Research Topics
| Liming ShaoSummaryAffiliation: Sepracor Inc Country: USA Publications
| Collaborators |
Detail Information
Publications
Derivatives of tramadol for increased duration of effectLiming Shao
Sepracor Inc, 84 Waterford Drive, Marlborough, MA 01752, USA
Bioorg Med Chem Lett 16:691-4. 2006..Tramadol is a centrally acting opioid analgesic structurally related to codeine and morphine. Analogs of tramadol with deuterium-for-hydrogen replacement at metabolically active sites were prepared and evaluated in vitro and in vivo...- In vitro and in vivo evaluation of O-alkyl derivatives of tramadolLiming Shao
Sepracor Inc, Medicinal Chemistry, 84 Waterford Drive, Marlborough, MA 01752, USA
Bioorg Med Chem Lett 18:1674-80. 2008..O-Alkyl, N-desmethyl, and non-phenol containing derivatives of tramadol were synthesized to probe their effect on metabolic stability and both in vitro and in vivo potency... - mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I)Liming Shao
Sepracor Inc, 84 Waterford Drive, Marlborough, MA 01752, USA
Bioorg Med Chem Lett 19:5679-83. 2009..Novel compounds were prepared that united the pharmacologies of the mu-opioid tramadol with the 5-HT4 agonists metoclopramide and norcisapride. The synthesis, chiral separation and in vitro activity of the new compounds is described... - The kinetic isotope effect in the search for deuterated drugsLiming Shao
Discovery and Early Clinical Research, Sepracor Inc, Marlborough, Massachusetts, USA
Drug News Perspect 23:398-404. 2010..Specific examples of compounds from the Concert and Auspex pipelines are also analyzed and the pros and cons of their approach are discussed... - Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitorsLiming Shao
Discovery and Early Clinical Research, Sepracor Inc, 84 Waterford Drive, Marlborough, MA 01752, USA
Bioorg Med Chem 19:663-76. 2011..The detailed synthesis and in vitro activity and ADME profile of compounds is described, which represent a previously undisclosed triple reuptake inhibitor chemotype... - Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitorLiming Shao
Discovery and Early Clinical Research, Sunovion Pharmaceuticals Inc, Marlborough, MA 01752, USA
Bioorg Med Chem Lett 21:1434-7. 2011..Prototype compound 31 (SERT, NET, DAT IC(50) ? 1, 21, 28 nM) was highly brain penetrant, had minimal CYP and hERG inhibition, and represents a previously undisclosed architecture with potential for treatment of major depressive disorder... - Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitorLiming Shao
Discovery and Early Clinical Research, Sunovion Pharmaceuticals Inc, Marlborough, MA 01752, USA
Bioorg Med Chem Lett 21:1438-41. 2011..Optimized compounds 1 (SERT, NET, DAT, IC(50)=169, 85, 21 nM) and 42 (SERT, NET, DAT IC(50)=34, 295, 90 nM) were highly brain penetrant, active in vivo in the mouse tail suspension test at 30 mpk po and were not general motor stimulants... - Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analoguesLiming Shao
Discovery and Early Clinical Research, Sunovion Pharmaceuticals, Marlborough, Massachusetts 01752, United States
J Med Chem 54:5283-95. 2011..Moderate in vitro cytochrome P450 (CYP) and potassium ion channel Kv11.1 (hERG) inhibition were uncovered as potential liabilities for the chemical series... - Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitorLiming Shao
Discovery and Early Clinical Research, Sunovion Pharmaceuticals Inc, 84 Waterford Drive, Marlborough, MA 01752, USA
Bioorg Med Chem Lett 21:520-3. 2011..1 (hERG) inhibition and synthetic accessibility. The detailed synthesis and in vitro activity and ADME profile of the compounds is described, which represent a previously undisclosed dual reuptake inhibitor chemotype...