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Research Output 1961 2019

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2019

Combined Glia Inhibition and Opioid Receptor Agonism Afford Highly Potent Analgesics without Tolerance

Akgun, E., Lunzer, M. M. & Portoghese, P. S., Apr 17 2019, In : ACS Chemical Neuroscience. 10, 4, p. 2004-2011 8 p.

Research output: Contribution to journalArticle

Opioid Receptors
Neuroglia
Astrocytes
Neurons
Analgesics
2018
1 Citation (Scopus)
Open Access
mu Opioid Receptor
Arthritis
Opioid Analgesics
Pain
Morphine
3 Citations (Scopus)

Bivalent ligand MCC22 potently attenuates nociception in a murine model of sickle cell disease

Cataldo, G., Lunzer, M. M., Olson, J., Akgun, E., Belcher, J. D., Vercellotti, G. M., Portoghese, P. S. & Simone, D. A., Jul 1 2018, In : Pain. 159, 7, p. 1382-1391 10 p.

Research output: Contribution to journalArticle

Open Access
Nociception
Sickle Cell Anemia
Ligands
Pain
Morphine
2017
7 Citations (Scopus)

Bivalent ligand that activates mu opioid receptor and antagonizes mGluR5 receptor reduces neuropathic pain in mice

Peterson, C. D., Kitto, K. F., Akgun, E., Lunzer, M. M., Riedl, M. S., Vulchanova, L., Wilcox, G. L., Portoghese, P. S. & Fairbanks, C. A., Jan 1 2017, In : Pain. 158, 12, p. 2431-2441 11 p.

Research output: Contribution to journalArticle

Metabotropic Glutamate 5 Receptor
Oxymorphone
mu Opioid Receptor
Neuralgia
Ligands
9 Citations (Scopus)

Heteromer Induction: An Approach to Unique Pharmacology?

Portoghese, P. S., Akgun, E. & Lunzer, M. M., Mar 15 2017, In : ACS Chemical Neuroscience. 8, 3, p. 426-428 3 p.

Research output: Contribution to journalArticle

Pharmacology
Ligands
Opioid Receptors
Opioid Analgesics
2016

Modulation of musculoskeletal hyperalgesia by brown adipose tissue activity in mice

Angelis, E. M. G. D., Abdelhamid, R. E., Nunez, M. G., Kissel, C. L., Kovacs, K. J., Portoghese, P. S. & Larson, A. A., Aug 19 2016, In : Pain. 157, 11, p. 2561-2570 10 p.

Research output: Contribution to journalArticle

Brown Adipose Tissue
Hyperalgesia
Thermogenesis
Rose Bengal
Adrenergic Agonists
2015
24 Citations (Scopus)

Inhibition of inflammatory and neuropathic pain by targeting a Mu opioid receptor/chemokine receptor5 heteromer (MOR-CCR5)

Akgun, E., Javed, M. I., Lunzer, M. M., Powers, M. D., Sham, Y. Y., Watanabe, Y. & Portoghese, P. S., Nov 12 2015, In : Journal of Medicinal Chemistry. 58, 21, p. 8647-8657 11 p.

Research output: Contribution to journalArticle

mu Opioid Receptor
Neuralgia
Chemokines
Chronic Pain
Morphine
2014
19 Citations (Scopus)

Putative kappa opioid heteromers as targets for developing analgesics free of adverse effects

Le Naour, M., Lunzer, M. M., Powers, M. D., Kalyuzhny, A. E., Benneyworth, M. A., Thomas, M. J. & Portoghese, P. S., Aug 14 2014, In : Journal of Medicinal Chemistry. 57, 15, p. 6383-6392 10 p.

Research output: Contribution to journalArticle

Arrestin
Opioid Analgesics
Analgesics
HEK293 Cells
G-Protein-Coupled Receptors
24 Citations (Scopus)
Metabotropic Glutamate 5 Receptor
Bone Neoplasms
Opioid Analgesics
Nociception
Hyperalgesia
2013
22 Citations (Scopus)

An immunocytochemical-derived correlate for evaluating the bridging of heteromeric mu-delta opioid protomers by bivalent ligands

Yekkirala, A. S., Kalyuzhny, A. E. & Portoghese, P. S., Jul 19 2013, In : ACS Chemical Biology. 8, 7, p. 1412-1416 5 p.

Research output: Contribution to journalArticle

Protein Subunits
Opioid Analgesics
HEK293 Cells
Ligands
Pharmacology
50 Citations (Scopus)

Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB 1) receptors are potent analgesics devoid of tolerance

Le Naour, M., Akgun, E., Yekkirala, A., Lunzer, M. M., Powers, M. D., Kalyuzhny, A. E. & Portoghese, P. S., Jul 11 2013, In : Journal of Medicinal Chemistry. 56, 13, p. 5505-5513 9 p.

