AZD5213: A novel histamine H3 receptor antagonist permitting high daytime and low nocturnal H3 receptor occupancy, a PET study in human subjects

International Journal of Neuropsychopharmacology

Volumn 16, Issue 6, 2013, Pages 1231-1239

  Jucaite, Aurelija ^a   Takano, Akihiro ^b   Boström, Emma ^a   Jostell, Karl Gustav ^a   Stenkrona, Per ^b   Halldin, Christer ^b   Segerdahl, Märta ^a   Nyberg, Svante ^a  

^a ASTRAZENECA R AND D   (Sweden)

^b KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

AZD5213; histamine H3 antagonists; histamine H3 receptors; PET

Indexed keywords

6 (3 CYCLOBUTYL 2,3,4,5 TETRAHYDRO 1H 3 BENZAZEPIN 7 YLOXY) N METHYLNICOTINAMIDE CARBON 11; AZ 12807110 CARBON 11; AZD 5213; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; RADIOLIGAND; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; CIRCADIAN RHYTHM; DRUG BLOOD LEVEL; DRUG EFFICACY; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; SINGLE DRUG DOSE; SLEEP DISORDER;

ADULT; AUTORADIOGRAPHY; BENZAZEPINES; BRAIN; CARBON RADIOISOTOPES; CIRCADIAN RHYTHM; DOSE-RESPONSE RELATIONSHIP, DRUG; HISTAMINE H3 ANTAGONISTS; HUMANS; MALE; NIACINAMIDE; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; RADIOLIGAND ASSAY; RECEPTORS, HISTAMINE H3; YOUNG ADULT;

EID: 84878887148     PISSN: 14611457     EISSN: 14695111     Source Type: Journal    
DOI: 10.1017/S1461145712001411     Document Type: Article

References (40)

