Mark H Pausch
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Explore the profile of Mark H Pausch including associated specialties, affiliations and a list of published articles.
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18
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1471
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Recent Articles
1.
Kuduk S, Skudlarek J, DiMarco C, Bruno J, Pausch M, OBrien J, et al.
Bioorg Med Chem Lett
. 2015 May;
25(12):2488-92.
PMID: 25981685
Antagonism of orexin receptors has shown clinical efficacy as a novel paradigm for the treatment of insomnia and related disorders. Herein, molecules related to the dual orexin receptor antagonist filorexant...
2.
Popiolek M, Ross J, Charych E, Chanda P, Gundelfinger E, Moss S, et al.
J Biol Chem
. 2011 Jun;
286(33):28867-28875.
PMID: 21700703
Schizophrenia is a highly heritable neuropsychiatric disorder affecting ∼1% of the world's population. Linkage and association studies have identified multiple candidate schizophrenia susceptibility genes whose functions converge on the glutamatergic...
3.
Ajit S, Pausch M, Kennedy J, Kaftan E
J Biomed Biotechnol
. 2010 Oct;
2010.
PMID: 20936132
MrgD, a member of the Mas-related gene family, is expressed exclusively in small diameter IB4(+) neurons in the dorsal root ganglion. This unique expression pattern, the presence of a single...
4.
Yan Y, Zhou P, Rotella D, Feenstra R, Kruse C, Reinders J, et al.
Bioorg Med Chem Lett
. 2010 Mar;
20(9):2983-6.
PMID: 20347298
A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D(2) ligands to prepare a series...
5.
Zhang J, Kowal D, Nawoschik S, Dunlop J, Pausch M, Peri R
Assay Drug Dev Technol
. 2009 Nov;
8(1):106-13.
PMID: 19922239
The 5-hydroxytryptamine 2C (5-HT(2C)) receptor is a member of the serotonin 5-HT(2) subfamily of G-protein-coupled receptors signaling predominantly via the phospholipase C (PLC) pathway. Stimulation of phosphoinositide (PI) hydrolysis upon...
6.
Brennan J, Graf R, Grauer S, Navarra R, Pulicicchio C, Hughes Z, et al.
J Pharmacol Exp Ther
. 2009 Oct;
332(1):190-201.
PMID: 19828876
The preclinical characterization of WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one] is described. In vitro binding and functional studies revealed highest affinity to the D(2) receptor (D(2L) K(i), 4.0 nM) and serotonin transporter (K(i), 7.1...
7.
Rotella D, McFarlane G, Greenfield A, Grosanu C, Robichaud A, Aldrin Denny R, et al.
Bioorg Med Chem Lett
. 2009 Sep;
19(19):5552-5.
PMID: 19720528
A 5-fluoro-tetrahydrocarbazole serotonin reuptake inhibitor (SRI) building block was combined with a variety of linkers and dopamine D2 receptor ligands in an attempt to identify potent D2 partial agonist/SRI molecules...
8.
Heinrich J, Butera J, Carrick T, Kramer A, Kowal D, Lock T, et al.
Eur J Pharmacol
. 2009 Jan;
605(1-3):53-6.
PMID: 19168056
In functional assay assessments using the five muscarinic receptor subtypes, a second generation of muscarinic M(1)-preferring receptor agonists [AC-42 (1), AC-260584 (2), 77-LH-28-1 (3) and LY-593039 (4)] was shown to...
9.
Fan Y, Lai M, Sullivan K, Popiolek M, Andree T, Dollings P, et al.
Bioorg Med Chem Lett
. 2008 Oct;
18(21):5789-91.
PMID: 18849166
We identified small molecule NTS1R agonist compounds through virtual screening of the corporate database using a ROCS approach that searches multi-conformer representations efficiently. As a starting point for the ROCS...
10.
Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, et al.
J Pharmacol Exp Ther
. 2008 Aug;
327(3):827-39.
PMID: 18753411
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor subtype 5 (mGlu5) enhance N-methyl-d-aspartate receptor function and may represent a novel approach for the treatment of schizophrenia. ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]oxadiazol-5-yl]-piperidin-1-yl}-methanone], a recently...