Thermodynamic analysis of ligands at cholecystokinin CCK 2 receptors in rat cerebral cortex

British Journal of Pharmacology

Volumn 151, Issue 8, 2007, Pages 1352-1367

  Harper, E A ^a   Roberts, S P ^a   Kalindjian, S B ^a  

^a James Black Foundation   (United Kingdom)

Author keywords

3H JB93182; CCK 2 receptors; Rat cerebral cortex; Thermodynamics

Indexed keywords

4 [[2 [2 [[(2 ADAMANTYLOXY)CARBONYL]AMINO] 3 (1H INDOL 3 YL) 2 METHYLPROPIONAMIDO] 1 PHENYLETHYL]AMINO] 4 OXOBUTYRIC ACID MEGLUMINE; BACITRACIN; BUFFER; CHLORIDE; CHOLECYSTOKININ B RECEPTOR; LIGAND; PENTAGASTRIN; RADIOLIGAND; TRITIUM;

ANIMAL TISSUE; ARTICLE; BIOASSAY; BRAIN CORTEX; BRAIN MEMBRANE; CHEMICAL STRUCTURE; CONTROLLED STUDY; INCUBATION TEMPERATURE; MALE; NONHUMAN; PH; PRIORITY JOURNAL; RAT; STOMACH; THERMODYNAMICS;

ANIMALS; BINDING, COMPETITIVE; BIOLOGICAL ASSAY; CEREBRAL CORTEX; INDOLES; LIGANDS; MALE; MICE; RADIOLIGAND ASSAY; RADIOPHARMACEUTICALS; RATS; RATS, WISTAR; RECEPTOR, CHOLECYSTOKININ B; TEMPERATURE; THERMODYNAMICS;

EID: 34547910596     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707355     Document Type: Article

References (81)

