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411 results on '"Portoghese, Philip S."'

5. Opioid receptors in GtoPdb v.2023.1

Author

Borsodi, Anna, primary, Bruchas, Michael, primary, Caló, Girolamo, primary, Chavkin, Charles, primary, Christie, MacDonald J., primary, Civelli, Olivier, primary, Connor, Mark, primary, Cox, Brian M., primary, Devi, Lakshmi A., primary, Evans, Christopher, primary, Höllt, Volker, primary, Henderson, Graeme, primary, Husbands, Stephen, primary, Kelly, Eamonn, primary, Kieffer, Brigitte, primary, Kitchen, Ian, primary, Kreek, Mary-Jeanne, primary, Liu-Chen, Lee-Yuan, primary, Malfacini, Davide, primary, Massot, Dominique, primary, Meunier, Jean-Claude, primary, Portoghese, Philip S., primary, Schulz, Stefan, primary, Shippenberg, Toni S., primary, Simon, Eric J., primary, Toll, Lawrence, primary, Traynor, John R., primary, Ueda, Hiroshi, primary, Wong, Yung H., primary, Zaveri, Nurulain, primary, and Zimmer, Andreas, primary

Published
2023
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15. Opioid receptors in GtoPdb v.2021.3

Author

Borsodi, Anna, primary, Bruchas, Michael, primary, Caló, Girolamo, primary, Chavkin, Charles, primary, Christie, MacDonald J., primary, Civelli, Olivier, primary, Connor, Mark, primary, Cox, Brian M., primary, Devi, Lakshmi A., primary, Evans, Christopher, primary, Höllt, Volker, primary, Henderson, Graeme, primary, Husbands, Stephen, primary, Kelly, Eamonn, primary, Kieffer, Brigitte, primary, Kitchen, Ian, primary, Kreek, Mary-Jeanne, primary, Liu-Chen, Lee-Yuan, primary, Massot, Dominique, primary, Meunier, Jean-Claude, primary, Portoghese, Philip S., primary, Schulz, Stefan, primary, Shippenberg, Toni S., primary, Simon, Eric J., primary, Toll, Lawrence, primary, Traynor, John R., primary, Ueda, Hiroshi, primary, Wong, Yung H., primary, Zaveri, Nurulain, primary, and Zimmer, Andreas, primary

Published
2021
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20. Opioid-induced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series

Author

Daniels, David J., Lenard, Natalie R., Etienne, Chris L., Law, Ping-Yee, Roerig, Sandra C., and Portoghese, Philip S.

Subjects
Ligand binding (Biochemistry) -- Research, Opioids -- Receptors, Opioids -- Research, Science and technology
Abstract

Given the mounting evidence for involvement of [delta] opioid receptors in the tolerance and physical dependence of [micro] opioid receptor agonists, we have investigated the possible physical interaction between [micro] and [delta] opioid receptors by using bivalent ligands. Based on reports of suppression of antinociceptive tolerance by the antagonist naltrindole (NTI), bivalent ligands [[micro]-[delta] a gonist-antagonist (MDAN) series] that contain different length spacers, and pharmacophores derived from NTI and the [micro] agonist oxymorphone, have been synthesized and evaluated by intracerebroventricular (i.c.v.) administration in the tail-flick test in mice. In acute i.c.v. studies, the bivalent ligands functioned as agonists with potencies ranging from 1.6- to 45-fold greater than morphine. In contrast, the monovalent [micro] agonist analogues were substantially more potent than the MDAN congeners and were essentially equipotent with one another and oxymorphone. Pretreatment with NTI decreased the E[D.sub.50] values for MDAN-19 to a greater degree than for MDAN-16 but had no effect on MDAN-21. Chronic i.c.v. studies revealed that MDAN ligands whose spacer was 16 atoms or longer produced less dependence than either morphine or [micro] monovalent control MA-19. On the other hand, both physical dependence and tolerance were suppressed at MDAN spacer lengths of 19 atoms or greater. These data suggest that physical interaction between the [micro] and [delta] opioid receptors modulates [micro]-mediated tolerance and dependence. Because MDAN-21 was found to be 50-fold more potent than morphine by the i.v. route (i.v.), it offers a previously uncharacterized approach for the development of analgesics devoid of tolerance and dependence. antinociception | heterodimers

Published
2005

22. Specific cross-linking of Lys233 and Cys235 in the mu opioid receptor by a reporter affinity label

Author

Yan Zhang, McCurdy, Christopher R., Metzger, Thomas G., and Portoghese, Philip S.

Subjects
Affinity labeling -- Usage, DNA-ligand interactions -- Research, Opioids -- Receptors, Opioids -- Research, Biological sciences, Chemistry
Abstract

The kinetics of isoindole formation resulting from covalent binding of NNA to wild type and mutant mu opioid receptors were followed in cultured cells using flow cytometry. The finding that NNA bound to mutant mu opioid receptors (K233R and C235s) without producing specific fluorescence enhancement suggested that covalent bonding occurred at these positions to produce an isoindole fluorophore in the wild type mu receptor.

Published
2005

24. GRAS flavoring substances 21: the 21st publication by the Expert Panel of the Flavor and Extract Manufacturers Association on recent progress in the consideration of flavoring ingredients generally recognized as safe under the Food Additives Amendment

Author

Smith, Robert L., Cohen, Samuel M., Doull, John, Feron, Victor J., Goodman, Jay I., Marnett, Lawrence J., Portoghese, Philip S., Waddell, William J., Wagner, Bernard M., and Adams, Timothy B.