Research output: Contribution to journalArticle

Cannabinoid Receptor CB1
Opioid Analgesics
Analgesics
Ligands
Nociception
50 Citations (Scopus)
Ligands
Pain
Opioid Analgesics
Lipopolysaccharides
Chronic Pain
27 Citations (Scopus)

Reduced antinociception of opioids in rats and mice by vaccination with immunogens containing oxycodone and hydrocodone haptens

Pravetoni, M., Le Naour, M., Tucker, A. M., Harmon, T. M., Hawley, T. M., Portoghese, P. S. & Pentel, P. R., Feb 14 2013, In : Journal of Medicinal Chemistry. 56, 3, p. 915-923 9 p.

Research output: Contribution to journalArticle

glycyl-glycyl-glycyl-glycine
Hydrocodone
Oxycodone
Haptens
Opioid Analgesics
2012
39 Citations (Scopus)

Allosteric interactions between δ and κ opioid receptors in peripheral sensory neurons

Berg, K. A., Rowan, M. P., Gupta, A., Sanchez, T. A., Silva, M., Gomes, I., McGuire, B. A., Portoghese, P. S., Hargreaves, K. M., Devi, L. A. & Clarke, W. P., Feb 1 2012, In : Molecular Pharmacology. 81, 2, p. 264-272 9 p.

Research output: Contribution to journalArticle

D-Penicillamine (2,5)-Enkephalin
Opioid Receptors
Sensory Receptor Cells
Hyperalgesia
Prostaglandins E
36 Citations (Scopus)

An oxycodone conjugate vaccine elicits drug-specific antibodies that reduce oxycodone distribution to brain and hot-plate analgesia

Pravetoni, M., Le Naour, M., Harmon, T. M., Tucker, A. M., Portoghese, P. S. & Pentel, P. R., Apr 1 2012, In : Journal of Pharmacology and Experimental Therapeutics. 341, 1, p. 225-232 8 p.

Research output: Contribution to journalArticle

Oxycodone
Conjugate Vaccines
glycyl-glycyl-glycyl-glycine
Analgesia
Antibodies
23 Citations (Scopus)

Clinically employed opioid analgesics produce antinociception via μ-δ Opioid receptor heteromers in rhesus monkeys

Yekkirala, A. S., Banks, M. L., Lunzer, M. M., Negus, S. S., Rice, K. C. & Portoghese, P. S., Sep 19 2012, In : ACS Chemical Neuroscience. 3, 9, p. 720-727 8 p.

Research output: Contribution to journalArticle

naltrindole
delta Opioid Receptor
Opioid Receptors
Macaca mulatta
Morphine
41 Citations (Scopus)

Co-administration of morphine and oxycodone vaccines reduces the distribution of 6-monoacetylmorphine and oxycodone to brain in rats

Pravetoni, M., Raleigh, M. D., Le Naour, M., Tucker, A. M., Harmon, T. M., Jones, J. M., Birnbaum, A. K., Portoghese, P. S. & Pentel, P. R., Jun 29 2012, In : Vaccine. 30, 31, p. 4617-4624 8 p.

Research output: Contribution to journalArticle

Oxycodone
morphine
Morphine
Vaccines
narcotics
14 Citations (Scopus)

Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor

Cawston, E. E., Lam, P. C. H., Harikumar, K. G., Dong, M., Ball, A. M., Augustine, M. L., Akgun, E., Portoghese, P. S., Orry, A., Abagyan, R., Sexton, P. M. & Miller, L. J., May 25 2012, In : Journal of Biological Chemistry. 287, 22, p. 18618-18635 18 p.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Ligands
Benzodiazepines
Stereochemistry
Cholecystokinin B Receptor
9 Citations (Scopus)

Opioid activity of spinally selective analogues of N -naphthoyl-β- naltrexamine in HEK-293 cells and mice

Le Naour, M., Lunzer, M. M., Powers, M. D. & Portoghese, P. S., Jan 26 2012, In : Journal of Medicinal Chemistry. 55, 2, p. 670-677 8 p.

Research output: Contribution to journalArticle

HEK293 Cells
Opioid Analgesics
Ligands
kappa Opioid Receptor
Opioid Receptors
16 Citations (Scopus)

The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ Opioid receptors

Metcalf, M. D., Yekkirala, A. S., Powers, M. D., Kitto, K. F., Fairbanks, C. A., Wilcox, G. L. & Portoghese, P. S., Jul 18 2012, In : ACS Chemical Neuroscience. 3, 7, p. 505-509 5 p.

