B
B. E. Cantrell
Researcher at Research Triangle Park
Publications - 9
Citations - 433
B. E. Cantrell is an academic researcher from Research Triangle Park. The author has contributed to research in topics: JDTic & Opioid receptor. The author has an hindex of 8, co-authored 9 publications receiving 422 citations.
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Journal ArticleDOI
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
James B. Thomas,Robert N. Atkinson,Richard B. Rothman,Scott E. Fix,S. W. Mascarella,Noelle Vinson,Heng Xu,Christina M. Dersch,YF Lu,B. E. Cantrell,D. M. Zimmerman,Frank I. Carroll +11 more
TL;DR: A structurally novel opioid kappa receptor selective ligand has been identified and demonstrated high affinity and highly potent and selective kappa antagonism in the [(35)S]GTP-gamma-S assay using cloned opioid receptors.
Journal ArticleDOI
Identification of (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 as a novel potent and selective opioid kappa receptor antagonist.
James B. Thomas,Robert N. Atkinson,Noelle Vinson,Jennifer L. Catanzaro,Carin Perretta,Scott E. Fix,S. W. Mascarella,Richard B. Rothman,Heng Xu,Christina M. Dersch,B. E. Cantrell,D. M. Zimmerman,Frank I. Carroll +12 more
TL;DR: The results suggest that, like other kappa opioid antagonists such as nor-BNI and GNTI, JDTic requires a second basic amino group to express potent and selective kappa antagonist activity in the [(35)S]GTPgammaS functional assay.
Journal ArticleDOI
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.
Paul L. Ornstein,D. M. Zimmerman,Macklin Brian Arnold,Thomas J. Bleisch,B. E. Cantrell,Richard Lee Simon,Hamideh Zarrinmayeh,Baker,Mary Gates,Joseph P. Tizzano,David Bleakman,Allan Mandelzys,K.R Jarvie,Ken H. Ho,Michele Deverill,Rajender Kamboj +15 more
Journal ArticleDOI
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine
James B. Thomas,Michael J. Fall,Julie B. Cooper,Richard B. Rothman,S. W. Mascarella,Heng Xu,John S. Partilla,Christina M. Dersch,K. B. Mccullough,B. E. Cantrell,D. M. Zimmerman,F. I. Carroll +11 more
TL;DR: According to its ability to inhibit agonist stimulated binding of [35S]GTPgammaS at all three opioid receptors, compound 8 behaves as a mu/kappa opioid receptor pure antagonist with negligible affinity for the delta receptor.
Journal ArticleDOI
Investigation of the N-Substituent Conformation Governing Potency and μ Receptor Subtype-Selectivity in (+)-(3R,4R)-Dimethyl-4-(3-hydroxyphenyl)- piperidine Opioid Antagonists
James B. Thomas,S. W. Mascarella,Richard B. Rothman,John S. Partilla,Heng Xu,K. B. Mccullough,Christina M. Dersch,B. E. Cantrell,D. M. Zimmerman,Frank I. Carroll +9 more
TL;DR: It is found that free rotation of the phenyl ring is necessary for high affinity binding and mu receptor subtype selectivity as the planar N-substituted thianaphthylmethyl and benzofuranylmethyl compounds 13 and 14 had significantly lower binding affinities.