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Results: 1 to 20 of 112

1.

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

Jucaite A, Takano A, Boström E, Jostell KG, Stenkrona P, Halldin C, Segerdahl M, Nyberg S.

Int J Neuropsychopharmacol. 2013 Jul;16(6):1231-9. doi: 10.1017/S1461145712001411. Epub 2012 Dec 10.

PMID:
23217964
[PubMed - indexed for MEDLINE]
2.

Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET.

Ashworth S, Rabiner EA, Gunn RN, Plisson C, Wilson AA, Comley RA, Lai RY, Gee AD, Laruelle M, Cunningham VJ.

J Nucl Med. 2010 Jul;51(7):1021-9. doi: 10.2967/jnumed.109.071753. Epub 2010 Jun 16.

PMID:
20554726
[PubMed - indexed for MEDLINE]
Free Article
3.

Blockade of the brain histamine H3 receptor by JNJ-39220675: preclinical PET studies with [¹¹C]GSK189254 in anesthetized baboon.

Logan J, Carruthers NI, Letavic MA, Sands S, Jiang X, Shea C, Muench L, Xu Y, Carter P, King P, Fowler JS.

Psychopharmacology (Berl). 2012 Oct;223(4):447-55. Epub 2012 May 22.

PMID:
22614669
[PubMed - indexed for MEDLINE]
Free PMC Article
4.

11C-GSK189254: a selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET.

Plisson C, Gunn RN, Cunningham VJ, Bender D, Salinas CA, Medhurst AD, Roberts JC, Laruelle M, Gee AD.

J Nucl Med. 2009 Dec;50(12):2064-72. doi: 10.2967/jnumed.109.062919. Epub 2009 Nov 12.

PMID:
19910432
[PubMed - indexed for MEDLINE]
Free Article
5.

Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.

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.

Br J Pharmacol. 2009 May;157(1):104-17. doi: 10.1111/j.1476-5381.2009.00205.x.

PMID:
19413575
[PubMed - indexed for MEDLINE]
Free PMC Article
6.

GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.

Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB, Davis RK, Davis RP, Dawson LA, Foley AG, Gartlon J, Gonzalez MI, Heslop T, Hirst WD, Jennings C, Jones DN, Lacroix LP, Martyn A, Ociepka S, Ray A, Regan CM, Roberts JC, Schogger J, Southam E, Stean TO, Trail BK, Upton N, Wadsworth G, Wald JA, White T, Witherington J, Woolley ML, Worby A, Wilson DM.

J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. Epub 2007 Feb 27.

PMID:
17327487
[PubMed - indexed for MEDLINE]
Free Article
7.

(11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists.

Van Laere KJ, Sanabria-Bohórquez SM, Mozley DP, Burns DH, Hamill TG, Van Hecken A, De Lepeleire I, Koole M, Bormans G, de Hoon J, Depré M, Cerchio K, Plalcza J, Han L, Renger J, Hargreaves RJ, Iannone R.

J Nucl Med. 2014 Jan;55(1):65-72. doi: 10.2967/jnumed.113.122515. Epub 2013 Nov 21.

PMID:
24263088
[PubMed - indexed for MEDLINE]
8.

Use of the H3 receptor antagonist radioligand [3H]-A-349821 to reveal in vivo receptor occupancy of cognition enhancing H3 receptor antagonists.

Miller TR, Milicic I, Bauch J, Du J, Surber B, Browman KE, Marsh K, Cowart M, Brioni JD, Esbenshade TA.

Br J Pharmacol. 2009 May;157(1):139-49. doi: 10.1111/j.1476-5381.2009.00239.x.

PMID:
19413577
[PubMed - indexed for MEDLINE]
Free PMC Article
9.

Kinetic analysis of drug-target interactions with PET for characterization of pharmacological hysteresis.

Salinas C, Weinzimmer D, Searle G, Labaree D, Ropchan J, Huang Y, Rabiner EA, Carson RE, Gunn RN.

J Cereb Blood Flow Metab. 2013 May;33(5):700-7. doi: 10.1038/jcbfm.2012.208. Epub 2013 Feb 6.

PMID:
23385202
[PubMed - indexed for MEDLINE]
Free PMC Article
10.

Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists.

Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H.

J Pharmacol Exp Ther. 2008 Jun;325(3):902-9. doi: 10.1124/jpet.107.135343. Epub 2008 Feb 27.

PMID:
18305012
[PubMed - indexed for MEDLINE]
Free Article
11.

Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain.

Medhurst SJ, Collins SD, Billinton A, Bingham S, Dalziel RG, Brass A, Roberts JC, Medhurst AD, Chessell IP.

Pain. 2008 Aug 15;138(1):61-9. doi: 10.1016/j.pain.2007.11.006. Epub 2007 Dec 31.

PMID:
18164820
[PubMed - indexed for MEDLINE]
12.

Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over-expressing TASTPM mice.

Medhurst AD, Roberts JC, Lee J, Chen CP, Brown SH, Roman S, Lai MK.

Br J Pharmacol. 2009 May;157(1):130-8. doi: 10.1111/j.1476-5381.2008.00075.x. Epub 2009 Feb 16.

PMID:
19222483
[PubMed - indexed for MEDLINE]
Free PMC Article
13.

In vivo receptor occupancy assay of histamine H₃ receptor antagonist in rats using non-radiolabeled tracer.

Nirogi R, Kandikere V, Bhyrapuneni G, Muddana N, Saralaya R, Ponnamaneni RK, Manoharan AK.

J Pharmacol Toxicol Methods. 2012 May-Jun;65(3):115-21. doi: 10.1016/j.vascn.2012.03.003. Epub 2012 Apr 1.

PMID:
22487318
[PubMed - indexed for MEDLINE]
14.

Inverse agonist histamine H3 receptor PET tracers labelled with carbon-11 or fluorine-18.

Hamill TG, Sato N, Jitsuoka M, Tokita S, Sanabria S, Eng W, Ryan C, Krause S, Takenaga N, Patel S, Zeng Z, Williams D Jr, Sur C, Hargreaves R, Burns HD.

Synapse. 2009 Dec;63(12):1122-32. doi: 10.1002/syn.20689.

PMID:
19670309
[PubMed - indexed for MEDLINE]
15.

Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand.

Witte DG, Yao BB, Miller TR, Carr TL, Cassar S, Sharma R, Faghih R, Surber BW, Esbenshade TA, Hancock AA, Krueger KM.

Br J Pharmacol. 2006 Jul;148(5):657-70. Epub 2006 May 22.

PMID:
16715122
[PubMed - indexed for MEDLINE]
Free PMC Article
16.

Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems.

Hsieh GC, Honore P, Pai M, Wensink EJ, Chandran P, Salyers AK, Wetter JM, Zhao C, Liu H, Decker MW, Esbenshade TA, Cowart MD, Brioni JD.

Brain Res. 2010 Oct 1;1354:74-84. doi: 10.1016/j.brainres.2010.07.083. Epub 2010 Aug 1.

PMID:
20682302
[PubMed - indexed for MEDLINE]
17.

Regional differential effects of the novel histamine H3 receptor antagonist 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254) on histamine release in the central nervous system of freely moving rats.

Giannoni P, Medhurst AD, Passani MB, Giovannini MG, Ballini C, Corte LD, Blandina P.

J Pharmacol Exp Ther. 2010 Jan;332(1):164-72. doi: 10.1124/jpet.109.158444. Epub 2009 Oct 8.

PMID:
19815811
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

Histamine H3-receptor inverse agonists as novel antipsychotics.

Ito C.

Cent Nerv Syst Agents Med Chem. 2009 Jun;9(2):132-6. Review.

PMID:
20021346
[PubMed - indexed for MEDLINE]
19.

Detection of low level histamine H3 receptor occupancy by autoradiography.

Le S, Finn JP, Larijani ME, Marino MJ, Schaffhauser H.

J Neurosci Methods. 2009 Dec 15;185(1):70-5. doi: 10.1016/j.jneumeth.2009.09.015. Epub 2009 Sep 16.

PMID:
19765611
[PubMed - indexed for MEDLINE]
20.

CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities.

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.

J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. doi: 10.1124/jpet.111.186585. Epub 2011 Oct 14.

PMID:
22001260
[PubMed - indexed for MEDLINE]
Free Article

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