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Structure of the human κ-opioid receptor in complex with JDTic.
Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V, Stevens RC. Wu H, et al. Among authors: mascarella sw. Nature. 2012 Mar 21;485(7398):327-32. doi: 10.1038/nature10939. Nature. 2012. PMID: 22437504 Free PMC article.
Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues 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 (JDTic).
Cueva JP, Cai TB, Mascarella SW, Thomas JB, Navarro HA, Carroll FI. Cueva JP, et al. Among authors: mascarella sw. J Med Chem. 2009 Dec 10;52(23):7463-72. doi: 10.1021/jm900756t. J Med Chem. 2009. PMID: 19954245 Free PMC article.
Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.
Kormos CM, Gichinga MG, Maitra R, Runyon SP, Thomas JB, Brieaddy LE, Mascarella SW, Navarro HA, Carroll FI. Kormos CM, et al. Among authors: mascarella sw. J Med Chem. 2014 Sep 11;57(17):7367-81. doi: 10.1021/jm5008177. Epub 2014 Aug 25. J Med Chem. 2014. PMID: 25133923 Free PMC article.
Analogues 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 (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.
Runyon SP, Brieaddy LE, Mascarella SW, Thomas JB, Navarro HA, Howard JL, Pollard GT, Carroll FI. Runyon SP, et al. Among authors: mascarella sw. J Med Chem. 2010 Jul 22;53(14):5290-301. doi: 10.1021/jm1004978. J Med Chem. 2010. PMID: 20568781 Free PMC article.
Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)- N-[1 R)-1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic).
Kormos CM, Ondachi PW, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI. Kormos CM, et al. Among authors: mascarella sw. J Med Chem. 2018 Sep 13;61(17):7546-7559. doi: 10.1021/acs.jmedchem.8b00674. Epub 2018 Aug 29. J Med Chem. 2018. PMID: 30032602 Free PMC article.
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.
Thomas JB, Atkinson RN, Vinson NA, Catanzaro JL, Perretta CL, Fix SE, Mascarella SW, Rothman RB, Xu H, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI. Thomas JB, et al. Among authors: mascarella sw. J Med Chem. 2003 Jul 3;46(14):3127-37. doi: 10.1021/jm030094y. J Med Chem. 2003. PMID: 12825951
Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)-7-Hydroxy- N-[(1 S)-2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic).
Ondachi PW, Kormos CM, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI. Ondachi PW, et al. Among authors: mascarella sw. J Med Chem. 2018 Sep 13;61(17):7525-7545. doi: 10.1021/acs.jmedchem.8b00673. Epub 2018 Aug 29. J Med Chem. 2018. PMID: 30117738 Free PMC article.
80 results