Výsledky vyhledávání - "Brett Janosky"

Relationship between Passive Permeability, Efflux, and Predictability of Clearance from In Vitro Metabolic Intrinsic Clearance

Autor: Sindhura Ganga, April Chen, Loren Berry, Adria Colletti, Liyue Huang, Jonathan Roberts, Min-Hwa Jasmine Lin, Brett Janosky

Publikováno v: Drug Metabolism and Disposition. 38:223-231

In vitro intrinsic metabolic clearance (CL(int)) is used routinely for compound selection in drug discovery; however, in vitro CL(int) often underpredicts in vivo clearance (CL). Forty-one proprietary compounds and 16 marketed drugs were selected to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f10295474d8955d00668b24e8f8dc97
https://doi.org/10.1124/dmd.109.029066

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Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant α4β2 nicotinic acetylcholine receptor potentiators

Autor: Katrina S. Woodin, Brian K. Albrecht, Virginia Berry, Alessandro Boezio, Liyue Huang, Kristie Clarkin, Jean-Christophe Harmange, Hung Q. Nguyen, Markus Hierl, Stephanie Springer, Annika B. Malmberg, Johannes Knop, Stefan I. McDonough, Jeff S. McDermott, Wenhong Guo, Brett Janosky, Daniel Waldon, Lei Cao

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:5209-5212

The discovery of a series of small molecule alpha4beta2 nAChR potentiators is reported. The structure-activity relationship leads to potent compounds selective against nAChRs including alpha3beta2 and alpha3beta4 and optimized for CNS penetrance. Com

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d75cc6e79c24998288a86bfd81a77fe5
https://doi.org/10.1016/j.bmcl.2008.08.080

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Differential role of P-glycoprotein and breast cancer resistance protein in drug distribution into brain, CSF and peripheral nerve tissues in rats

Autor: Min-Hwa Jasmine Lin, Brett Janosky, Liyue Huang, Jonathan Roberts, Xingwen Li

Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 45(6)

1. This study was designed to evaluate how the absence of P-glycoprotein (Pgp, Mdr1a), breast cancer-resistance protein (Bcrp, Abcg2) or both affects drug distribution into sciatic nerves, brain and cerebrospinal fluid (CSF) in rats. 2. Pgp substrate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c28814bcb1afc76299ff038b2fdf2732
https://pubmed.ncbi.nlm.nih.gov/25539457

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Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain

Publikováno v: Journal of medicinal chemistry. 54(13)

Clinical human genetic studies have recently identified the tetrodotoxin (TTX) sensitive neuronal voltage gated sodium channel Nav1.7 (SCN9A) as a critical mediator of pain sensitization. Herein, we report structure-activity relationships for a novel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0554d821ede56752ff72b8f427a167f
https://pubmed.ncbi.nlm.nih.gov/21634377

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In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases

Autor: Wei-Jian Pan, Loren Berry, Min-Hwa Jasmine Lin, Brett Janosky, Liyue Huang, Zhiyang Zhao, Xuhai Be, Mary C. Wells, Earl Moore

Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 41(5)

AMG 900 is a small molecule being developed as an orally administered, highly potent, and selective pan-aurora kinase inhibitor. The aim of the investigations was to characterize in vitro and in vivo pharmacokinetic (PK) properties of AMG 900 in prec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fd110ffb02ce0a8a935c3d3a5146df1
https://pubmed.ncbi.nlm.nih.gov/21294625

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Corrigendum to 'Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2' [Bioorg. Med. Chem. Lett. 18 (2008) 4267–4274]

Autor: Erin F. DiMauro, John L. Buchanan, Alan Chen, Renee Emkey, Stephen A. Hitchcock, Liyue Huang, Ming Y. Huang, Brett Janosky, Josie H. Lee, Xingwen Li, Matthew W. Martin, Susan A. Tomlinson, Ryan D. White, Xiao Mei Zheng, Vinod F. Patel, Robert T. Fremeau

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:284

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f7af9a4cd918a8c28ec7fb4b02d0a29f
https://doi.org/10.1016/j.bmcl.2008.07.131

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Erratum to 'Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2' [Bioorg. Med. Chem. Lett. 18 (2008) 4267–4274]

Autor: Xingwen Li, Ryan White, Susan A. Tomlinson, Brett Janosky, Erin F. DiMauro, Stephen Hitchcock, Xiao Mei Zheng, Renee Emkey, Josie H. Lee, Ming Y. Huang, John L. Buchanan, Alan Chen, Vinod F. Patel, Robert T. Fremeau, Matthew W. Martin, Liyue Huang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:5156

Corrigendum to ‘‘Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2” [Bioorg. Med. Chem. Lett. 18 (2008) 4267–4274] Erin F. DiMauro *, John L. Buchanan ,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dd00dff5b85d6fc0ce7db73d0d5db421
https://doi.org/10.1016/j.bmcl.2008.08.049

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