
  6. Differential role of cholecystokinin receptor subtypes in opioid modulation of ongoing maternal behavior. Miranda-Paiva, C.M., Felicio, L.F. Pharmacol. Biochem. Behav. (1999) [Pubmed]
  7. Reciprocal interaction of 5-hydroxytryptamine and cholecystokinin in the control of feeding patterns in rats. Grignaschi, G., Mantelli, B., Fracasso, C., Anelli, M., Caccia, S., Samanin, R. Br. J. Pharmacol. (1993) [Pubmed]
  8. Effect of intracerebroventricular and systemic injections of caerulein, a CCK analogue, on electrical self-stimulation and its interaction with the CCKA receptor antagonist, L-364,718 (MK-329). Hamilton, M.H., Rose, I.C., Herberg, L.J., de Belleroche, J.S. Psychopharmacology (Berl.) (1990) [Pubmed]
  9. Intracerebroventricular cholecystokinin A-receptor antagonist does not reduce satiation by endogenous CCK. Brenner, L.A., Ritter, R.C. Physiol. Behav. (1998) [Pubmed]
  10. A cholecystokinin-releasing factor mediates ethanol-induced stimulation of rat pancreatic secretion. Saluja, A.K., Lu, L., Yamaguchi, Y., Hofbauer, B., Rünzi, M., Dawra, R., Bhatia, M., Steer, M.L. J. Clin. Invest. (1997) [Pubmed]
  11. Distribution of CCK1 and CCK2 receptors in normal and diseased human pancreatic tissue. Reubi, J.C., Waser, B., Gugger, M., Friess, H., Kleeff, J., Kayed, H., Büchler, M.W., Laissue, J.A. Gastroenterology (2003) [Pubmed]
  12. Expression of cholecystokinin A receptors in neurons innervating the rat stomach and intestine. Sternini, C., Wong, H., Pham, T., De Giorgio, R., Miller, L.J., Kuntz, S.M., Reeve, J.R., Walsh, J.H., Raybould, H.E. Gastroenterology (1999) [Pubmed]
  13. Characterization of the receptors and mechanisms involved in the cardiovascular actions of sCCK-8 in the pithed rat. Gaw, A.J., Hills, D.M., Spraggs, C.F. Br. J. Pharmacol. (1995) [Pubmed]
  14. Participation of central descending nociceptive facilitatory systems in secondary hyperalgesia produced by mustard oil. Urban, M.O., Jiang, M.C., Gebhart, G.F. Brain Res. (1996) [Pubmed]
  15. Cholecystokinin acts as an essential factor in the exacerbation of pancreatic bile duct ligation-induced rat pancreatitis model under non-fasting condition. Yoshinaga, K., Washizuka, M., Segawa, Y. Jpn. J. Pharmacol. (2000) [Pubmed]
  16. Endogenous CCK inhibits colonic contractions in unrestrained conscious rats. Hayashi, K., Kishimoto, S., Kannbe, M. Regul. Pept. (1997) [Pubmed]
  17. Effects of short-term administration of the CCK receptor antagonist, KSG-504, on regeneration of pancreatic acinar cells in acute pancreatitis in rats. Okumura, Y., Inoue, H., Fujiyama, Y., Bamba, T. J. Gastroenterol. (1995) [Pubmed]
  18. Photoaffinity labeling of rat pancreatic cholecystokinin type A receptor antagonist binding sites demonstrates the presence of a truncated cholecystokinin type A receptor. Poirot, S.S., Escrieut, C., Dufresne, M., Martinez, J., Bouisson, M., Vaysse, N., Fourmy, D. Mol. Pharmacol. (1994) [Pubmed]
  19. Overexpression of messenger RNA for cholecystokinin-A receptor and novel expression of messenger RNA for gastrin (cholecystokinin-B) receptor in azaserine-induced rat pancreatic carcinoma. Zhou, W., Povoski, S.P., Bell, R.H. Carcinogenesis (1993) [Pubmed]
  20. Immunohistochemical analysis of cholecystokinin A receptor distribution in the rat pancreas. Kageyama, H., Kita, T., Horie, S., Takenoya, F., Funahashi, H., Kato, S., Hirayama, M., Young Lee, E., Sakurai, J., Inoue, S., Shioda, S. Regul. Pept. (2005) [Pubmed]
  21. Structure-activity function for binding and signaling in CHO-K1 and COS-7 cells expressing the cholecystokinin A receptor. Tsunoda, Y., Song, I., Taylor, L.P., Owyang, C. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
