Výsledky vyhledávání - "Larry W. Hardy"

In vitro and in vivo pharmacological characterization of dasotraline, a dual dopamine and norepinephrine transporter inhibitor in vivo

Autor: Rudy Schreiber, Una Campbell, Maria S. Quinton, Larry W. Hardy, Q. Kevin Fang, Robert Lew

Publikováno v: Biomedicine & Pharmacotherapy, 153:113359. Elsevier Masson

Inhibitors of dopamine transporters (DAT), norepinephrine transporters (NET) and serotonin transporters (SERT) are effective treatments for neuropsychiatric diseases. Dasotraline [(1R,4 S)- 4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydro-1-naphthalenamine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba10d6cd2b0764ee878f02f6869cdff4
https://cris.maastrichtuniversity.nl/en/publications/8618a28d-0e35-41c8-bd13-853dab205e89

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Functional deficit in hippocampal activity during fear extinction recall in the single prolonged-stress model of PTSD in male rats

Autor: Surabhi Nair, Mohammed Q. Qutaish, Noel Aaron Powell, Dima Chaar, Ali Ghayoor, Jack Heimann, Jesse J. Winters, Jenna M. Sullivan, Larry W. Hardy, Jon Oscherwitz, Israel Liberzon, Lauren E. Chaby, Ildiko Polyak, Elizabeth Rodriguez

Publikováno v: Behavioural Brain Research. 396:112902

To interrogate whether altered function of the hippocampal-mPFC circuit underlies the deficit in fear extinction recall in rats subjected to single-prolonged stress (SPS), changes in brain region-specific metabolic rate were measured in male rats (co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02b3db76315ba0485690508e9a6816e3
https://doi.org/10.1016/j.bbr.2020.112902

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Synthesis and Pharmacological Characterization of Bicyclic Triple Reuptake Inhibitor 3-Aryl Octahydrocyclopenta[c]pyrrole Analogues

Autor: Michael C. Hewitt, Larry W. Hardy, Una Campbell, Liming Shao, Scott Christopher Malcolm, Mark A. Varney, Zhi-Dong Jiang, Fengjiang Wang, Kerry L. Spear, Sharon Rae Engel, Rudy Schreiber, Nancy A. Spicer, Jianguo Ma

Publikováno v: Journal of Medicinal Chemistry. 54:5283-5295

The present work expands the chemical space known to offer potent inhibition of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) and discloses novel bicyclic octahydrocyclopenta[c]pyrrole and octahydr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aed0afc224aeeeca77078f581960d256
https://doi.org/10.1021/jm101312a

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Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor

Autor: Sharon Rae Engel, Larry W. Hardy, Michael C. Hewitt, Kerry L. Spear, John Emmerson Campbell, Rudy Schreiber, Liming Shao, Jianguo Ma, Una Campbell, Fengjiang Wang, Nancy A. Spicer, Scott Christopher Malcolm, Mark A. Varney

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:1438-1441

Novel chiral cyclohexylaryl amines were developed with potent reuptake inhibition against the serotonin, norepinephrine and dopamine transporters and activity at 10 and 30 mpk PO in the mouse tail suspension test. Prototype compound 31 (SERT, NET, DA

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7042369b79aee5fac51b2c9ee2e85dad
https://doi.org/10.1016/j.bmcl.2011.01.016

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Design, Synthesis, and Structure−Activity Relationships of Novel Bicyclic Azole-amines as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5

Autor: Tao Hu, Jun Wang, Maria S. Quinton, Kerry L. Spear, Zhiqiang Huang, M. A. Orsini, Douglas F. Burdi, Lei Fan, Michel Detheux, Zihong Guo, Chengde Wu, Robert Lew, Larry W. Hardy, Rachel Hunt

Publikováno v: Journal of Medicinal Chemistry. 53:7107-7118

A novel series of diaryl bicyclic azole-amines that are potent selective negative modulators of metabotropic glutamate receptor 5 (mGluR5) were identified through rational design. An initial hit compound 5a of modest potency (IC(50) = 1.2 μM) was sy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bc0a278fd2a021f16b64c35d492ba3c
https://doi.org/10.1021/jm100736h

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Affinity Ligand Selection from a Library of Small Molecules: Assay Development, Screening, and Application

Autor: Lakshmi D. Saraswat, Rama Bhikhabhai, Larry W. Hardy, Huiyun Zhang, Annika Bergenstråhle, Rolf Haglund, Steven L. Gallion, Simon S. Jones, Charlotte Brink

Publikováno v: Biotechnology Progress. 21:300-308

A facile and cost-effective process for screening synthetic libraries for an affinity ligand is described. A high throughput 96-well plate filtration method was designed to screen both discrete compounds and mixtures of compounds attached to a solid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f35c5fb4db2117fb1256c842d9ad93f
https://doi.org/10.1021/bp040019w

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Exploratory Biomarker Study of the Triple Reuptake Inhibitor SEP-432 Compared to the Dual Reuptake Inhibitor Duloxetine in Healthy Normal Subjects

Autor: Hong Ding, Jahnavi Kharidia, Cynthia Zamora, Todd Grinnell, Larry W. Hardy, Yu-Luan Chen, Peter Bieck, Neal R. Cutler, Mark Versavel, Michael Sullivan, John J. Sramek

Publikováno v: CNS neurosciencetherapeutics. 22(5)

SUMMARY Introduction: SEP-432 is a triple monoamine reuptake inhibitor of norepinephrine (NE), serotonin (5-HT), and dopamine (DA), based on in vitro binding studies. We sought evi- dence that SEP-432 engages these monoamine systems by measuring conc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ab376d2f424abb6d156a3ea1f337aaf
https://pubmed.ncbi.nlm.nih.gov/26849844

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The multiple orthogonal tools approach to define molecular causation in the validation of druggable targets

Autor: Norton P. Peet, Larry W Hardy

Publikováno v: Drug Discovery Today. 9:117-126

Many genetic (gene deletion, interruption or mutation), epigenetic (such as antisense or small interfering RNA) and immunological methods are being applied in 'high-throughput target validation' studies of the novel potential targets arising from who

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aa44f0df13b2eb5252a2dc6efdd7cf0
https://doi.org/10.1016/s1359-6446(03)02969-6

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Structure‐Based Drug Design

Autor: Donald J. Abraham, Larry W. Hardy, Martin K. Safo

Publikováno v: Burger's Medicinal Chemistry and Drug Discovery

Structure-based drug design is achievable by exploiting the three-dimensional information intrinsic in structural models of proteins that are involved in human disease. Many other tools (biochemistry, cellular and whole-animal biology, organic synthe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0deaf68eea3483d5dc06ca29d930020d
https://doi.org/10.1002/0471266949.bmc110

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Drug Absorption, Distribution, and Elimination

Autor: Beatrice Y. T. Perotti, Leslie Z. Benet, Larry W. Hardy

Publikováno v: Burger's Medicinal Chemistry and Drug Discovery

The chapter provides basic quantitative explanations of practical pharmacokinetic concepts that are key to understanding how drugs enter and depart from the body. The parameters that are discussed include hepatic and renal clearance, bioavailability,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::162fa5b9e7ad7712c5ea5dee9774d6cd
https://doi.org/10.1002/0471266949.bmc037

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