Zobrazeno 1 - 10 of 31 pro vyhledávání: '"Philip R. Tiller"'
1
Discovery of GlyT1 inhibitors with improved pharmacokinetic properties
Autor: Cyrille Sur, Scott E. Wolkenberg, Bennett Ma, David L. Williams, Gene G. Kinney, Doug J. Pettibone, Craig W. Lindsley, William H. Leister, David D. Wisnoski, Christopher R. Gibson, Philip R. Tiller, Sheri Smith, Julie A. O'Brien, Wei Lemaire, Marlene A. Jacobson, Stacey L. Polsky-Fisher, George D. Hartman, Zhijian Zhao
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:1492-1495
Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::931f930bc1ff290285ad6e77f0c71bb8
https://doi.org/10.1016/j.bmcl.2009.01.015
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2
Fractional mass filtering as a means to assess circulating metabolites in early human clinical studies
Autor: Thomas A. Baillie, Kevin P. Bateman, Philip R. Tiller, Sean Yu, Jose Castro-Perez, Yushin Kuo, Ian McIntosh
Publikováno v: Rapid Communications in Mass Spectrometry. 22:3510-3516
Recent changes in the regulatory environment have led to a need for new methods to assess circulating human drug metabolites in early clinical studies with respect to their potential toxicological impact. The specific goals of such studies are to det
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bb23754dfe5d31df82c23c07bf8003e3
https://doi.org/10.1002/rcm.3758
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3
A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral Models
Autor: Mark E. Duggan, Cyrille Sur, Marlene A. Jacobson, Craig W. Lindsley, Tsing-Bau Chen, David D. Wisnoski, Gene G. Kinney, Michelle K. Clements, Douglas J. Pettibone, Philip R. Tiller, Wei Lemaire, P. Jeffrey Conn, Maryann Burno, David L. Williams, Sheri Smith, Julie A. O'Brien, Denise J. Bickel
Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 313:199-206
We found that 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide (CDPPB) is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). In Chinese hamster ovary cells expressing human mGluR5, CDPPB p
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d62906d66536c68f6fbed712a8f57cee
https://doi.org/10.1124/jpet.104.079244
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4
Liquid chromatography/tandem mass spectrometric quantification with metabolite screening as a strategy to enhance the early drug discovery process
Autor: Philip R. Tiller, Leslie A. Romanyshyn
Publikováno v: Rapid Communications in Mass Spectrometry. 16:1225-1231
Throughput for early discovery drug metabolism studies can be increased with the concomitant acquisition of metabolite screening information and quantitative analysis using ultra-fast gradient chromatographic methods. Typical ultra-fast high-performa
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f854da707b6242eaef7a4cb8f90293ef
https://doi.org/10.1002/rcm.708
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5
Ultra-short columns and ballistic gradients: considerations for ultra-fast chromatographic liquid chromatographic–tandem mass spectrometric analysis
Autor: Philip R. Tiller, Leslie A. Romanyshyn
Publikováno v: Journal of Chromatography A. 928:41-51
Ultra-fast chromatographic separations has enabled fast chromatographic method development and rapid analysis for sample quantification. Decreasing over-all analytical time has become a factor of major importance for all aspects of drug discovery. Ho
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06f1135139f17290113b93ab4c7cf2fa
https://doi.org/10.1016/s0021-9673(01)01112-8
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6
Implications of matrix effects in ultra-fast gradient or fast isocratic liquid chromatography with mass spectrometry in drug discovery
Autor: Philip R. Tiller, Leslie A. Romanyshyn
Publikováno v: Rapid Communications in Mass Spectrometry. 16:92-98
In the analysis of biological samples it is important to reduce the risk of interferences from the matrix itself, other analytes, the dosing vehicle (commonly PEG), and from the MS/MS transitions used for the analysis. Rapid analysis is essential for
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8198269a7b4cd009cb37bb6d45e1c2e
https://doi.org/10.1002/rcm.544
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7
Ultra-fast gradient vs. fast isocratic chromatography in bioanalytical quantification by liquid chromatography/tandem mass spectrometry
Autor: Cornelis E. C. A. Hop, Antonio Pereira, Leslie A. Romanyshyn, Philip R. Tiller, Raul F. Alvaro
Publikováno v: Rapid Communications in Mass Spectrometry. 15:313-319
Liquid chromatography/tandem mass spectrometry (LC/MS/MS) methods developed for quantification using rapid (‘ballistic’) gradients on narrow bore, short HPLC columns have been previously described by this laboratory. This paper compares the fast
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c8db337588e1bd66709eae758867b30
https://doi.org/10.1002/rcm.229
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8
Automated strategies for obtaining standardized collisionally induced dissociation spectra on a benchtop ion trap mass spectrometer
Autor: Jae C. Schwartz, Philip R. Tiller, Michael W. Senko, Linda L. Lopez
Publikováno v: Rapid Communications in Mass Spectrometry. 13:663-668
An automated method for obtaining standardized collisionally induced dissociation (CID) spectra using two novel ion activation techniques on a quadrupole ion trap mass spectrometer is described. This strategy simultaneously produces optimal CID spect
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::35c57621ba631ed3c5434495148f8658
https://doi.org/10.1002/(sici)1097-0231(19990430)13:8<663::aid-rcm538>3.0.co
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9
Automated identification of isotopically labeled pesticides and metabolites by intelligent ‘real time’ liquid chromatography tandem mass spectrometry using a bench-top ion trap mass spectrometer
Autor: Dieter M. Drexler, Frederick Q. Bramble, Jae C. Schwartz, Philip R. Tiller, Sibylle M. Wilbert
Publikováno v: Rapid Communications in Mass Spectrometry. 12:1501-1507
A screening method was developed to specifically detect and identify isotopically labeled compounds automatically in real-time using a HPLC/ion trap mass spectrometer utilizing newly developed isotopic pattern recognition software. The ion trap mass
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a1c5b2a888254d1942c1edf34ea52921
https://doi.org/10.1002/(sici)1097-0231(19981030)12:20<1501::aid-rcm355>3.0.co
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10
‘Intelligent’ fraction collection to improve structural characterization by mass spectrometry
Autor: Philip R. Tiller, Dieter M. Drexler
Publikováno v: Rapid Communications in Mass Spectrometry. 12:895-900
A method to collect high performance liquid chromatography (HPLC) fractions in an automated manner based upon mass spectrometric data is described. The use of modern ion-trap mass spectrometry affords molecular mass, structural data and the collectio
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4df693bb968040236393c090f474d531
https://doi.org/10.1002/(sici)1097-0231(19980715)12:13<895::aid-rcm246>3.0.co
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