More information on this family may be found on the IUPHAR-DB family and introduction pages.
Cholecystokinin receptors (nomenclature recommended by the NC-IUPHAR Subcommittee on CCK receptors, [19]) are activated by the endogenous peptides cholecystokinin-4 (CCK-4), CCK-8, CCK-33 and gastrin (gastrin-17). There is evidence for species homologues of CCK2 receptors distinguished by the relative affinities of the two stereoisomers of devazepide, R-L365260 and S-L365260, or by the differences in affinity of the agonist BC264 [7].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Berna, M. J., Tapia, J. A., Sancho, V. and Jensen, R. T. (2007) Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol, 7: 583-592. [PMID:17997137]
Cawston, EE; Miller, LJ. (2010) Therapeutic potential for novel drugs targeting the type 1 cholecystokinin receptor. Br. J. Pharmacol., 159 (5): 1009-21. [PMID:19922535]
de Tullio, P; Delarge, J; Pirotte, B. (2000) Therapeutic and chemical developments of cholecystokinin receptor ligands. Expert Opin Investig Drugs, 9 (1): 129-46. [PMID:11060666]
Dockray, GJ. (2009) Cholecystokinin and gut-brain signalling. Regul. Pept., 155 (1-3): 6-10. [PMID:19345244]
Dufresne, M; Seva, C; Fourmy, D. (2006) Cholecystokinin and gastrin receptors. Physiol. Rev., 86 (3): 805-47. [PMID:16816139]
Herranz, R. (2003) Cholecystokinin antagonists: pharmacological and therapeutic potential. Med Res Rev, 23 (5): 559-605. [PMID:12789687]
Inui, A. (2003) Neuropeptide gene polymorphisms and human behavioural disorders. Nat Rev Drug Discov, 2 (12): 986-98. [PMID:14654797]
Kopin, AS; McBride, EW; Schaffer, K; Beinborn, M. (2000) CCK receptor polymorphisms: an illustration of emerging themes in pharmacogenomics. Trends Pharmacol. Sci., 21 (9): 346-53. [PMID:10973088]
Lovick, TA. (2009) CCK as a modulator of cardiovascular function. J. Chem. Neuroanat., 38 (3): 176-84. [PMID:19563885]
Miller, LJ; Gao, F. (2008) Structural basis of cholecystokinin receptor binding and regulation. Pharmacol. Ther., 119 (1): 83-95. [PMID:18558433]
Moran, TH. (2000) Cholecystokinin and satiety: current perspectives. Nutrition, 16 (10): 858-65. [PMID:11054590]
Noble, F., Wank, S. A., Crawley, J. N., Bradwejn, J., Seroogy, K. B., Hamon, M. and Roques, B. P. (1999) International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors. Pharmacol Rev, 51: 745-781. [PMID:10581329]
Noble, F; Roques, BP. (1999) CCK-B receptor: chemistry, molecular biology, biochemistry and pharmacology. Prog. Neurobiol., 58 (4): 349-79. [PMID:10368033]
Peter, SA; D'Amato, M; Beglinger, C. (2006) CCK1 antagonists: are they ready for clinical use?. Dig Dis, 24 (1-2): 70-82. [PMID:16699265]
Raybould, HE. (2007) Mechanisms of CCK signaling from gut to brain. Curr Opin Pharmacol, 7 (6): 570-4. [PMID:17954038]
Rozengurt, E; Walsh, JH. (2001) Gastrin, CCK, signaling, and cancer. Annu. Rev. Physiol., 63: 49-76. [PMID:11181948]
1. Asin, K. E., Bednarz, L., Nikkel, A. L., Gore, P. A., Montana, W. E., Cullen, M. J., Shiosaki, K., Craig, R. and Nadzan, A. M. (1992) Behavioral effects of A71623, a highly selective CCK-A agonist tetrapeptide. Am J Physiol, 263: R125-R135. [PMID:1636779]
