Zobrazeno 1 - 10
of 242
pro vyhledávání: '"A E Takemori"'
7-Spiroindanyl Derivatives of Naltrexone and Oxymorphone as Selective Ligands for δ Opioid Receptors
Publikováno v:
Journal of Medicinal Chemistry. 40:1720-1725
A series consisting of spiroindanyl (5-7), benzospiroindanyl (8-10), and spiroperinaphthyl (11) derivatives of naltrexone and oxymorphone were synthesized in order to investigate the role of an orthogonal-oriented "address" for delta opioid receptors
Publikováno v:
Journal of Medicinal Chemistry. 39:4478-4482
Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-(3-aminophenyl)-2-(1-pyrrol idinyl) ethyl]acetamide (5) were synthesized and evaluated in mice for antinociceptive activity by intravenous and intracerebroventricular routes of adm
Publikováno v:
Journal of Medicinal Chemistry. 37:1882-1885
The indolic nitrogen of the delta-opioid receptor antagonist, naltrindole (1), was derivatized with benzyl or substituted benzyl to afford a series (2-9) that retained delta-opioid receptor antagonist activity and selectivity in vitro. The two most p
Publikováno v:
Journal of Medicinal Chemistry. 37:579-585
Naltrindole (1) (NTI) is a highly potent and selective delta-opioid receptor antagonist. In an effort to understand the origin of the high potency, affinity, and selectivity of NTI, we have examined the conformational role of its indolic benzene moie
Autor:
Ronald C. Haaseth, Terry O. Matsunaga, Todd W. Vanderah, Philip S. Portoghese, Victor J. Hruby, A. E. Takemori, Frank Porreca, M. Sultana, Henry I. Mosberg
Publikováno v:
European Journal of Pharmacology. 252:133-137
The interaction of [D-Pen2,D-Pen5]enkephalin (DPDPE) and [D-Ala2,Glu4]deltorphin with delta-opioid receptor subtypes was investigated. Pretreatment of mice with the delta 1-opioid receptor antagonist, [D-Ala2,Leu5,Cys6]enkephalin (DALCE), produced a
Publikováno v:
Journal of Medicinal Chemistry. 36:3669-3673
The fumaramate derivative of naltrexone, beta-funaltrexamine (beta-FNA), is a highly selective long-lasting mu opioid receptor antagonist that is active both in vitro and in vivo, presumably as a result of covalent binding to a mu receptor-based sulf
Autor:
Laurane G. Mendelsohn, B G Johnson, A E Takemori, J D Leander, W N Shaw, J D Snoddy, Jon K. Reel, David T.W. Wong, Buddy E. Cantrell, Charles H. Mitch
Publikováno v:
Journal of Medicinal Chemistry. 36:2842-2850
A series of (3R*,4R*)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists with varying substituents on the nitrogen were evaluated for their effect on food consumption in obese Zucker rats. Opioid affinity (mu, kappa, and delta for selected
Unexpected antinociceptive potency of cyclic [D-Tca1]CTAP: potential for a novel mechanism of action
Autor:
Richard J. Knapp, Wieslaw W. Kazmierski, Lei Fang, Henry I. Yamamura, Kenneth D. Wild, Thomas F. Burks, Frank Porreca, Thomas H. Kramer, Victor J. Hruby, Wayne D. Bowen, P J Horan, Ronald D. Ferguson, Thomas P. Davis, Steven J. Weber, A. E. Takemori
Publikováno v:
European Journal of Pharmacology. 233:53-62
This study tested the hypothesis that compounds which may bind simultaneously to delta and mu receptors may be more potent antinociceptive agents than would be predicted from their binding affinities at individual mu and delta opioid receptors. D-Tca
Autor:
A. E. Takemori, Philip S. Portoghese
Publikováno v:
Life Sciences. 53:1049-1052
beta-Endorphin(1-27) (i.c.v.) has been reported to inhibit the antinociceptive activity of i.c.v. administered beta-endorphin in mice. In this study the antagonist activity of beta-endorphin(1-27) has been confirmed and the antagonism appears to be m
Publikováno v:
Life Sciences. 52:769-775
Recent reports provided evidence that at least two δ opioid receptors may mediate antinociception in mice. In this study, we studied further the involvement of δ opioid receptor subtypes in mediating antinociception at spinal sites in mice using su