Research output: Contribution to journalArticle

Opioid Receptors
Cells
Chemical activation
GTP-Binding Proteins
Knockout Mice
2011
5 Citations (Scopus)

A κ opioid pharmacophore becomes a spinally selective κ-δ Agonist when modified with a basic extender arm

Tang, Y., Yang, J., Lunzer, M. M., Powers, M. D. & Portoghese, P. S., Jan 13 2011, In : ACS Medicinal Chemistry Letters. 2, 1, p. 7-10 4 p.

Research output: Contribution to journalArticle

Opioid Receptors
Opioid Analgesics
Atoms
HEK293 Cells
Amines
15 Citations (Scopus)

GRAS flavoring substances 25

Smith, R. L., Waddell, W. J., Cohen, S. M., Fukushima, S., Gooderham, N. J., Hecht, S. S., Marnett, L. J., Portoghese, P. S., Rietjens, I. M. C. M., Adams, T. B., Gavin, C. L., Mcgowen, M. M. & Taylor, S. V., Jul 2011, In : Food Technology. 65, 7, p. 44-75 32 p.

Research output: Contribution to journalArticle

Flavors
flavorings
Ammonium Compounds
flavor
Salts
47 Citations (Scopus)

N-naphthoyl-β-naltrexamine (NNTA), a highly selective and potent activator of μ/κ-opioid heteromers

Yekkirala, A. S., Lunzer, M. M., McCurdy, C. R., Powers, M. D., Kalyuzhny, A. E., Roerig, S. C. & Portoghese, P. S., Mar 22 2011, In : Proceedings of the National Academy of Sciences of the United States of America. 108, 12, p. 5098-5103 6 p.

Research output: Contribution to journalArticle

Opioid Receptors
Opioid Analgesics
HEK293 Cells
G-Protein-Coupled Receptors
Knockout Mice
2010
10 Citations (Scopus)

Consequences of opioid receptor mutation on actions of univalent and bivalent kappa and delta ligands

Ansonoff, M. A., Portoghese, P. S. & Pintar, J. E., Apr 1 2010, In : Psychopharmacology. 209, 2, p. 161-168 8 p.

Research output: Contribution to journalArticle

D-Penicillamine (2,5)-Enkephalin
Opioid Receptors
Ligands
Mutation
delta Opioid Receptor
14 Citations (Scopus)

Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization

Harikumar, K. G., Akgun, E., Portoghese, P. S. & Miller, L. J., Apr 8 2010, In : Journal of Medicinal Chemistry. 53, 7, p. 2836-2842 7 p.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Ligands
Cholecystokinin B Receptor
Fluorescence
CHO Cells
34 Citations (Scopus)
Enkephalins
Opioid Receptors
Morphine
Opioid Analgesics
Ligands
2009
27 Citations (Scopus)

A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors

Zhang, S., Yekkirala, A., Tang, Y. & Portoghese, P. S., Dec 15 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 24, p. 6978-6980 3 p.

Research output: Contribution to journalArticle

Narcotic Antagonists
Ligands
HEK293 Cells
Chemical activation
Atoms
15 Citations (Scopus)

Gras flavoring substances 24

Smith, R. L., Waddell, W. J., Cohen, S. M., Feron, V. J., Marnett, L. J., Portoghese, P. S., Rietjens, I. M. C. M., Adams, T. B., Gavin, C. L., Mcgowen, M. M., Taylor, S. V. & Williams, M. C., Aug 10 2009, Food Technology, 63, 6, p. 46-62 17 p.

Research output: Contribution to specialist publicationArticle

Flavors
flavorings
Publications
flavor
ingredients
42 Citations (Scopus)

Induced association of μ opioid (MOP) and type 2 cholecystokinin (CCK 2) receptors by novel bivalent ligands

Zheng, Y., Akgun, E., Harikumar, K. G., Hopson, J., Powers, M. D., Lunzer, M. M., Miller, L. J. & Portoghese, P. S., Jan 22 2009, In : Journal of Medicinal Chemistry. 52, 2, p. 247-258 12 p.

Research output: Contribution to journalArticle

Cholecystokinin B Receptor
Cholecystokinin Receptors
Opioid Analgesics
Ligands
Energy Transfer
20 Citations (Scopus)

Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and Type 2 cholecystokinin receptors

Akgun, E., Körner, M., Gao, F., Harikumar, K. G., Waser, B., Reubi, J. C., Portoghese, P. S. & Miller, L. J., Apr 9 2009, In : Journal of Medicinal Chemistry. 52, 7, p. 2138-2147 10 p.

Research output: Contribution to journalArticle

Cholecystokinin A Receptor
Cholecystokinin B Receptor
Benzodiazepines
Neoplasms
Binding Sites
2007
53 Citations (Scopus)
delta Opioid Receptor
Narcotic Antagonists
mu Opioid Receptor
Morphine
Ligands
18 Citations (Scopus)

GRAS flavoring substances 23

Waddell, W. J., Cohen, S. M., Feron, V. J., Goodman, J. I., Marnett, L. J., Portoghese, P. S., Rietjens, I. M. C. M., Smith, R. L., Adams, T. B., Lucas Gavin, C., McGowen, M. M. & Williams, M. C., Aug 1 2007, Food Technology, 61, 8, p. 22-28 7 p.