  22. Mechanisms of exocrine pancreatic toxicity induced by oral treatment with 2,3,7,8-tetrachlorodibenzo-p-dioxin in female Harlan Sprague-Dawley Rats. Yoshizawa, K., Marsh, T., Foley, J.F., Cai, B., Peddada, S., Walker, N.J., Nyska, A. Toxicol. Sci. (2005) [Pubmed]
  23. Brain and gastrointestinal cholecystokinin receptor family: structure and functional expression. Wank, S.A., Pisegna, J.R., de Weerth, A. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  24. Role for the cholecystokinin-A receptor in fever: a study of a mutant rat strain and a pharmacological analysis. Ivanov, A.I., Kulchitsky, V.A., Romanovsky, A.A. J. Physiol. (Lond.) (2003) [Pubmed]
  25. Cholecystokinin type A and type B receptor antagonists produce opposing effects on cholecystokinin-stimulated beta-endorphin secretion from the rat pituitary. Millington, W.R., Mueller, G.P., Lavigne, G.J. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  26. CCK-8 excites substantia nigra dopaminergic neurons by increasing a cationic conductance. Wu, T., Wang, H.L. Neurosci. Lett. (1994) [Pubmed]
  27. CCKA receptor activation stimulates p130(Cas) tyrosine phosphorylation, translocation, and association with Crk in rat pancreatic acinar cells. Ferris, H.A., Tapia, J.A., García, L.J., Jensen, R.T. Biochemistry (1999) [Pubmed]
  28. High-affinity cholecystokinin type A receptor/cytosolic phospholipase A2 pathways mediate Ca2+ oscillations via a positive feedback regulation by calmodulin kinase in pancreatic acini. Lankisch, T.O., Nozu, F., Owyang, C., Tsunoda, Y. Eur. J. Cell Biol. (1999) [Pubmed]
  29. Pancreatic endocrine dysfunction in rats not expressing the cholecystokinin-A receptor. Funakoshi, A., Miyasaka, K., Kanai, S., Masuda, M., Yasunami, Y., Nagai, T., Ikeda, S., Jimi, A., Kawanami, T., Kono, A. Pancreas (1996) [Pubmed]
  30. Pharmacology of a cholecystokinin receptor on 5-hydroxytryptamine neurones in the dorsal raphe of the rat brain. Boden, P.R., Woodruff, G.N., Pinnock, R.D. Br. J. Pharmacol. (1991) [Pubmed]
  31. Pepsinogen secretion in cholecystokinin-1 receptor-deficient rats. Kanagawa, K., Nakamura, H., Otsuki, M. Dig. Dis. Sci. (2004) [Pubmed]
  32. Rat pancreatic acinar cells express a cytosolic phospholipase D1b isoform that is not regulated by cholecystokinin. Bosch, R.R., Harris, A.B., van Emst-de Vries, S.E., De Pont, J.J., Willems, P.H. Pflugers Arch. (2001) [Pubmed]
  33. Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Schmassmann, A., Garner, A., Flogerzi, B., Hasan, M.Y., Sanner, M., Varga, L., Halter, F. Gut (1994) [Pubmed]
  34. The effects of intrathecally administered FK480, a cholecystokinin-A receptor antagonist, and YM022, a cholecystokinin-B receptor antagonist, on the formalin test in the rat. Yamamoto, T., Nozaki-Taguchi, N. Anesth. Analg. (1996) [Pubmed]
  35. Involvement of cholecystokinin receptor in the inhibition of gastric emptying by oxytocin in male rats. Wu, C.L., Hung, C.R., Chang, F.Y., Pau, K.Y., Wang, J.L., Wang, P.S. Pflugers Arch. (2002) [Pubmed]
  36. Expression and cell-specific localization of cholecystokinin receptors in rat lung. Cong, B., Li, S.J., Ling, Y.L., Yao, Y.X., Gu, Z.Y., Wang, J.X., You, H.Y. World J. Gastroenterol. (2003) [Pubmed]
  37. Cholecystokinin octapeptide increases spontaneous glutamatergic synaptic transmission to neurons of the nucleus tractus solitarius centralis. Baptista, V., Zheng, Z.L., Coleman, F.H., Rogers, R.C., Travagli, R.A. J. Neurophysiol. (2005) [Pubmed]
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