1. Beinborn M, Lee Y-M, McBride EW, Quinn SM, Kopin AS (1993). A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists. Nature 362: 348-350.
2. Black JW, Leff P (1983). Operational models of pharmacological agonism. Proc R Soc Lond B 220: 141-162.
3. 2-receptor antagonists in the isolated mouse stomach. Br J Pharmacol 86: 581-587.
4. Black JW, Shankley NP (1985a). The isolated stomach preparation of the mouse: a physiological unit for pharmacological analysis. Br J Pharmacol 86: 589-599.
5. Blaker M, Ren Y, Seshadri L, McBride EW, Beinborn M, Kopin AS (2000). CCK-B/gastrin receptor transmembrane domain mutations selectively alter synthetic agonist efficacy without affecting the activity of endogenous peptides. Mol Pharmacol 58: 399-406.
6. 3 receptor binding discriminates agonistic from antagonistic behaviour. Eur J Pharmacol 298: 329-334.
7. 2A adenosine receptors. Life Sci 59: 1373-1388.
8. Borea PA, Varani K, Gessi S, Gilli P, Gilli G (1998). Binding thermodynamics at the human neuronal nicotine receptor. Biochem Pharmacol 55: 1189-1197.
9. Bruylants G, Wouters J, Michaux C (2005). Differential scanning calorimetry in life science: thermodynamics, stability, molecular recognition and application in drug design. Curr Med Chem 12: 2011-2020.
10. 50 of an enzymic reaction. Biochem Pharmacol 22: 3099-3108.
11. Cheng Z-J, Harikumar KG, Holicky EL, Miller LJ (2003). Heterodimerisation of type A and B cholecystokinin receptors enhance signalling and promote cell growth. J Biol Chem 278: 52972-52979.
12. Contreras ML, Wolfe BB, Molinoff PB (1986). Thermodynamic properties of agonist interactions with the beta adrenergic receptor-coupled adenylate cyclase system. I. High- and low-affinity states of agonist binding to membrane-bound beta adrenergic receptors. J Biol Chem 237: 154-164.
13. 1A receptor ligands. Eur J Pharmacol 312: 107-114.
14. B receptor. Eur J Pharmacol 268: 29-41.
15. Detjen K, Yule D, Tseng MJ, Williams JA, Logsdon CD (1997). CCK-B receptors produce similar signals but have opposite growth effects in CHO and Swiss 3T3 cells. Am J Physiol 273: C1449-C1457.
16. Duarte EP, Oliveira CR, Carvalho AP (1988). Thermodynamic analysis of antagonist and agonist interactions with dopamine receptors. Eur J Pharmacol 147: 227-239.
17. Dunlop J, Brammer N, Evans N, Ennis C (1997). YM022 [R-1-[2,3- dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl] -3-(3-methylphenyl) urea]: an irreversible cholecystokinin type-B receptor antagonist. Biochem Pharmacol 54: 81-85.
18. Dunlop J, Pass I, Ennis C (1998). The cholecystokinin-B receptor antagonist L-740,093 produces an insurmountable antagonism of CCK-4 stimulated functional response in cells expressing the human CCK-B receptor. Neuropeptides 32: 157-160.
19. Fernando H, Nagle GT, Rajarathnam K (2006). Thermodynamic characterization of interleukin-8 monomer binding to CXCR1 receptor N-terminal domain. FEBS J 274: 241-251.
20. Fraeyman N, Baza A, Vanscheeuwijck P (1994). Thermodynamic analysis of isoproteronol binding to β-adrenoceptors in rat lung membranes. Eur J Pharmacol 267: 63-69.
21. Goldstein A, Barrett RW (1987). Ligand dissociation constants from competition binding assays: errors associated with ligand depletion. Mol Pharmacol 31: 603-609.
22. Grauschopf U, Lilie H, Honold K, Wozny M, Reusch D, Esswein A et al. (2000). The N-terminal fragment of human parathyroid hormone receptor 1 constitutes a hormone binding domain and reveals a distinct disulphide pattern. Biochem 39: 8878-8887.
23. 2L. FASEB J 14: A243.
24. B/gastrin receptor antagonists in radioligand binding assays performed in mouse and rat cerebral cortex. Br J Pharmacol 126: 1375-1382.
25. Harper EA, Shankley NP, Black JW (1996a). Analysis of variation in L-365,260 competition curves in radioligand binding assays. Br J Pharmacol 118: 1717-1726.
26. b/gastrin receptor radioligand binding assay. 10th Camerino Noordwijkerhout Symposium. Perspectives in receptor research: Camerino, 198pp.
27. B/gastrin receptors in membranes from rat cerebral cortex. Br J Pharmacol 126: 1504-1512.
28. Hellmich MR, Rui XL, Hellmich HL, Fleming RY, Evers BM, Townsend CM (2000). Human colorectal cancers express a constitutively active cholecystokinin-B/gastrin receptor that stimulates cell growth. J Biol Chem 275: 32122-32128.
29. Hitzeman R (1988). Thermodynamic aspects of drug-receptor interactions. Trends Pharmacol Sci 9: 408.