2. Ballaz, S., Barber, A., Fortuño, A., Del Río, J., Martin-Martínez, M., Gómez-Monterrey, I., Herranz, R., González-Muñiz, R. and García-López, M. T. (1997) Pharmacological evaluation of IQM-95,333, a highly selective CCKA receptor antagonist with anxiolytic-like activity in animal models. Br J Pharmacol, 121: 759-767. [PMID:9208145]
3. Bellier, B., Dugave, C., Etivant, F., Genet, R., Gigoux, V. and Garbay, C. (2004) Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties. Bioorg Med Chem Lett, 14: 369-372. [PMID:14698161]
4. Bertrand, P., Böhme, G. A., Durieux, C., Guyon, C., Capet, M., Jeantaud, B., Boudeau, P., Ducos, B., Pendley, C. E. and Martin, G. E. (1994) Pharmacological properties of ureido-acetamides, new potent and selective non-peptide CCKB/gastrin receptor antagonists. Eur J Pharmacol, 262: 233-245. [PMID:7813588]
5. Bold, RJ; Ishizuka, J; Townsend, CM; Thompson, JC. (1994) Gastrin stimulates growth of human colon cancer cells via a receptor other than CCK-A or CCK-B. Biochem. Biophys. Res. Commun., 202 (3): 1222-6. [PMID:8060296]
6. Chang, RS; Lotti, VJ; Chen, TB; Kunkel, KA. (1986) Characterization of the binding of [3H]-(+/-)-L-364,718: a new potent, nonpeptide cholecystokinin antagonist radioligand selective for peripheral receptors. Mol. Pharmacol., 30 (3): 212-7. [PMID:3018478]
7. Durieux, C., Ruiz-Gayo, M., Corringer, P. J., Bergeron, F., Ducos, B. and Roques, B. P. (1992) [3H]pBC 264, a suitable probe for studying cholecystokinin-B receptors: binding characteristics in rodent brains and comparison with [3H]SNF 8702. Mol Pharmacol, 41: 1089-1095. [PMID:1614411]
8. Gouldson, P; Legoux, P; Carillon, C; Delpech, B; Le Fur, G; Ferrara, P; Shire, D. (2000) The agonist SR 146131 and the antagonist SR 27897 occupy different sites on the human CCK(1) receptor. Eur. J. Pharmacol., 400 (2-3): 185-94. [PMID:10988332]
9. Henke, B. R., Aquino, C. J., Birkemo, L. S., Croom, D. K., Dougherty, R. W., Ervin, G. N., Grizzle, M. K., Hirst, G. C., James, M. K., Johnson, M. F., Queen, K. L., Sherrill, R. G., Sugg, E. E., Suh, E. M., Szewczyk, J. W., Unwalla, R. J., Yingling, J. and Willson, T. M. (1997) Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists. J Med Chem, 40: 2706-2725. [PMID:9276016]
10. Hughes, J., Boden, P., Costall, B., Domeney, A., Kelly, E., Horwell, D. C., Hunter, J. C., Pinnock, R. D. and Woodruff, G. N. (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A, 87: 6728-6732. [PMID:1975695]
11. Hunter, JC; Suman-Chauhan, N; Meecham, KG; Dissanayake, VU; Hill, DR; Pritchard, MC; Kneen, CO; Horwell, DC; Hughes, J; Woodruff, GN. (1993) [3H]PD 140376: a novel and highly selective antagonist radioligand for the cholecystokininB/gastrin receptor in guinea pig cerebral cortex and gastric mucosa. Mol. Pharmacol., 43 (4): 595-602. [PMID:8474432]
12. Ito, M., Matsui, T., Taniguchi, T., Tsukamoto, T., Murayama, T., Arima, N., Nakata, H., Chiba, T. and Chihara, K. (1993) Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin. J Biol Chem, 268: 18300-18305. [PMID:8349705]
