Zobrazeno 1 - 10
of 103
pro vyhledávání: '"Mario D. Aceto"'
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:
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
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
Autor:
Simon W. Breeden, Claire L. Neilan, James H. Woods, Jillian Helen Broadbear, Mario D. Aceto, Stephen M. Husbands, John W. Lewis, Peter Grundt, John R. Traynor
Publikováno v:
European Journal of Pharmacology. 509:117-125
In the search for opioid agonists with delayed antagonist actions as potential treatments for substance abuse, the bridged morphinan BU74 (17-cyclopropylmethyl-3-hydroxy-[5beta,7beta,3',5']-pyrrolidino-2'[S]-phenyl-7alpha-methyl-6,14-endoetheno morph
Autor:
Falko Schüllner, Helmut Schmidhammer, Radu C. Moisa, Louis S. Harris, Cynthia Dörfler, Mariana Spetea, and Andrew Coop, Barbara Schraml, Mario D. Aceto, ‡ Ilona P. Berzetei-Gurske
Publikováno v:
Journal of Medicinal Chemistry. 47:3242-3247
The synthesis, biological, and pharmacological evaluation of novel derivatives of cyprodime are described. Their binding affinities at mu, delta, and kappa opioid receptors were evaluated using receptor binding assay. It was observed that the affinit
Autor:
Mario D. Aceto, Irina Beletskaya, Olivia B Lowery, Billy R. Martin, Susan M. Scates, Christopher S. Breivogel
Publikováno v:
European Journal of Pharmacology. 459:139-150
The effects of chronic Delta(9)-tetrahydrocannabinol on cannabinoid receptor levels and receptor-G-protein coupling were investigated. Male Sprague-Dawley rats were infused continuously with low or high dose regimens of Delta(9)-tetrahydrocannabinol