Neurokinin 1 receptor antagonists: Correlation between in vitro receptor interaction and in vivo efficacy

Journal of Pharmacology and Experimental Therapeutics

Volumn 322, Issue 3, 2007, Pages 1286-1293

  Lindström, Erik ^a   Von Mentzer, Bengt ^a   Påhlman, Ingrid ^a   Ahlstedt, Ingela ^a   Uvebrant, Anna ^a   Kristensson, Elin ^a   Martinsson, Rakel ^a   Novén, Anna ^a   De Verdier, Jennie ^a   Vauquelin, Georges ^b  

^a ASTRAZENECA R AND D   (Sweden)

^b VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 METHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; 3 CYANO N [[2 (3,4 DICHLOROPHENYL) 4 [4 [2 (METHYLSULFINYL)PHENYL]PIPERIDINO]BUTYL] N METHYL]NAPTHAMIDE; APREPITANT; CALCIUM ION; NEUROKININ 1 RECEPTOR ANTAGONIST; PIPERIDINE DERIVATIVE; SUBSTANCE P; UNCLASSIFIED DRUG; ZD 6021;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING COMPETITION; BIOLOGICAL MONITORING; CALCIUM MOBILIZATION; CHRONOPHARMACOLOGY; CONCENTRATION RESPONSE; CONTROLLED STUDY; CORPUS STRIATUM; CORRELATION ANALYSIS; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; FLUOROMETRY; FOOT; GERBIL; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; SINGLE DRUG DOSE; STIMULUS RESPONSE;

ANIMALS; BEHAVIOR, ANIMAL; CALCIUM SIGNALING; CELL LINE; GERBILLINAE; HUMANS; PIPERIDINES; RECEPTORS, NEUROKININ-1; SULFOXIDES;

EID: 34548087297     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.107.124958     Document Type: Article

References (53)

