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Items: 1 to 50 of 213

1.

Binding characterization of N-(2-chloro-5-thiomethylphenyl)-N'-(3-[3 H]3 methoxy phenyl)-N'-methylguanidine ([3 H]GMOM), a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist.

Metaxas A, van Berckel BNM, Klein PJ, Verbeek J, Nash EC, Kooijman EJM, Renjaän VA, Golla SSV, Boellaard R, Christiaans JAM, Windhorst AD, Leysen JE.

Pharmacol Res Perspect. 2019 Feb;7(1):e00458. doi: 10.1002/prp2.458.

2.

Lipophilic nalmefene prodrugs to achieve a one-month sustained release.

Gaekens T, Guillaume M, Borghys H, De Zwart LL, de Vries R, Embrechts RC, Vermeulen A, Megens AA, Leysen JE, Herdewijn P, Annaert PP, Atack JR.

J Control Release. 2016 Jun 28;232:196-202. doi: 10.1016/j.jconrel.2016.04.029. Epub 2016 Apr 21.

PMID:
27107723
3.

Preclinical evaluation of [(18)F]PK-209, a new PET ligand for imaging the ion-channel site of NMDA receptors.

Golla SS, Klein PJ, Bakker J, Schuit RC, Christiaans JA, van Geest L, Kooijman EJ, Oropeza-Seguias GM, Langermans JA, Leysen JE, Boellaard R, Windhorst AD, van Berckel BN, Metaxas A.

Nucl Med Biol. 2015 Feb;42(2):205-12. doi: 10.1016/j.nucmedbio.2014.09.006. Epub 2014 Sep 30.

PMID:
25451213
4.

The dopamine stabilizer (-)-OSU6162 occupies a subpopulation of striatal dopamine D2/D3 receptors: an [(11)C]raclopride PET study in healthy human subjects.

Tolboom N, Berendse HW, Leysen JE, Yaqub M, van Berckel BN, Schuit RC, Ponsen MM, Bakker E, Hoetjes NJ, Windhorst AD, Carlsson ML, Lammertsma AA, Carlsson A.

Neuropsychopharmacology. 2015 Jan;40(2):472-9. doi: 10.1038/npp.2014.195. Epub 2014 Aug 5.

5.

Subchronic treatment with phencyclidine in adolescence leads to impaired exploratory behavior in adult rats without altering social interaction or N-methyl-D-aspartate receptor binding levels.

Metaxas A, Willems R, Kooijman EJ, Renjaän VA, Klein PJ, Windhorst AD, Donck LV, Leysen JE, Berckel BN.

J Neurosci Res. 2014 Nov;92(11):1599-607. doi: 10.1002/jnr.23433. Epub 2014 Jun 23.

PMID:
24953757
6.

Synthesis and preclinical evaluation of carbon-11 labelled N-((5-(4-fluoro-2-[(11)C]methoxyphenyl)pyridin-3-yl)methyl)cyclopentanamine as a PET tracer for NR2B subunit-containing NMDA receptors.

Christiaans JA, Klein PJ, Metaxas A, Kooijman EJ, Schuit RC, Leysen JE, Lammertsma AA, van Berckel BN, Windhorst AD.

Nucl Med Biol. 2014 Sep;41(8):670-80. doi: 10.1016/j.nucmedbio.2014.04.131. Epub 2014 May 10.

PMID:
24929961
7.

Radiosynthesis and preclinical evaluation of [11C]prucalopride as a potential agonist PET ligand for the 5-HT4 receptor.

Buiter HJ, Windhorst AD, Huisman MC, De Maeyer JH, Schuurkes JA, Lammertsma AA, Leysen JE.

EJNMMI Res. 2013 Apr 4;3(1):24. doi: 10.1186/2191-219X-3-24.

8.

[11C]AF150(S), an agonist PET ligand for M1 muscarinic acetylcholine receptors.

Buiter HJ, Windhorst AD, Huisman MC, Yaqub M, Knol DL, Fisher A, Lammertsma AA, Leysen JE.

EJNMMI Res. 2013 Mar 21;3(1):19. doi: 10.1186/2191-219X-3-19.

9.

Reproducible Analysis of Rat Brain PET Studies Using an Additional [(18)F]NaF Scan and an MR-Based ROI Template.

