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Items: 24

1.

Investigation of an 18F-labelled Imidazopyridotriazine for Molecular Imaging of Cyclic Nucleotide Phosphodiesterase 2A.

Schröder S, Wenzel B, Deuther-Conrad W, Teodoro R, Kranz M, Scheunemann M, Egerland U, Höfgen N, Briel D, Steinbach J, Brust P.

Molecules. 2018 Mar 2;23(3). pii: E556. doi: 10.3390/molecules23030556.

2.

Radiosynthesis and biological evaluation of the new PDE10A radioligand [18 F]AQ28A.

Wagner S, Teodoro R, Deuther-Conrad W, Kranz M, Scheunemann M, Fischer S, Wenzel B, Egerland U, Hoefgen N, Steinbach J, Brust P.

J Labelled Comp Radiopharm. 2017 Jan;60(1):36-48. doi: 10.1002/jlcr.3471. Epub 2016 Nov 29.

PMID:
27896836
3.

Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.

Wagner S, Scheunemann M, Dipper K, Egerland U, Hoefgen N, Steinbach J, Brust P.

Eur J Med Chem. 2016 Jan 1;107:97-108. doi: 10.1016/j.ejmech.2015.10.028. Epub 2015 Oct 19.

PMID:
26562545
4.

Synthesis, 18F-Radiolabelling and Biological Characterization of Novel Fluoroalkylated Triazine Derivatives for in Vivo Imaging of Phosphodiesterase 2A in Brain via Positron Emission Tomography.

Schröder S, Wenzel B, Deuther-Conrad W, Teodoro R, Egerland U, Kranz M, Scheunemann M, Höfgen N, Steinbach J, Brust P.

Molecules. 2015 May 26;20(6):9591-615. doi: 10.3390/molecules20069591.

5.

Large-scale mining for similar protein binding pockets: with RAPMAD retrieval on the fly becomes real.

Krotzky T, Grunwald C, Egerland U, Klebe G.

J Chem Inf Model. 2015 Jan 26;55(1):165-79. doi: 10.1021/ci5005898. Epub 2014 Dec 18.

PMID:
25474400
6.

Fluorine-containing 6,7-dialkoxybiaryl-based inhibitors for phosphodiesterase 10 A: synthesis and in vitro evaluation of inhibitory potency, selectivity, and metabolism.

Schwan G, Barbar Asskar G, Höfgen N, Kubicova L, Funke U, Egerland U, Zahn M, Nieber K, Scheunemann M, Sträter N, Brust P, Briel D.

ChemMedChem. 2014 Jul;9(7):1476-87. doi: 10.1002/cmdc.201300522. Epub 2014 Apr 11.

PMID:
24729456
7.

Discovery of triazines as potent, selective and orally active PDE4 inhibitors.

Gewald R, Grunwald C, Egerland U.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4308-14. doi: 10.1016/j.bmcl.2013.05.099. Epub 2013 Jun 10.

PMID:
23806553
8.

Phosphodiesterase 2 inhibitors promote axonal outgrowth in organotypic slice co-cultures.

Heine C, Sygnecka K, Scherf N, Berndt A, Egerland U, Hage T, Franke H.

Neurosignals. 2013;21(3-4):197-212. doi: 10.1159/000338020. Epub 2012 Aug 31.

9.

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.

Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076. Epub 2012 Jul 31.

PMID:
22902656
10.

Effect of PDE10A inhibitors on MK-801-induced immobility in the forced swim test.

Langen B, Dost R, Egerland U, Stange H, Hoefgen N.

Psychopharmacology (Berl). 2012 May;221(2):249-59. doi: 10.1007/s00213-011-2567-y. Epub 2011 Nov 16.

PMID:
22147257
11.

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.

Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ.

J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138. Epub 2011 Oct 11.

PMID:
21988093
12.

Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors.

Gewald R, Rueger C, Grunwald C, Egerland U, Hoefgen N.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6652-6. doi: 10.1016/j.bmcl.2011.09.065. Epub 2011 Sep 21.

PMID:
21983442
13.

5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiazepines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors.

Grunwald C, Kronbach C, Egerland U, Schindler R, Dieckmann R, Heinecke K, Höfgen N, Unverferth K.

Pharmazie. 2011 Feb;66(2):98-104.

PMID:
21434570
14.

Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.

Höfgen N, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Tremmel P, Pangalos MN, Marquis KL, Hage T, Harrison BL, Malamas MS, Brandon NJ, Kronbach T.

J Med Chem. 2010 Jun 10;53(11):4399-411. doi: 10.1021/jm1002793.

PMID:
20450197
15.

Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia.

Grauer SM, Pulito VL, Navarra RL, Kelly MP, Kelley C, Graf R, Langen B, Logue S, Brennan J, Jiang L, Charych E, Egerland U, Liu F, Marquis KL, Malamas M, Hage T, Comery TA, Brandon NJ.

J Pharmacol Exp Ther. 2009 Nov;331(2):574-90. doi: 10.1124/jpet.109.155994. Epub 2009 Aug 6.

PMID:
19661377
16.

New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity.

Lankau HJ, Unverferth K, Grunwald C, Hartenhauer H, Heinecke K, Bernöster K, Dost R, Egerland U, Rundfeldt C.

Eur J Med Chem. 2007 Jun;42(6):873-9. Epub 2007 Jan 12.

PMID:
17303289
17.

Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.

Grunwald C, Rundfeldt C, Lankau HJ, Arnold T, Höfgen N, Dost R, Egerland U, Hofmann HJ, Unverferth K.

J Med Chem. 2006 Mar 23;49(6):1855-66.

PMID:
16539371
18.

[Synthesis of substituted 6-phenylpyrazolo[3,4-d]pyrimidines with potential adenosin-A2A antagonistic activity].

Briel D, Aurich R, Egerland U, Unverferth K.

Pharmazie. 2005 Oct;60(10):732-5. German.

PMID:
16259118
19.

Characterization in rats of the anxiolytic potential of ELB139 [1-(4-chlorophenyl)-4-piperidin-1-yl-1,5-dihydro-imidazol-2-on], a new agonist at the benzodiazepine binding site of the GABAA receptor.

Langen B, Egerland U, Bernöster K, Dost R, Unverferth K, Rundfeldt C.

J Pharmacol Exp Ther. 2005 Aug;314(2):717-24. Epub 2005 Apr 28.

PMID:
15860576
20.

RNA-based drug screening using automated RNA purification and real-time RT-PCR1.

Ullmann S, Hage T, Draheim R, Egerland U, Oelmüller U, Brune K, Pahl A.

J Biomol Screen. 2004 Mar;9(2):95-102.

PMID:
15006132
22.

Refolding, purification, and characterization of human recombinant PDE4A constructs expressed in Escherichia coli.

Richter W, Hermsdorf T, Lilie H, Egerland U, Rudolph R, Kronbach T, Dettmer D.

Protein Expr Purif. 2000 Aug;19(3):375-83.

PMID:
10910728
23.

1,5-Disubstituted indazol-3-ols with anti-inflammatory activity.

Schindler R, Fleischhauer I, Höfgen N, Sauer W, Egerland U, Poppe H, Heer S, Szelenyi I, Kutscher B, Engel J.

Arch Pharm (Weinheim). 1998 Jan;331(1):13-21.

PMID:
9507697
24.

New 5-aminoacyl-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-ones with antiarrhythmic activity.

Poppe H, Kaverina NV, Lyskovzev VV, Egerland U, Sauer W, Lichoscherstow A, Rüger C, Skoldinow A.

Pharmazie. 1997 Nov;52(11):821-30.

PMID:
9399338

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