Steven M. Grauer

Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain

Gregory L. Adams, Parul S. Pall, Steven M. Grauer, Xiaoping Zhou et autres

Inhibitor cystine knot peptides, derived from venom, have evolved to block ion channel function but are often toxic when dosed at pharmacologically relevant levels in vivo . The article describes the design of analogues of ProTx-II that safely display systemic in vivo …

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Antinociceptive effects of potent, selective and brain penetrant muscarinic M4 positive allosteric modulators in rodent pain models

Steven M. Grauer, Raul Sanoja, Dominic Poulin, Harunor Rashid et autres

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MitoPark mice, an animal model of Parkinson’s disease, show enhanced prepulse inhibition of acoustic startle and no loss of gating in response to the adenosine A2A antagonist SCH 412348

Steven M. Grauer, Robert A. Hodgson, Lynn A. Hyde

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Preclinical assessment of an adjunctive treatment approach for cognitive impairment associated with schizophrenia using the alpha7 nicotinic acetylcholine receptor agonist WYE-103914/SEN34625

Karen L. Marquis, Thomas A. Comery, Flora Jow, Rachel L. Navarra et autres

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The Synthesis and Biological Evaluation of Quinolyl-piperazinyl Piperidines as Potent Serotonin 5-HT1AAntagonists

Wayne E. Childers, Lisa M. Havran, Magda Asselin, James Bicksler et autres

As part of an effort to identify 5-HT(1A) antagonists that did not possess typical arylalkylamine or keto/amido-alkyl aryl piperazine scaffolds, prototype compound 10a was identified from earlier work in a combined 5-HT(1A) antagonist/SSRI program. This quinolyl-piperazinyl piperidine analogue displayed potent, selective 5-HT(1A) …

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Phosphodiesterase 11A in brain is enriched in ventral hippocampus and deletion causes psychiatric disease-related phenotypes

Michy P. Kelly, Sheree F. Logue, Julie Brennan, Jonathon P. Day et autres

Phosphodiesterase 11A (PDE11A) is the most recently identified family of phosphodiesterases (PDEs), the only known enzymes to break down cyclic nucleotides. The tissue expression profile of this dual specificity PDE is controversial, and little is understood of its biological function, particularly in …

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COMPOUND 1, A POTENT AND SELECTIVE DAO INHIBITOR, DEMONSTRATES EFFICACY IN SEVERAL PRECLINICAL ANIMAL MODELS OF SCHIZOPHRENIA

Steven M. Grauer, Paul Dollings, Michael Popiolek, Mark Pausch et autres

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WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: A Novel Dopamine D2 Receptor Partial Agonist/Serotonin Reuptake Inhibitor with Preclinical Antipsychotic-Like and Antidepressant-Like Activity

Julie Brennan, Radka Graf, Steven M. Grauer, Rachel L. Navarra et autres

The orphan GPCR, GPR88, modulates function of the striatal dopamine system: A possible therapeutic target for psychiatric disorders?

Sheree F. Logue, Steven M. Grauer, Janet Paulsen, Radka Graf et autres

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Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia

David P. Rotella, Geraldine McFarlane, Alexander Greenfield, Cristina Grosanu et autres

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Phosphodiesterase 10A Inhibitor Activity in Preclinical Models of the Positive, Cognitive, and Negative Symptoms of Schizophrenia

Steven M. Grauer, Virginia Pulito, Rachel L. Navarra, Michy P. Kelly et autres

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Receptor and behavioral pharmacology of WAY-267464, a non-peptide oxytocin receptor agonist

Robert H. Ring, Lee E. Schechter, Sarah K. Leonard, Jason M. Dwyer et autres

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