Buiter HJ, van Velden FH, Leysen JE, Fisher A, Windhorst AD, Lammertsma AA, Huisman MC.

Int J Mol Imaging. 2012;2012:580717. doi: 10.1155/2012/580717. Epub 2012 Sep 23.

10.

Quantification of the neurokinin 1 receptor ligand [¹¹C]R116301.

Wolfensberger SP, Maruyama K, van Berckel BN, Lubberink M, Airaksinen AJ, Boellaard R, Luurtsema G, Reddingius W, Janssens FE, Veltman DJ, Windhorst AD, Leysen JE, Lammertsma AA.

Nucl Med Commun. 2011 Oct;32(10):896-902. doi: 10.1097/MNM.0b013e328347e96f.

PMID:
21876400
11.

Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor.

Al Hussainy R, Verbeek J, van der Born D, Braker AH, Leysen JE, Knol RJ, Booij J, Herscheid JK.

J Med Chem. 2011 May 26;54(10):3480-91. doi: 10.1021/jm1009956. Epub 2011 Apr 26.

PMID:
21520940
12.

Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats.

Luurtsema G, Schuit RC, Klok RP, Verbeek J, Leysen JE, Lammertsma AA, Windhorst AD.

Nucl Med Biol. 2009 Aug;36(6):643-9. doi: 10.1016/j.nucmedbio.2009.03.004.

PMID:
19647170
13.

First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man.

Wolfensberger SP, van Berckel BN, Airaksinen AJ, Maruyama K, Lubberink M, Boellaard R, Carey WD, Reddingius W, Veltman DJ, Windhorst AD, Leysen JE, Lammertsma AA.

Mol Imaging Biol. 2009 Jul-Aug;11(4):241-5. doi: 10.1007/s11307-009-0204-5. Epub 2009 Mar 31.

14.

Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor.

Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P.

Life Sci. 2006 Dec 3;80(1):74-81. Epub 2006 Aug 25.

PMID:
16978659
15.

Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: evaluation of a potential PET ligand.

Airaksinen AJ, Jablonowski JA, van der Mey M, Barbier AJ, Klok RP, Verbeek J, Schuit R, Herscheid JD, Leysen JE, Carruthers NI, Lammertsma AA, Windhorst AD.

Nucl Med Biol. 2006 Aug;33(6):801-10.

PMID:
16934699
16.

Synthesis and biodistribution of [11C]R107474, a new radiolabeled alpha2-adrenoceptor antagonist.

Van der Mey M, Windhorst AD, Klok RP, Herscheid JD, Kennis LE, Bischoff F, Bakker M, Langlois X, Heylen L, Jurzak M, Leysen JE.

Bioorg Med Chem. 2006 Jul 1;14(13):4526-34. Epub 2006 Mar 6.

PMID:
16517171
17.

Internalization of human 5-HT4a and 5-HT4b receptors is splice variant dependent.

Pindon A, Van Hecke G, Josson K, Van Gompel P, Lesage A, Leysen JE, Jurzak M.

Biosci Rep. 2004 Jun;24(3):215-23.

PMID:
16209130
19.

Antagonist-induced supersensitivity of mGlu1 receptor signalling in cerebellar granule cells.

Lavreysen H, Willemoens T, Leysen JE, Lesage AS.

Eur J Neurosci. 2005 Mar;21(6):1610-6.

PMID:
15845088
20.

Synthesis and biodistribution of [(11)C]R116301, a promising PET ligand for central NK(1) receptors.

Van der Mey M, Janssen CG, Janssens FE, Jurzak M, Langlois X, Sommen FM, Verreet B, Windhorst AD, Leysen JE, Herscheid JD.

Bioorg Med Chem. 2005 Mar 1;13(5):1579-86.

PMID:
15698775
21.

MK-801 alters RGS2 levels and adenylyl cyclase sensitivity in the rat striatum.

Taymans JM, Cruz C, Lesage A, Leysen JE, Langlois X.

Neuroreport. 2005 Feb 8;16(2):159-62.

PMID:
15671868
22.

Metabotropic glutamate 1 receptor distribution and occupancy in the rat brain: a quantitative autoradiographic study using [3H]R214127.

Lavreysen H, Pereira SN, Leysen JE, Langlois X, Lesage AS.