13. Iwamoto, Y., Yamamoto, R. and Kuzuya, T. (1987) CR-1409: a potent inhibitor of cholecystokinin-stimulated amylase release and cholecystokinin binding in rat pancreatic acini. Pancreas, 2: 85-90. [PMID:2437574]
14. Jagerschmidt, A; Guillaume-Rousselet, N; Vikland, ML; Goudreau, N; Maigret, B; Roques, BP. (1996) His381 of the rat CCKB receptor is essential for CCKB versus CCKA receptor antagonist selectivity. Eur. J. Pharmacol., 296 (1): 97-106. [PMID:8720482]
15. Kennedy, K; Escrieut, C; Dufresne, M; Clerc, P; Vaysse, N; Fourmy, D. (1995) Identification of a region of the N-terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK. Biochem. Biophys. Res. Commun., 213 (3): 845-52. [PMID:7654246]
16. Lee, Y. M., Beinborn, M., McBride, E. W., Lu, M., Kolakowski, L. F. and Kopin, A. S. (1993) The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem, 268: 8164-8169. [PMID:7681836]
17. Lindström, E; Björkqvist, M; Håkanson, R. (1999) Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br. J. Pharmacol., 127 (2): 530-6. [PMID:10385255]
18. Nilsson, I., Monstein, H. J., Lindström, E., Håkanson, R. and Svensson, S. (2002) Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor. Regul Pept, 103: 29-37. [PMID:11738246]
19. Noble, F., Wank, S. A., Crawley, J. N., Bradwejn, J., Seroogy, K. B., Hamon, M. and Roques, B. P. (1999) International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors. Pharmacol Rev, 51: 745-781. [PMID:10581329]
20. Rasmussen, SG; Choi, HJ; Fung, JJ; Pardon, E; Casarosa, P; Chae, PS; Devree, BT; Rosenbaum, DM; Thian, FS; Kobilka, TS; et al.. (2011) Structure of a nanobody-stabilized active state of the β(2) adrenoceptor. Nature, 469 (7329): 175-80. [PMID:21228869]
21. Seva, C; Dickinson, CJ; Yamada, T. (1994) Growth-promoting effects of glycine-extended progastrin. Science, 265 (5170): 410-2. [PMID:8023165]
22. Singh, L., Field, M. J., Hill, D. R., Horwell, D. C., McKnight, A. T., Roberts, E., Tang, K. W. and Woodruff, G. N. (1995) Peptoid CCK receptor antagonists: pharmacological evaluation of CCKA, CCKB and mixed CCKA/B receptor antagonists. Eur J Pharmacol, 286: 185-191. [PMID:8605955]
23. Singh, P; Owlia, A; Espeijo, R; Dai, B. (1995) Novel gastrin receptors mediate mitogenic effects of gastrin and processing intermediates of gastrin on Swiss 3T3 fibroblasts. Absence of detectable cholecystokinin (CCK)-A and CCK-B receptors. J. Biol. Chem., 270 (15): 8429-38. [PMID:7721737]
24. Taniguchi, H., Yazaki, N., Endo, T. and Nagasaki, M. (1996) Pharmacological profile of T-0632, a novel potent and selective CCKA receptor antagonist, in vitro. Eur J Pharmacol, 304: 147-154. [PMID:8813597]
25. Ursini, A; Capelli, AM; Carr, RA; Cassarà, P; Corsi, M; Curcuruto, O; Curotto, G; Dal Cin, M; Davalli, S; Donati, D; et al.. (2000) Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists. J. Med. Chem., 43 (20): 3596-613. [PMID:11020274]
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A mitogenic gastrin receptor, which can be radiolabelled with [125I]gastrin-(1–17) (human) and which appears to couple to the Gs family of G proteins, has been described in human colon cancer cells [5] and other cell lines (e.g. pancreatic AR42J and Swiss 3T3 fibroblasts, [21,23]).