Subjects
United States. Food and Drug Administration -- Laws, regulations and rules, Flavoring essences -- Research, Government regulation, Company legal issue, Business, Food and beverage industries, Expert Panel of the Flavor and Extract Manufacturers Association -- Investigations
Abstract

The latest flavoring safety assessments performed by the Expert Panel of the Flavor and Extract Manufacturers Association are presented. A full list of flavorings that are generally recognized as safe is also included.

Published
2003

29. Opioid receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

Author

Borsodi, Anna, primary, Bruchas, Michael, primary, Caló, Girolamo, primary, Chavkin, Charles, primary, Christie, MacDonald J., primary, Civelli, Olivier, primary, Connor, Mark, primary, Cox, Brian M., primary, Devi, Lakshmi A., primary, Evans, Christopher, primary, Höllt, Volker, primary, Henderson, Graeme, primary, Husbands, Stephen, primary, Kelly, Eamonn, primary, Kieffer, Brigitte, primary, Kitchen, Ian, primary, Kreek, Mary-Jeanne, primary, Liu-Chen, Lee-Yuan, primary, Massot, Dominique, primary, Meunier, Jean-Claude, primary, Portoghese, Philip S., primary, Schulz, Stefan, primary, Shippenberg, Toni S., primary, Simon, Eric J., primary, Toll, Lawrence, primary, Traynor, John R., primary, Ueda, Hiroshi, primary, Wong, Yung H., primary, Zaveri, Nurulain, primary, and Zimmer, Andreas, primary

Published
2019
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33. Boron tribromide-catalyzed rearrangement of 7,7-diphenylhydromorphone to 6,7-diphenylmorphine: a novel conversion of ketones to allylic alcohols

Author

Gao, Peng and Portoghese, Philip S.

Subjects
Rearrangements (Chemistry) -- Research, Ketones -- Research, Alcohols -- Research, Biological sciences, Chemistry
Abstract

A unique ketone to allylic alcohol rearrangement has been discovered in the 7-phenylmorphinan-6-one system. The rearrangement is catalyzed by boron tribromide. Its mechanistic pathway is postulated to involve the coordination of the carbonyl group by boron tribromide, which would consequently promote migration of the axial 7-beta-phenyl group.

Published
1996

41. Stereochemistry and innate immune recognition: (+)‐norbinaltorphimine targets myeloid differentiation protein 2 and inhibits toll‐like receptor 4 signaling

Author

Zhang, Xiaozheng, primary, Peng, Yinghua, additional, Grace, Peter M., additional, Metcalf, Matthew D., additional, Kwilasz, Andrew J., additional, Wang, Yibo, additional, Zhang, Tianshu, additional, Wu, Siru, additional, Selfridge, Brandon R., additional, Portoghese, Philip S., additional, Rice, Kenner C., additional, Watkins, Linda R., additional, Hutchinson, Mark R., additional, and Wang, Xiaohui, additional

Published
2019
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42. FBNTI, a DOR-Selective Antagonist That Allosterically Activates MOR within a MOR–DOR Heteromer

Author

Akgün, Eyup, Lunzer, Mary M., Tian, Defeng, Ansonoff, Michael, Pintar, John, Bruce, Daniel, Hawkinson, Jon E., Wilcox, George L., and Portoghese, Philip S.

Abstract

This report describes the unique pharmacological profile of FBNTI, a potent DOR antagonist that acts as a MOR agonist via an allosteric mechanism. Binding of FBNTI to opioid receptors expressed in HEK 293 cells revealed a 190-fold greater affinity for DOR (Ki= 0.84 nM) over MOR (Ki= 160 nM). In mice, intrathecal FBNTI produced potent antinociception (ED50= 46.9 pmol/mouse), which was antagonized by selective MOR antagonists (CTOP, β-FNA). Autoantagonism of the MOR agonism by FBNTI was observed above the ED75dose, suggesting antagonism of activated MOR. That FBNTI is devoid of agonism in DOR knockout mice is consistent with allosteric activation of the MOR protomer via FBNTI bound to within a MOR–DOR heteromer. This proposed mechanism is supported by calcium mobilization assays, which indicate that FBNTI selectively activates the MOR–DOR heteromer and functionally antagonizes the MOR protomer at >ED75. The unprecedented mode of MOR activation by FBNTI may be responsible for the lack of tolerance after intrathecal (i.t.) administration. FBNTI was highly effective upon topical administration to the ipsolateral hind paw in the Hargreaves assay (EC50= 0.17 ± 0.08 μM) and without significant contralateral activity, suggesting a lack of systemic exposure.

Published
2021
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43. Opiate dienes as dienophiles in the Diels-Alder reaction with 1-cyano-o-quinodimethane

Author

Kshirsagar, Tushar A. and Portoghese, Philip S.

Subjects
Diels-Alder reaction -- Research, Narcotics -- Research, Biological sciences, Chemistry
Abstract

The Diels-Alder reaction of opiate dienophiles with o-quinodimethanes is a route to tetrahydronaphthalene-fused opiates. This was gleaned from an examination of the Diels-Alder reactions of thebaine and a related opiate with the reactive diene, which led to the synthesis of tetrahydronaphthalene-fused opiates that are not easily available using other means. The 6-methoxy group of thebaine is also found to play a key role in the reaction.

Published
1998

46. Monophenylation of morphinan-6-ones with diphenyliodonium iodide

Author

Gao, Peng and Portoghese, Philip S.

Subjects
Iodides -- Research, Ketones -- Analysis, Biological sciences, Chemistry
Abstract

By reacting lithium enolate of hydrocodone with commercially available diphenyliodonium iodide (DII), the conversion of hydrocodone into 7-phenylhydrocodone can be obtained in good amount. The DII approaches the beta-face of the enolate, resulting in enolization and epimerization of the 6-beta isomer, which is then ketonized to the stable 6-alpha epimer.

Published
1995

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