1. Arrang JM, Garbarg M, Schwartz JC (1983)Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 302:832-837.
2. Ashworth S, Rabiner EA, Gunn RN, Plisson C, Wilson AA, Comley RA, Lai RY, Gee AD, Laruelle M, Cunningham VJ (2010) Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET. J Nucl Med 51:1021-1029.
3. Blandina P, Giorgetti M, Bartolini L, Cecchi M, Timmerman H, Leurs R, Pepeu G, GiovanniniMG (1996) Inhibition of cortical acetylcholine release and cognitive performance by histamine H3 receptor activation in rats. Brit J Pharmacol 119:1656-1664.
4. Brioni JD, Esbenshade TA, Garrison TR, Bitner SR, Covart MD (2011). Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease. J Pharmacol Exp Ther 336:38-46.
5. Broderick M, Masri T (2011). Histamine H(3) receptor (H(3)R) antagonists and inverse agonists in the treatment of sleep disorders. Curr Pharm Des 17:1426-1429.
6. Catafau AM, Penengo MM, Nucci G, Bullich S, Corripio I, Parellada E, García-Ribera C, Gomeni R, Merlo-Pich E; Barcelona Clinical Imaging in Psychiatry Group (2008). Pharmacokinetics and time-course of D(2) receptor occupancy induced by atypical antipsychotics in stabilized schizophrenic patients. J Psychopharmacol 22:882-894.
7. Clapham J, Kilpatrick GJ (1992). Histamine H3 receptors modulate the release of [3H]-acetylcholine from slices of rat entorhinal cortex : Evidence for the possible existence of H3 receptor subtypes. Brit J Pharmacol 107:919-923.
8. Cunningham VJ, Rabiner EA, Slifstein M, Laruelle M, Gunn RN (2010). Measuring drug occupancy in the absence of a reference region : The Lassen plot re-visited. J Cereb Blood Flow Metab 30:46-50.
9. Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (2008). The histamine H3 receptor : An attractive target for the treatment of cognitive disorders. Br J Pharmacol 154:1166-1181.
10. Farde L, Eriksson L, Blomquist G, Halldin C (1989). Kinetic analysis of central [11C]raclopride binding to D2-dopamine receptors studied by PET - a comparison to the equilibrium analysis. J Cereb Blood Flow Metab 9 :696-708.
11. Guo RX, Anaclet C, Roberts JC, Parmentier R, Zhang M, Guidon G, Buda C, Sastre JP, Feng JQ, Franco P, Brown SH, Upton N, Medhurst AD, Lin JS (2009). Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox -/- mice. Brit J Pharmacol 157:104-117.
12. Iannone R et al. (2009). The relationship between brain receptor occupancy (RO) and alerting effects in humans support MK-0249 and MK-3134 as inverse agonists at the histamine subtype-3 pre-synaptic receptor (H3R). ACNP 48th Annual Meeting; December 6-10; Hollywood, FL. Nashville, TN, USA: American College of Neuropsychopharmacology.
13. Iannone R, Palcza J, Renger JJ, Calder N, Cerchio K, Gottesdiener K, Hargreaves R, Dijk DJ, Boyle J, Murphy MG (2010). Acute alertness-promoting effects of a novel histamine subtype-3 receptor inverse agonist in healthy sleep-deprived male volunteers. Clin Pharmacol Ther 88:831-839.
14. Kapur S, Zipursky R, Jones C, Shammi CS, Remington G, Seeman P (2000). A positron emission tomography study of quetiapine in schizophrenia : A preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry 57:553-559.
15. Kiviranta T, Tuomisto L, Airaksinen EM (1994). Diurnal and age-related changes in cerebrospinal fluid tele-methylhistamine levels during infancy and childhood. Pharmacol Biochem Behav 49:997-1000.
16. Lassen NA, Bartenstein PA, Lammertsma AA, Prevett MC, Turton DR, Luthra SK, Osman S, Bloomfield PM, Jones T, Patsalos PN, O'Connell MT, JS, Duncan JS, Vanggaard Andersen (1995). Benzodiazepine receptor quantification in vivo in humans using [11C]flumazenil and PET: application of the steady-state principle. J Cereb Blood Flow Metab 15:152-165.
17. Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H (2008). Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists. J Pharmacol Exp Ther 325:902-909.
18. Lin JS, Sakai K, Vanni-Mercier G, Arrang JM, Garbarg M, Schwartz JC, Jouvet M (1990). Involvement of histaminergic neurons in arousal mechanisms demonstrated with H3-receptor ligands in the cat. Brain Res 523:325-330.
19. Lin JS, Sergeeva OA, Haas HL (2011). Histamine H3 receptors and sleep-wake regulation. J Pharmacol Exp Ther 336:17-23.