30. Ito M, Iwata N, Taniguchi T, Murayama T, Chihara K, Matsui T (1994). Functional characterisation of two cholecystokinin-B/gastrin receptor isoforms: a preferential splice donor site in the human receptor gene. Cell Growth Differ 5: 1127-1135.
31. B/gastrin receptors. Bioorgan Med Chem Lett 6: 1171-1174.
32. Kalindjian SB, Dunstone DJ, Low CMR, Pether MJ, Roberts SP, Tozer MJ et al. (2001). Nonpeptide cholecystokinin-2 receptor agonists. J Med Chem 44: 1125-1133.
33. Kaufman R, Lindschau C, Schoneberg T, Haller H, Henklein P, Boomgaarden M et al. (1994). Type B cholecystokinin receptors on rat glioma C6 cells. Binding studies and measurement of intracellular calcium mobilisation. Br Res 639: 109-114.
34. Kenakin T (2003). Ligand-selective receptor conformations revisited: the promise and the problem. Trends Pharmacol Sci 24: 346-354.
35. Kent RS, DeLean A, Lefkowitz RJ (1980). A quantitative analysis of beta-adrenergic receptor interactions: resolution of high and low affinity states of the receptor by computer modelling of ligand binding data. Mol Pharmacol 17: 14-23.
36. 2 receptors. Mol Pharmacol 30: 226-234.
37. Kinoshita Y, Nakata H, Kishi K, Kawanami C, Sawada M, Chiba T (1998). Comparison of the signal transduction pathways activated by gastrin in enterochromaffinlike cells and parietal cells. Gastroenterology 115: 93-100.
38. Kombian SB, Anathalakshmi KV, Parvathy SS, Matowe WC (2006). Cholecystokinin-2 receptors couple to cAMP-protein kinase A to depress excitatory synaptic currents in rat nucleus accumbens in vitro. Can J Physiol Pharmacol 84: 203-211.
39. Kopin AS, Lee YM, McBride EW, Miller LJ, Lu M, Lin HY et al. (1992). Expression cloning and characterisation of the canine parietal cell gastrin receptor. Proc Natl Acad Sci USA 89: 3605-3609.
40. Kopin AS, McBride EW, Gordon MC, Quinn SM, Beinborn M (1997). Inter- and intraspecies polymorphisms in the cholecystokinin-B/gastrin receptor alter drug efficacy. Proc Natl Acad Sci USA 94: 11043-11048.
41. Kopin AS, McBride EW, Schaffer K, Beinborn M (2000). CCK receptor polymorphisms: an illustration of emerging themes in pharmacogenomics. Trends Pharmacol Sci 21: 346-353.
42. 2+ levels in a pituitary cell line. Peptides 14: 801-805.
43. Langer I, Tikhonova IG, Travers M-A, Archer-Lahlou E, Escrieut C, Maigret B, Fourmy D (2005). Evidence that interspecies polymorphism in the human and rat cholecystokinin receptor-2 affects structure of the binding site for the endogenous agonist cholecystokinin. J Biol Chem 280: 22198-22204.
44. Lay JM, Jenkins C, Friis-Hansen L, Samuelson LC (2000). Structure and developmental expression of the mouse CCK-B receptor gene. Biochem Biophys Res Commun 272: 837-842.
45. Lee YM, Beinborn M, McBride EW, Lu M, Kolakowski LF, Kopin AS (1993). The human brain cholecystokinin-B/gastrin receptor cloning and characterisation. Biol Chem 268: 8164-8168.
46. Li J-G, Raffa RB, Cheung P, Tzeng T-B, Liu-Chen L-Y (1998). Apparent thermodynamic parameters of ligand binding to the cloned rat μ-opioid receptor. Eur J Pharmacol 354: 227-237.
47. Lindström E, Björkqvist M, Boketoft A, Chen D, Zhao C-M, Kimura K et al. (1997). Neurohormonal regulation of histamine and pancreastatin secretion from isolated rat stomach ECL cells. Regulat Peptides 71: 73-86.
48. 2 receptor antagonists using rat stomach ECL cells. Br J Pharmacol 127: 530-536.
49. Lorenzen A, Guerra L, Campi F, Lang H, Schwabe U, Borea PA (2000). Thermodynamically distinct high and low affinity states of the A1 adenosine receptor induced by G protein coupling and guanine nucleotide ligation states of G proteins. Br J Pharmacol 130: 595-604.
50. 2 receptors coupled to adenylate cyclase/protein kinase A signalling cascade. J Clin Endocrinol Metab 89: 1277-1284.
51. 2 receptor antagonists. Exp Opin Ther Patents 11: 445-462.
52. Meester BJ, Shankley NP, Welsh NJ, Wood J, Meijler FL, Black JW (1998). Phamacological classification of adenosine receptors in the sinoatrial and atrioventricular nodes of the guinea-pig. Br J Pharmacol 124: 685-692.
53. 3 adenosine receptors. Biochem Pharmacol 63: 157-161.
54. Miyake A (1995). A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon. Biochem Biophys Res Commun 208: 230-237.
55. Monstein H-J, Nilsson I, Ellnebo-Svedlund K, Svensson SPS (1998). Clonign and characterisation of 5′-end alternatively spliced human cholecystokinin-B receptor mRNAs. Receptors Channels 6: 165-177.
