Výsledky vyhledávání - "B. E. Cantrell"

Importance of Phenolic Address Groups in Opioid Kappa Receptor Selective Antagonists

Autor: D. M. Zimmerman, S. W. Mascarella, Richard B. Rothman, Carroll Fi, Jim A. Thomas, B. E. Cantrell, Christina M. Dersch, Scott E. Fix

Publikováno v: Journal of Medicinal Chemistry. 47:1070-1073

In vitro characterization and comparison of JDTic, its dehydroxy analogue and nor-BNI, and its dehydroxy analogue demonstrates that the N-substituted 3,4-dimethyl-(3-hydroxyphenyl)piperidine-derived antagonist, JDTic, relies more heavily on its pheno

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0b24556bf4151aa3a01efb2f3da289f
https://doi.org/10.1021/jm030467v

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Discovery of an Opioid κ Receptor Selective Pure Antagonist from a Library of N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)morphans

Autor: Jim A. Thomas, Robert N. Atkinson, D. M. Zimmerman, Noelle Vinson, Richard B. Rothman, Christina M. Dersch, Kenneth M. Gigstad, Nivedita Namdev, Scott E. Fix, Jason P. Burgess, Heng Xu, F. I. Carroll, S. W. Mascarella, B. E. Cantrell

Publikováno v: Journal of Medicinal Chemistry. 45:3524-3530

A library of compounds biased toward opioid receptor antagonist activity was prepared by incorporating N-phenylpropyl-4beta-methyl-5-(3-hydroxyphenyl)morphans as the core scaffold using simultaneous solution phase synthetic methodology. From this lib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09cf41f988f4d576a71855a6c19e3670
https://doi.org/10.1021/jm020084h

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Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity

Autor: Frank I. Carroll, S. W. Mascarella, Richard B. Rothman, YF Lu, Heng Xu, D. M. Zimmerman, Noelle Vinson, James B. Thomas, Scott E. Fix, Robert N. Atkinson, B. E. Cantrell, Christina M. Dersch

Publikováno v: Journal of medicinal chemistry. 44(17)

A structurally novel opioid kappa receptor selective ligand has been identified. This compound, (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JD

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b717ad937b82498698cf306c09898aab
https://pubmed.ncbi.nlm.nih.gov/11495579

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Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine

Autor: Julie B. Cooper, James B. Thomas, S. W. Mascarella, John S. Partilla, F. I. Carroll, B. E. Cantrell, Michael J. Fall, Christina M. Dersch, Heng Xu, K. B. Mccullough, D. M. Zimmerman, Richard B. Rothman

Publikováno v: Journal of medicinal chemistry. 41(26)

A three-component library of compounds was prepared in parallel using multiple simultaneous solution-phase synthetic methodology. The compounds were biased toward opioid receptor antagonist activity by incorporating (+)-(3R,4R)-dimethyl-4-(3-hydroxyp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00372543f065638fbbd522662137afc7
https://pubmed.ncbi.nlm.nih.gov/9857089

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N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists

Autor: Richard B. Rothman, John S. Partilla, J. L. Flippen-Anderson, D. M. Zimmerman, S. W. Mascarella, B. E. Cantrell, James B. Thomas, Christina M. Dersch, C. F. George, Frank I. Carroll, Xiaoling Zheng

Publikováno v: Journal of medicinal chemistry. 41(21)

The inhibition of radioligand binding and [35S]GTPgammaS functional assay data for N-methyl- and N-phenethyl-9beta-methyl-5-(3-hydroxyphenyl)morphans (5b and 5c) show that these compounds are pure antagonists at the micro, delta, and kappa opioid rec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83c2dc2fd0c8bb13a78d71f2a63fdd9e
https://pubmed.ncbi.nlm.nih.gov/9767649

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Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists

Autor: S. W. Mascarella, Heng Xu, Frank I. Carroll, James B. Thomas, John S. Partilla, Richard B. Rothman, K. B. Mccullough, D. M. Zimmerman, B. E. Cantrell, Christina M. Dersch

Publikováno v: Journal of medicinal chemistry. 41(11)

A study of the binding site requirements associated with the N-substituent of (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine (4) derivatives was undertaken using a set of rigid vs flexible N-substituents. The study showed that compounds 7-9 beari

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4e7bf91f869cc33995010cbe7984a05
https://pubmed.ncbi.nlm.nih.gov/9599247

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