Neuropharmacology. 2004 Apr;46(5):609-19.

PMID:
14996538
23.

5-HT2 receptors.

Leysen JE.

Curr Drug Targets CNS Neurol Disord. 2004 Feb;3(1):11-26. Review.

PMID:
14965241
24.

Functional study of rat 5-HT2A receptors using antisense oligonucleotides.

Van Oekelen D, Megens A, Meert T, Luyten WH, Leysen JE.

J Neurochem. 2003 Jun;85(5):1087-100.

25.

Ten years of antisense inhibition of brain G-protein-coupled receptor function.

Van Oekelen D, Luyten WH, Leysen JE.

Brain Res Brain Res Rev. 2003 May;42(2):123-42. Review.

PMID:
12738054
26.

[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.

Lavreysen H, Janssen C, Bischoff F, Langlois X, Leysen JE, Lesage AS.

Mol Pharmacol. 2003 May;63(5):1082-93.

PMID:
12695537
27.

5-HT2A and 5-HT2C receptors and their atypical regulation properties.

Van Oekelen D, Luyten WH, Leysen JE.

Life Sci. 2003 Apr 18;72(22):2429-49. Review.

PMID:
12650852
28.
29.

Expression and regulation of interleukin-10 and interleukin-10 receptor in rat astroglial and microglial cells.

Ledeboer A, Brevé JJ, Wierinckx A, van der Jagt S, Bristow AF, Leysen JE, Tilders FJ, Van Dam AM.

Eur J Neurosci. 2002 Oct;16(7):1175-85.

PMID:
12405978
30.

Daphnane-type diterpene orthoesters and their biological activities.

He W, Cik M, Appendino G, Puyvelde LV, Leysen JE, De Kimpe N.

Mini Rev Med Chem. 2002 Apr;2(2):185-200.

PMID:
12370079
31.

Role of 5-HT(2) receptors in the tryptamine-induced 5-HT syndrome in rats.

Van Oekelen D, Megens A, Meert T, Luyten WH, Leysen JE.

Behav Pharmacol. 2002 Jul;13(4):313-8.

PMID:
12218512
32.

Detailed localization of regulator of G protein signaling 2 messenger ribonucleic acid and protein in the rat brain.

Taymans JM, Wintmolders C, Te Riele P, Jurzak M, Groenewegen HJ, Leysen JE, Langlois X.

Neuroscience. 2002;114(1):39-53.

PMID:
12207953
33.

Neurotrophic and antileukemic daphnane diterpenoids from Synaptolepis kirkii.

He W, Cik M, Van Puyvelde L, Van Dun J, Appendino G, Lesage A, Van der Lindin I, Leysen JE, Wouters W, Mathenge SG, Mudida FP, De Kimpe N.

Bioorg Med Chem. 2002 Oct;10(10):3245-55.

PMID:
12150870
34.

Pharmacological profile of (2R-trans)-4-[1-[3,5-bis(trifluoromethyl)benzoyl]-2-(phenylmethyl)-4-piperidinyl]-N-(2,6-dimethylphenyl)-1-acetamide (S)-Hydroxybutanedioate (R116301), an orally and centrally active neurokinin-1 receptor antagonist.

Megens AA, Ashton D, Vermeire JC, Vermote PC, Hens KA, Hillen LC, Fransen JF, Mahieu M, Heylen L, Leysen JE, Jurzak MR, Janssens F.

J Pharmacol Exp Ther. 2002 Aug;302(2):696-709.

PMID:
12130734
35.

Nuclei and subnuclei gene expression profiling in mammalian brain.

Bonaventure P, Guo H, Tian B, Liu X, Bittner A, Roland B, Salunga R, Ma XJ, Kamme F, Meurers B, Bakker M, Jurzak M, Leysen JE, Erlander MG.

Brain Res. 2002 Jul 5;943(1):38-47.

PMID:
12088837
36.

Supersensitivity of human metabotropic glutamate 1a receptor signaling in L929sA cells.

Lavreysen H, Le Poul E, Van Gompel P, Dillen L, Leysen JE, Lesage AS.

Mol Pharmacol. 2002 May;61(5):1244-54.

PMID:
11961143
37.