56. 2 receptors. Br J Pharmacol 140: 218-224.
57. Motulsky HJ, Mahan LC (1983). The kinetics of competitive radioligand binding predicted by the law of mass action. Mol Pharmacol 25: 1-9.
58. Muller W, Heinemann U, Berlin K (1997). Cholecystokinin activates CCK-B receptor-mediated signalling in hippocampal astrocytes. J Neurophysiol 78: 1997-2001.
59. Nakata H, Matsui T, Ito M, Taniguchi T, Naribayashi Y, Arima N et al. (1992). Cloning and characterisation of gastrin receptor from ECL carcinoid tumor of mastomys natalensis. Bioche Biophys Res Commun 187: 1151-1157.
60. Noble F, Wank SA, Crawley JN, Bradwejn J, Seroogy KB, Hamon M et al. (1999). International Union of Pharmacology XXI. Structure, distribution, and functions of cholecystokinin receptors. Pharmacol Rev 51: 745-781.
61. Pisegna JR, De Weerth A, Huppi K, Wank SA (1992). Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localisation. Biochem Biophys Res Commun 189: 296-303.
62. Perozzo R, Folkers G, Scapozza L (2004). Thermodynamics of protein-ligand interactions: history, presence, and future aspects. J Recept Signal Transduct Res 24: 1-52.
63. Pommier B, Da Nascimento S, Dumont S, Bellier B, Million E, Garbay C et al. (1999). The cholecystokininB receptor is coupled to two effector pathways through pertussis toxin-sensitive and -insensitive G proteins. J Neurochem 73: 281-288.
64. Prinz C, Kajimura M, Scott DR, Mercier F, Helander H, Sachs G (1993). Histamine secretion from rat enterochromaffin-like cells. Gastroenterology 105: 449-461.
65. Prinz C, Scott DR, Hurwitz D, Helander HF, Sachs G (1994). Gastrin effects on isolated enterochromaffin-like cells in primary culture. Am J Physiol 267: G663-675.
66. Raffa RB, Porreca F (1989). Thermodynamic analysis of drug-receptor interactions. Life Sci 44: 245.
67. Rajagopalan L, Rosgen J, Bolen DW, Rajarathnam K (2005). Novel use of an osmolyte to dissect multiple thermodynamic linkages in a chemokine ligand-receptor system. Biochem 44: 12932-12939.
68. B/gastrin receptors in rat, guinea-pig and mouse isolated gastric tissue assays. Br J Pharmacol 118: 1779-1789.
69. Roberts SP, Watt GF, Sykes DA, Gerskowitch VP, Hull RAD, Shankley NP et al. (1996b). JB93182: a potent and selective CCKB/gastrin receptor antagonist in isolated stomach preparations of the immature rat, mouse and guinea-pig. FASEB J 10: A2199.
70. Sandvik AK, Waldum HL (1991). CCK-B (gastrin) receptor regulates histamine release and acid secretion. Am J Physiol 260: G925-928.
71. Schmitz F, Schrader H, Otte J, Schmitz H, Stuber E, Herzig K et al. (2001). Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells. Regul Pept 15: 25-33.
72. B) receptors to phospholipase C and protein kinase C in AR4-2J tumoral cells. Regul Peptides 52: 31-38.
73. Shankley NP, Roberts SP, Watt GF, Kotecha A, Hull RAD, Black JW (1997). Analysis of the complex pharmacology expressed by the CCK-B/ gastrin ligand PD134,308 on gastric assays. ASPET Pharmacol 39: P65.
74. Shankley NP, Welsh NJ, Black JW (1992). Histamine dependence of pentagastrin-stimulated gastric acid secretion in rats. Yale J Biol Med 65: 613-619.
75. Smith AJ, Freedman SB (1996). CCK-B receptor-mediated stimulation of polyphosphoinositide turnover in GH3 pituitary cells in response to cholecystokinin and pentagastrin. Life Sci 58: 883-895.
76. Song I, Brown DR, Wiltshire RN, Gantz I, Trent JM, Yamada T (1993). The human gastrin/cholecystokinin type B receptor gene: alternative splice donor site in exon 4 generates two variant mRNAs. Proc Natl Acad Sci USA 90: 9085-9089.
77. Wank SA, Pisegna JR, De Weerth A (1992). Brain and gastrointestinal cholecystokinin receptor family: structure and functional expression. Proc Natl Acad Sci USA 89: 8691-8695.
78. Weiland GA, Minneman KP, Molinoff PB (1979). Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor. Nature 281: 114.
79. Wells JW, Birdsall NJM, Burgen ASV, Hulme EC (1980). Competitive binding studies with multiple sites - effects arising from depletion of the free radioligand. Biochem Biophys Acta 632: 464-469.
80. Wu SV, Yang M, Avedian D, Birnbaumer M, Walsh JH (1999). Single amino acid substitution of serine82 to asparagines in first intracellular loop of human cholecystokinin (CCK)-B receptors confers full cyclic AMP responses to CCK and gastrin. Mol Pharmacol 55: 795-803.
81. 3H] spiroperidol in rat striatum. Mol Pharmacol 23: 303-309.