20. Logan J, Carruthers NI, Letavic MA, Sands S, Jiang X, Shea C, Muench L, Xu Y, Carter P, King P, Fowler JS (2012). Blockade of the brain histamine H3 receptor by JNJ-39220675: Preclinical PET studies with [(11)C]GSK189254 in anesthetized baboon. Psychopharmacol (Berl) 223:447-455.
21. Martinez-Mir MI, Pollard H, Moreau J, Arrang JM, Ruat M, Traiffort E, Schwartz JC, Palacios JM (1990). Three histamine receptors (H1, H2 and H3) visualized in the brain of human and non-human primates. Brain Res 526:322-327.
22. Medhurst AD et al. (2007). GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther 321:1032-1045.
23. Murillo-Rodríguez E, Arias-Carrión O, Sanguino- Rodríguez K, González-Arias M, Haro A (2009). Mechanisms of sleep-wake cycle modulation. CNS Neurol Disord Drug Targets 8 :245-253.
24. Nord M, Nyberg S, Brogren J, Jucaite A, Halldin C, Farde L (2011). Comparison of D2 dopamine receptor occupancy after oral administration of quetiapine fumarate immediate-release and extended-release formulations in healthy subjects. Int J Neuropsychopharmacol 14:1357-1366.
25. Nuutinen S, Panula P (2010). Histamine in neurotransmission and brain diseases. Adv Exp Med Biol 709:95-107.
26. Olsson H, Farde L (2005). Half-life of receptor occupancy-a meaningless concept. Int J Neuropsychopharmacol 8:141-142.
27. Passani MB, Blandina P (2011). Histamine receptors in the CNS as targets for therapeutic intervention. Trends Pharmacol Sci 32:242-249.
28. Plisson C, Gunn RN, Cunningham VJ, Bender D, Salinas CA, Medhurst AD, Roberts JC, Laruelle M, Gee AD (2009). 11CGSK189254 : A selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET. J Nucl Med 50:2064-2072.
29. Prell GD, Khandelwal JK, Burns RS, Green JP (1989). Diurnal fluctuation in levels of histamine metabolites in cerebrospinal fluid of rhesus monkey. Agents Actions 26:279-286.
30. Raddatz R, Hudkins RL, Mathiasen JR, Gruner JA, Flood DG, Aimone LD, Le S, Schaffhauser H, Duzic E, Gasior M, Bozyczko-Coyne D, Marino MJ, Ator MA, Bacon ER, Mallamo JP, Williams M (2012). CEP-26401 (irdabisant), a potent and selective histamine H3 receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities. J Pharmacol Exp Ther 340:124-133.
31. Schlicker E, Fink K, Detzner M, Göthert M (1993). Histamine inhibits dopamine release in the mouse striatum via presynaptic H3 receptors. J Neural Transm Gen Sect 93:1-10.
32. Schlicker E, Fink K, Hinterthaner M, GöthertM(1989). Inhibition of noradrenaline release in the rat brain cortex via presynaptic H3 receptors. Naunyn Schmiedebergs Arch Pharmacol 340:633-638.
33. Schwartz JC (2011). The histamineH3 receptor : From discovery to clinical trials with pitolisant. Br J Pharmacol 163:713-721.
34. Shan L, Bossers K, Luchetti S, Balesar R, Lethbridge N, Chazot PL, Bao AM, Swaab DF (2012a). Alterations in the histaminergic system in the substantia nigra and striatum of Parkinson's patients : A postmortem study. Neurobiol Aging 33:1488.e1-13.
35. Shan L, Bossers K, Unmehopa U, Bao AM, Swaab DF (2012b) Alterations in the histaminergic system in Alzheimer's disease : A postmortem study. Neurobiol Aging 33:2585-2598.
36. Soares H, Wagner T, Schmidt A, Sweeney F, McLellan T, Nelson F, Spracklin D, Wang E, Faessel H, Pinter G, Li X, Chappel P (2009). H3 receptor antagonism increases methylhistamine level in the cerebrospinal fluid of dogs and healthy human volunteers. In International Conference on Alzheimer's Disease, 11-16 July, Vienna, Austria. Chicago, IL, USA: Alzheimer's Association.
37. Stocking EM, LEtavic MA (2008). Histamine H3 antagonists as wake-promoting and pro-cognitive agents. Curr Top Med Chem 8 :988-1002.
38. Tzourio-Mazoyer N, Landeau B, Papathanassiou D, Crivello F, Etard O, Delcroix N, Mazoyer B, Joliot M (2002). Automated anatomical labeling of activiations in SPM using a macroscopic anatomical parcellation of the MNI MRI singlesubject brain. NeuroImage 15:273-289.
39. van Wamelen DJ, Shan L, Aziz NA, Anink JJ, Bao AM, Roos RA, Swaab DF (2011). Functional increase of brain histaminergic signaling in Huntington's disease. Brain Pathol 21:419-427.
40. Varrone A, Sjöholm N, Eriksson L, Gulyás B, Halldin C, Farde L (2009). Advancement in PET quantification using 3D-OP-OSEM point spread function reconstruction with the HRRT. Eur J Nucl Med Mol Imaging 36:1639-1650.