Estimation of the dissociation rate of unlabelled ligand-receptor complexes by a 'two-step' competition binding approach

British Journal of Pharmacology

Volumn 161, Issue 6, 2010, Pages 1311-1328

  Packeu, A ^a   Wennerberg, M ^b   Balendran, A ^b   Vauquelin, G ^a  

^a VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

CB 1 cannabinoid; Computer simulations; D 2 dopamine; Dissociation; Kinetics; Membrane partitioning; Radioligand binding

Indexed keywords

CANNABINOID 1 RECEPTOR; DOPAMINE 2 RECEPTOR; RACLOPRIDE; RADIOLIGAND; RIMONABANT; SPIPERONE; TARANABANT;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CELL STRAIN HEK293; CHO CELL; COMPUTER SIMULATION; DISSOCIATION; DRUG RECEPTOR BINDING; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; BINDING, COMPETITIVE; CHO CELLS; COMPUTER SIMULATION; CRICETINAE; CRICETULUS; HEK293 CELLS; HUMANS; LIGANDS; PROTEIN BINDING; RADIOLIGAND ASSAY; RECEPTOR, CANNABINOID, CB1; RECEPTORS, DOPAMINE D2;

EID: 77956840539     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.00931.x     Document Type: Article

References (53)

1. 1 receptor antagonist. Eur J Pharmacol 283: 63-72.
2. Alexander SPH, Mathie A, Peters JA (2009). Guide to receptors and channels (GRAC). Br J Pharmacol 158 (Suppl. 1): S1-S254.
3. 2-adrenoceptor agonist bronchodilator. Life Sci 52: 2145-2160.
4. Anderson GP, Lindén A, Rabe KF (1994). Why are long-acting beta-adrenoceptor agonists long-acting? Eur Respir J 7: 569-578.
5. Anthes JC, Gilchrest H, Richard C, Ecke LS, Hesk D, West RE Jr et al. (2002). Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol 449: 229-237.
6. 2-adrenoceptor agonists. J Med Chem 46: 3210-3320.
7. Bergendal A, Lindén A, Skoogh B-E, Gerspacher M, Anderson GP, Lolfdahl C-G (1996). Salmeterol mediated reassertion of relaxation persists in guinea-pig trachea pretreated with aliphatic side chain structural analogues. Br J Pharmacol 117: 1009-1015.
8. El Bizri H, Clarke PB (1994). Blockade of nicotinic receptor-mediated release of dopamine from striatal synaptosomes by chlorisondamine administered in vivo. Br J Pharmacol 111: 414-418.
9. Blower PR (2003). Granisetron: relating pharmacology to clinical efficacy. Support Care Cancer 11: 93-100.
10. Coleman RA, Johnson M, Nials AT, Vardey CJ (1996). Exosites: their current status, and their relevance to the duration of action of long-acting beta 2-adrenoceptor agonists. Trends Pharmacol Sci 17: 324-330.
11. Copeland RA, Pompliano DL, Meek TD (2006). Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov 5: 730-739.
12. Creese I, Burt DR, Snyder SH (1976). Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science 192: 481-483.
13. 1 receptor antagonist, UR 7280. Eur J Pharmacol 318: 341-347.
14. 3 receptor. Br J Pharmacol 148: 927-937.
15. 11C]JHU75575) as potential radioligands for PET imaging ofα cerebral cannabinoid receptor. J Label Compd Radiopharm 49: 1021-1036.
16. 1 receptor-transfected Chinese hamster ovary cells. Eur J Pharmacol 367: 413-422.
17. Hara M, Kiyama R, Nakajima S, Kawabata T, Kawakami M, Ohtani K et al. (1995). Kinetic studies on the interaction of nonlabelled antagonists with the angiotensin II receptor. Eur J Pharmacol 289: 267-273.
18. Härtter S, Hüwel S, Lohmann T, Abou El Ela A, Langguth P, Hiemke C (2003). How does the benzamide antipsychotic amisulpride get into the brain? An in vitro approach comparing amisulpride with clozapine. Neuropsychopharmacology 28: 1916-1922.
19. Heise CE, Sullivan S, Crowe PD (2007). Scintillation proximity assay as high-throughput method to identify slowly dissociating nonpeptide ligand binding to the GnRH receptor. J Biomol Screen 12: 235-239.
20. 1 receptors. J Pharmacol Exp Ther 308: 105-110.
21. Johnson M (2001). Beta2-adrenoceptors: mechanisms of action of beta2-agonists. Paediatr Respir Rev 2: 57-62.