Differences in signal transduction of two 5-HT4 receptor splice variants: compound specificity and dual coupling with Galphas- and Galphai/o-proteins.

Pindon A, van Hecke G, van Gompel P, Lesage AS, Leysen JE, Jurzak M.

Mol Pharmacol. 2002 Jan;61(1):85-96.

PMID:
11752209
38.
39.

Different regulation of rat 5-HT(2A) and rat 5-HT(2C) receptors in NIH 3T3 cells upon exposure to 5-HT and pipamperone.

Oekelen DV, Jurzak M, Van de Wiel D, Van Hecke G, Luyten WH, Leysen JE.

Eur J Pharmacol. 2001 Aug 3;425(1):21-32.

PMID:
11672571
40.

Use of the beta-imager for rapid ex vivo autoradiography exemplified with central nervous system penetrating neurokinin 3 antagonists.

Langlois X, te Riele P, Wintmolders C, Leysen JE, Jurzak M.

J Pharmacol Exp Ther. 2001 Nov;299(2):712-7.

PMID:
11602685
41.

Evaluation of the tetracycline- and ecdysone-inducible systems for expression of neurotransmitter receptors in mammalian cells.

Van Craenenbroeck K, Vanhoenacker P, Leysen JE, Haegeman G.

Eur J Neurosci. 2001 Sep;14(6):968-76.

PMID:
11595035
42.

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Briejer MR, Bosmans JP, Van Daele P, Jurzak M, Heylen L, Leysen JE, Prins NH, Schuurkes JA.

Eur J Pharmacol. 2001 Jun 29;423(1):71-83.

PMID:
11438309
43.

Does phenylethylamine act as an endogenous amphetamine in some patients?

Janssen PA, Leysen JE, Megens AA, Awouters FH.

Int J Neuropsychopharmacol. 1999 Sep;2(3):229-240.

PMID:
11281991
44.

Detailed distribution of Neurokinin 3 receptors in the rat, guinea pig and gerbil brain: a comparative autoradiographic study.

Langlois X, Wintmolders C, te Riele P, Leysen JE, Jurzak M.

Neuropharmacology. 2001;40(2):242-53.

PMID:
11114403
45.

Kirkinine, a new daphnane orthoester with potent neurotrophic activity from Synaptolepis kirkii.

He W, Cik M, Lesage A, Van der Linden I, De Kimpe N, Appendino G, Bracke J, Mathenge SG, Mudida FP, Leysen JE, Van Puyvelde L.

J Nat Prod. 2000 Sep;63(9):1185-7.

PMID:
11000015
46.

G-protein sensitivity of ligand binding to human dopamine D(2) and D(3) receptors expressed in Escherichia coli: clues for a constrained D(3) receptor structure.

Vanhauwe JF, Josson K, Luyten WH, Driessen AJ, Leysen JE.

J Pharmacol Exp Ther. 2000 Oct;295(1):274-83.

PMID:
10991990
47.

Effects of recent and reference antipsychotic agents at human dopamine D2 and D3 receptor signaling in Chinese hamster ovary cells.

Vanhauwe JF, Ercken M, van de Wiel D, Jurzak M, Leysen JE.

Psychopharmacology (Berl). 2000 Jul;150(4):383-90.

PMID:
10958079
48.

Quantitative autoradiographic distribution of gamma-hydroxybutyric acid binding sites in human and monkey brain.

Castelli MP, Mocci I, Langlois X, Gommerendagger W, Luyten WH, Leysen JE, Gessa GL.

Brain Res Mol Brain Res. 2000 May 31;78(1-2):91-9.

PMID:
10891588
49.

Binding of GDNF and neurturin to human GDNF family receptor alpha 1 and 2. Influence of cRET and cooperative interactions.

Cik M, Masure S, Lesage AS, Van Der Linden I, Van Gompel P, Pangalos MN, Gordon RD, Leysen JE.

J Biol Chem. 2000 Sep 8;275(36):27505-12.

50.

Reconstitution of the human 5-HT(1D) receptor-G-protein coupling: evidence for constitutive activity and multiple receptor conformations.

Brys R, Josson K, Castelli MP, Jurzak M, Lijnen P, Gommeren W, Leysen JE.

Mol Pharmacol. 2000 Jun;57(6):1132-41.

PMID:
10825383

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