1. Aiyar N, Baker E, Vickery-Clark L, Ohlstein EH, Gellai M, Fredrickson TA, Brooks DP, Weinstock J, Weidley EF, and Edwards RM (1995) Pharmacology of a potent long-acting imidazole-5-acrylic acid angiotensin AT1 receptor antagonist. Eur J Pharmacol 283:63-72.
2. Anthes JC, Gilchrest H, Richard C, Eckel S, Hesk D, West RE Jr, Williams SM, Greenfeder S, Billah M, Kreutner W, et al. (2002) Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol 449:229-237.
3. Beresford IJM, Birch PJ, Hagan RM, and Ireland SJ (1991) Investigation into species variants in tachykinin NK1 receptors by use of the non-peptide antagonist, CP-96,345. Br J Pharmacol 104:292-293.
4. Bergström M, Fasth KJ, Kilpatrick G, Ward P, Cable KM, Wipperman MD, Sutherland DR, and Långström B (2000) Brain uptake and receptor binding of two [11C]labelled selective high affinity NK1-antagonists, GR203040 and GR205171-PET studies in rhesus monkey. Neuropharmacology 39:664-670.
5. Bernstein PR, Aharony D, Albert JS, Andisik D, Barthlow HG, Bialecki R, Davenport T, Dedinas RF, Dembofsky BT, Koether G, et al. (2001) Discovery of novel, orally active dual NK1/NK2 antagonists. Bioorg Med Chem Lett 11:2769-2773.
6. Blower PR (2003) Granisetron: relating pharmacology to clinical efficacy. Support Care Cancer 11:93-100.
7. Bond RA, Ornstein AG, and Clarke DE (1989) Unsurmountable antagonism to 5-hydroxytryptamine in rat kidney results from pseudoirreversible inhibition rather than multiple receptors or allosteric receptor modulation. J Pharmacol Exp Ther 249:401-410.
8. Bristow LJ and Young L (1994) Chromodacryorrhea and repetitive hind paw tapping: models of peripheral and central tachykinin NK1 receptor activation in gerbils. Eur J Pharmacol 253:245-252.
9. Chu CL, Buczek-Thomas JA, and Nugent MA (2004) Heparan sulphate proteoglycans modulate fibroblast growth factor-2 binding through a lipid raft-mediated mechanism. Biochem J 379:331-341.
10. 1 receptor antagonist. Eur J Pharmacol 341:201-209.
11. Copeland RA, Pompliano DL, and Meek TD (2006) Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov 5:730-739.
12. De Arriba AF, Gomez-Casajus LA, Cavalcanti F, Almansa C, Garcia-Rafanell J, and Forn J (1996) In vitro pharmacological characterization of a new selective angiotensin AT1 receptor antagonist, UR 7280. Eur J Pharmacol 318:341-347.
13. Duffy RA, Varty GB, Morgan CA, and Lachowicz JE (2002) Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists. J Pharmacol Exp Ther 301:536-542.
14. Eistetter HR, Mills A, Brewster R, Alouani S, Rambossom C, and Kawashima E (1992) Functional characterization of neurokinin-1- receptors on human U373MG astrocytoma cells. Glia 6:89-95.
15. Emonds-Alt X, Doutremepuich JD, Heaulme M, Neliat G, Santucci V, Steinberg R, Vilain P, Bichon D, Ducoux JP, Proietto V, et al. (1993) In vitro and in vivo biological activities of SR140333, a novel potent non-peptide tachykinin NK1 receptor antagonist. Eur J Pharmacol 250:403-413.
16. el-Bizri H and 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.
17. Engberg S, Ahlstedt A, Leffler A, Lindström E, Kristensson E, Svensson A, Påhlman I, Johansson A, Drmota T, and von Mentzer B (2007) Molecular cloning, mutations and effects of NK1 receptor antagonists reveal the human-like pharmacology of gerbil NK1 receptors. Biochem Pharmacol 73:259-269.
18. 1 receptor-transfected Chinese hamster ovary cells. Eur J Pharmacol 367:413-422.
19. 1 receptor antagonists: the role of tight antagonist binding. Eur J Pharmacol 372:199-206.
20. Gaddum JH, Hameed KA, Hathway DE, and Stephens FF (1955) Quantitative studies of antagonists for 5-hydroxytryptamine. Q J Exp Physiol 40:49-74.
21. 3H]GR205171 displays similar NK1 receptor binding profile in gerbil and human brain. Br J Pharmacol 148:39-45.
22. Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, Ber E, Chicchi GG, Kurtz M, Metzger J, et al. (1998) Structural optimization affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S) -(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist. J Med Chem 41:4607-4614.
23. Hargreaves R (2002) Imaging substance P receptor antagonists in the living human brain using positron emission tomography. J Clin Psychiatry 63:18-24.
24. 2 receptors: evidence for selective sorting of receptor and ligand. Mol Endocrinol 11:1266-1177.
25. Huskey S-EW, Dean BJ, Bakhtiar R, Sanchez RI, Tattersall FD, Rycroft W, Hargreaves R, Watt AP, Chicchi GG, Keohane C, et al. (2003) Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets. Drug Metab Dispos 31:785-791.