22. 2-adrenoceptor agonists. In: Busse WW, Holgate ST (eds). Asthma & Rhinitis. Blackwell: Cambridge, pp. 1278-1295.
23. Kakuta H, Sudoh K, Sasamata M, Yamagashi S (2005). Telmisartan has the strongest binding affinity to angiotensin II type 1 receptor: comparison with other angiotensin II type 1 receptor blockers. Int J Clin Pharmacol 25: 41-46.
24. 1 muscarinic acdetylcholine receptor. Bioorg Med Chem 16: 1376-1392.
25. 2 receptors. Implications for atypical antipsychotic action. J Psychiatry Neurosci 25: 161-166.
26. Kapur S, Seeman P (2001). Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: a new hypothesis. Am J Psychiatry 158: 360-369.
27. 2-adrenoceptor antagonists. Eur J Pharmacol 335: 99-105.
28. 1 receptors. J Recept Signal Transduct Res 29: 84-93.
29. 1-receptor blockers in isolated vessels of different origin. Hypertension 33: 1406-1413.
30. Motulsky HJ, Mahan LC (1984). The kinetics of competitive radioligand binding predicted by the law of mass action. Mol Pharmacol 25: 1-9.
31. Norman JA, Drummond AH, Moser P (1979). Inhibition of calcium-dependent regulator-stimulated phosphodiesterase activity by neuroleptic drugs is unrelated to their clinical efficacy. Mol Pharmacol 16: 1089-1094.
32. 1 receptor. Eur J Pharmacol 319: 137-146.
33. 2L- receptor interactions in intact cells. Biochem Pharmacol 75: 2192-2203.
34. 2S-dopamine receptor interactions in intact Chinese recombinant ovary cells. Fund Clin Pharmacol 24: 293-303.
35. 2L-receptors in intact recombinant Chinese Hamster Ovary cells. Fund Clin Pharmacol 24: 283-291.
36. Rhodes DG, Newton R, Butler R, Herbette L (1992). Equilibrium and kinetic studies of the interactions of salmeterol with membrane bilayers. Mol Pharmacol 42: 596-602.
37. Schneider LS, Dagerman K, Insel PS (2006). Efficacy and adverse effects of atypical antipsychotics for dementia: meta-analysis of randomized, placebocontrolled trials. Am J Geriatr Psychiatry 14: 191-210.
38. Seeman P, Chau-Wong M, Tedesco J, Wong K (1975). Brain receptors for antipsychotic drugs and dopamine: direct binding assays. Proc Natl Acad Sci U S A 72: 4376-4380.
39. 7 Serotonin Receptor. Mol Pharmacol 70: 1264-1270.
40. 2 adrenoceptors. J Pharmacol Toxicol Methods 58: 189-197.
41. Swinney DC (2004). Biochemical mechanisms of drug action: what does it take for success? Nat Rev Drug Discov 3: 801-808.
42. Swinney DC (2006). Can Binding Kinetics Translate to a Clinically Differentiated Drug? From Theory to Practice. Lett Drug Des Discov 3: 569-574.
43. 2-adrenoceptor agonist salmeterol. Br J Pharmacol 158: 183-194.
44. Timmermans PBMWM (1999). Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol 15: 16F-28F.
45. Tummino PJ, Copeland RA (2008). Residence time of receptor-ligand complexes and its effect on biological function. Biochemistry 47: 5481-5492.
46. Unger T (1999). Significance of angiotensin type 1 receptor blockade: why are angiotensin II receptor blockers different? Am J Cardiol 84: 9S-15S.
47. 1 receptors expressed in CHO-K1 cells. Biochem Pharmacol 59: 927-935.
48. Vauquelin G, Szczuka A (2007). Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation. Neurochem Int 51: 254-260.
49. Vauquelin G, Van Liefde I (2006). Slow antagonist dissociation and long-lasting in vivo receptor protection. Trends Pharmacol Sci 27: 356-359.
50. 1 receptor antagonism: the need for different antagonist binding states of the receptor. Trends Pharmacol Sci 22: 343-344.
51. Vauquelin G, Van Liefde I, Vanderheyden P (2002). Models and methods for studying insurmountable antagonism. Trends Pharmacol Sci 23: 514-518.
52. 1 cannabinoid receptor-expressing cells. Fund Clin Pharmacol 24: 181-187.
53. Wienen W, Hauel N, Van Meel JCA, Narr B, Ries U, Entzeroth M (1993). Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br J Pharmacol 110: 245-252.