Zobrazeno 1 - 10
of 153
pro vyhledávání: '"Louis S. Harris"'
Autor:
Ian Derrick, Louis S. Harris, Jillian Helen Broadbear, Stephen M. Husbands, John R. Traynor, James H. Woods, John W. Lewis, Humphrey A. Moynihan, Benjamin M. Greedy, Mark P. Thomas, Mario D. Aceto, Lauren C. Purington
Publikováno v:
Journal of Medicinal Chemistry
We have previously shown that cinnamoyl derivatives of 14β-amino-17-cyclopropylmethyl-7,8-dihydronormorphinone and 7α-aminomethyl-6,14-endoethanonororipavine have pronounced pseudoirreversible μ opioid receptor (MOR) antagonism. The present commun
Autor:
Olivier George, Robert E. Vann, Louis S. Harris, Jenny L. Wiley, F. I. Carroll, Marc R. Azar, D.M. Walentiny, M. I. Damaj, George F. Koob, K.M. Tobey
Publikováno v:
Psychopharmacology. 223:159-168
Alleviating addiction to tobacco products could prevent millions of deaths. Investigating novel compounds selectively targeting α4β2 nAChRs hypothesized to have a key role in the rewarding effects of nicotine may be a useful approach for future tre
Autor:
Andrew J. Kwilasz, M.D. Aceto, Robert E. Vann, S.L. Lobe, B. Kipps, Louis S. Harris, K.M. Tobey
Publikováno v:
Drug Development Research. 72:310-314
The partial α4β2 nicotinic acetylcholine receptor (nAChR) agonist, varenicline, shares some but not all preclinical effects of nicotine. This unique profile may be crucial to its effectiveness as a therapeutic aid for smoking cessation. The present
Autor:
Louis S. Harris, Matthew D. Metcalf, Mario D. Aceto, John R. Traynor, James H. Woods, Andrew Coop, Everette L. May
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:869-873
To investigate the effects of carboxylic ester and acid moieties as the N-substituent of opioids, a short series of racemic N-substituted normetazocines was prepared. The introduction of both groups as the normetazocine N-substituent produced compoun
Autor:
Anne-Cécile Hiebel,†,‡, Yong Sok Lee, Everette L. May, K. C. Rice, Denise Giuvelis, and Arthur E. Jacobson, Kejun Cheng, Louis S. Harris, Mario D. Aceto, Damon A. Parrish, Andrew Coop, John S. Partilla, Richard B. Rothman, Edward J. Bilsky, Christina M. Dersch, Jeffrey R. Deschamps
Publikováno v:
Journal of Medicinal Chemistry. 50:3765-3776
Both of the enantiomers of 5-(3-hydroxyphenyl)-N-phenylethylmorphan with C9alpha-methyl, C9-methylene, C9-keto, and C9alpha- and C9beta-hydroxy substituents were synthesized and pharmacologically evaluated. Three of the 10 compounds, (1R,5R,9S)-(-)-9
Publikováno v:
European Journal of Pharmacology. 566:88-93
In the search for a selective delta-opioid receptor agonist, (−)-(1 R ,5 R ,9 R )-5,9-dimethyl-2′-hydroxy-2-(6-hydroxyhexyl)-6,7-benzomorphan hydrochloride ((−)-NIH 11082) and the (+)-enantiomer were synthesized and tested. (−)-NIH 11082 disp
Autor:
Edward J. Bilsky, Kenner C. Rice, Steven A. Adah, Mei-Jing Lee, Christina M. Dersch, Louis S. Harris, In Jong Kim, Arthur E. Jacobson, Andrew Coop, Tyler J. Raymond, Richard B. Rothman, Mario D. Aceto, Everette L. May, Kejun Cheng
Publikováno v:
Organic & Biomolecular Chemistry. 5:1177-1190
Enantiomeric N-phenethyl-m-hydroxyphenylmorphans with various substituents in the ortho, meta or para positions of the aromatic ring in the phenethylamine side-chain (chloro, hydroxy, methoxy, nitro, methyl), as well as a pyridylethyl and a indolylet
Autor:
Louis S. Harris
Publikováno v:
Drug and Alcohol Dependence. 83:S48-S51
This article is part of a supplemental issue of the journal devoted entirely to papers on how abuse liability of medications is affected by their formulation for medical use. This article reviews the history of the development of the concept of "exem
Publikováno v:
European Journal of Pharmacology. 524:89-94
JDTic, (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-isoquinoline-carboxamide, is a potent and selective κ - opioid antagonist with a very long duration of action [Carr
Autor:
and Andrew Coop, Mario D. Aceto, Elisabeth Greiner, Helmut Schmidhammer, Louis S. Harris, Mariana Spetea
Publikováno v:
Journal of Medicinal Chemistry. 48:5052-5055
In a continued effort to find new substitution patterns in morphinans that would produce strong antinociception while inducing lesser side effects, 4,5-oxygen bridge-opened 6-cyano-substituted N-methylmorphinans (1-3) were synthesized. All compounds