26. Jenkinson KM, Southwell BR, and Furness JB (1999) Two affinities for a single antagonist at the neuronal NK1 tachykinin receptor: evidence from quantitation of receptor endocytosis. Br J Pharmacol 126:131-136.
27. Keller M, Montgomery S, Ball W, Morrison M, Snavely D, Liu G, Hargreaves R, Hietala J, Lines C, Beebe K, et al. (2006) Lack of efficacy of the substance P (neurokinin1 receptor) antagonist aprepitant in the treatment of major depressive disorder. Biol Psychiatry 59:216-223.
28. Kukkonen JP, Huifang G, Jansson CC, Wurster S, Cockcroft V, Savola JM, and Akerman KE (1997) Different apparent modes of inhibition of alpha2A-adrenoceptor by alpha2-adrenoceptor antagonists. Eur J Pharmacol 335:99-105.
29. 1 receptors transiently and stably expressed in CHO-K1 cells. Eur J Pharmacol 513:35-45.
30. 2-like receptors: can they be classified with the available antagonists? Br J Pharmacol 88:585-593.
31. Liu YJ, Shankley NP, Welsh NJ, and Black JW (1992) Evidence that the apparent complexity of receptor antagonism by angiotensin II analogues is due to a reversible, synoptic action. Br J Pharmacol 106:233-241.
32. 3H]methylscopolamine from isolated guinea pig atria is controlled by diffusion and rebinding. J Pharmacol Exp Ther 247:710-714.
33. McLean S, Ganong A, Seymour PA, Bryce DK, Crawford RT, Morrone J, Reynolds LS, Schmidt AW, Zorn S, Watson J, et al. (1996) Characterization of CP-122,721; a nonpeptide antagonist of the neurokinin NK1 receptor. J Pharmacol Exp Ther 277:900-908.
34. McLean S, Ganong A, Seymour PA, Snider RM, Desai MC, Rosen T, Bryce DK, Longo KP, Reynolds LS, and Robinson G (1993) Pharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J Pharmacol Exp Ther 267:472-479.
35. Page NM (2006) Characterization of the gene structures, precursor processing and pharmacology of the endokinin peptides. Vascul Pharmacol 45:200-208.
36. Paton WDM and Rang HP (1966) A kinetic approach to the mechanism of drug action. Adv Drug Res 3:57-80.
37. Paton WDM and Waud DR (1967) The margin of safety of neuromuscular transmission. J Physiol 191:59-90.
38. Pedersen KE. Buckner CK, Meeker SN, and Undem BJ (2000) Pharmacological examination of the neurokinin-1 receptor mediating relaxation of human intralobar pulmonary artery. J Pharmacol Exp Ther 292:319-325.
39. Pennefather JN, Alessandro L, Candenas ML, Patak E, Pinto FM, and Maggi CA (2004) Tachykinins and tachykinin receptors: a growing family. Life Sci 74:1445-1463.
40. Quartara L and Altamura M (2006) Tachykinin receptors antagonists: from research to clinic. Curr Drug Targets 7:975-992.
41. Rumsey WL, Aharony D, Bialecki RA, Abbott BM, Barthlow HG, Caccese R, Ghanekar S, Lengel D, McCarthy M, Wenrich B, et al. (2001) Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors. J Pharmacol Exp Ther 298:307-315.
42. Severini C, Improta G, Falconieri-Erspamer G, Salvadori S, and Erspamer V (2002) The tachykinin peptide family. Pharm Rev 54:285-322.
43. Smith DW, Hewson L, Fuller P, Williams AR, Wheeldon A, and Rupniak NMJ (1999) The substance P antagonist L-760735 inhibits stress-induced NK1 receptor internalisation in the basolateral amygdala. Brain Res 848:90-95.
44. Southwell BR, Woodman HL, Murphy R, Royal SJ, and Furness JB (1996) Characterisation of substance P-induced endocytosis of NK1 receptors on enteric neurons. Histochem Cell Biol 106:563-571.
45. Swinney DC (2004) Biochemical mechanisms of drug action: what does it take for success? Nat Rev Drug Discov 3:801-808.
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. 1 receptors and their non-peptide antagonists. Biochem Pharmacol 61:277-284.
49. Vauquelin G and Van Liefde I (2006) Slow antagonist dissociation and long-lasting in vivo receptor protection. Trends Pharmacol Sci 27:356-359.
50. Vauquelin G, Van Liefde I, Birzbier BB, and Vanderheyden PML (2002a) New insights in insurmountable antagonism. Fundam Clin Pharmacol 16:263-272.
51. Vauquelin G, Van Liefde I, and Vanderheyden P (2002b) Models and methods for studying insurmountable antagonism. Trends Pharmacol Sci 23:514-518.
52. Verheijen I, Fierens FLP, De Backer J-P, Vauquelin G, and Vanderheyden PML (2000) Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors. Fundam Clin Pharmacol 14:577-585.
53. Wienen W, Hauel N, Van Meel JC, Narr B, Ries U, and Entzeroth M (1993) Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br J Pharmacol 110:245-252.