Research output: Contribution to specialist publicationArticle

Flavors
flavorings
GRAS substances
flavor
Organic Chemistry
19 Citations (Scopus)

Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia

Lunzer, M. M., Yekkirala, A., Hebbel, R. P. & Portoghese, P. S., Apr 3 2007, In : Proceedings of the National Academy of Sciences of the United States of America. 104, 14, p. 6061-6065 5 p.

Research output: Contribution to journalArticle

Sickle Cell Anemia
Naloxone
Transgenic Mice
Analgesics
Analgesia
6 Citations (Scopus)

o-naphthalenedicarboxaldehyde derivative of 7′-aminonaltrindole as a selective δ-opioid receptor affinity label

Haris, S. P., Zhang, Y., Le Bourdonnec, B., McCurdy, C. R. & Portoghese, P. S., Jul 12 2007, In : Journal of Medicinal Chemistry. 50, 14, p. 3392-3396 5 p.

Research output: Contribution to journalArticle

Affinity Labels
Schiff Bases
Opioid Receptors
Flow Cytometry
Fluorescence
16 Citations (Scopus)

Selectivity of δ- and κ-opioid ligands depends on the route of central administration in mice

Lunzer, M. M. & Portoghese, P. S., Jul 1 2007, In : Journal of Pharmacology and Experimental Therapeutics. 322, 1, p. 166-171 6 p.

Research output: Contribution to journalArticle

naltrindole
Narcotic Antagonists
Opioid Receptors
Analgesia
Opioid Analgesics
8 Citations (Scopus)
Oxymorphone
Sodium Acetate
delta Opioid Receptor
Opioid Receptors
Positrons
2006
9 Citations (Scopus)
naltrindole
delta Opioid Receptor
Imaging techniques
D-Penicillamine (2,5)-Enkephalin
Vas Deferens
2005
92 Citations (Scopus)

A bivalent ligand (KDAN-18) containing δ-antagonist and κ-agonist pharmacophores bridges δ2 and κ1 opioid receptor phenotype

Daniels, D. J., Kulkarni, A., Xie, Z., Bhushan, R. G. & Portoghese, P. S., Mar 24 2005, In : Journal of Medicinal Chemistry. 48, 6, p. 1713-1716 4 p.

Research output: Contribution to journalArticle

naltrindole
Opioid Receptors
Ligands
Phenotype
Tail
267 Citations (Scopus)

A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers

Waldhoer, M., Fong, J., Jones, R. M., Lunzer, M. M., Sharma, S. K., Kostenis, E., Portoghese, P. S. & Whistler, J. L., Jun 21 2005, In : Proceedings of the National Academy of Sciences of the United States of America. 102, 25, p. 9050-9055 6 p.

Research output: Contribution to journalArticle

G-Protein-Coupled Receptors
Opioid Receptors
Opioid Analgesics
Analgesics
Drug Delivery Systems
15 Citations (Scopus)

Comparison of peptidic and nonpeptidic δ-opioid agonists on guanosine 5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding in brain slices from Sprague-Dawley rats

Jutkiewicz, E. M., Walker, N. P., Folk, J. E., Rice, K. C., Portoghese, P. S., Woods, J. H. & Traynor, J. R., Mar 1 2005, In : Journal of Pharmacology and Experimental Therapeutics. 312, 3, p. 1314-1320 7 p.

Research output: Contribution to journalArticle

Guanosine 5'-O-(3-Thiotriphosphate)
Opioid Analgesics
Sprague Dawley Rats
Brain
naltrindole
33 Citations (Scopus)

GRAS flavoring substances 22

Smith, R. L., Cohen, S. M., Doull, J., Feron, V. J., Goodman, J. I., Marnett, L. J., Portoghese, P. S., Waddell, W. J., Wagner, B. M. & Adams, T. B., Aug 1 2005, Food Technology, 59, 8, p. 24-62 39 p.

Research output: Contribution to specialist publicationArticle

Mentha
Food Additives
Corn Oil
Food Safety
Flavors
51 Citations (Scopus)

Homology modeling and molecular dynamics simulations of the mu opioid receptor in a membrane-aqueous system

Zhang, Y., Sham, Y. Y., Rajamani, R., Gao, J. & Portoghese, P. S., May 1 2005, In : ChemBioChem. 6, 5, p. 853-859 7 p.

Research output: Contribution to journalArticle

Rhodopsin
mu Opioid Receptor
Molecular Dynamics Simulation
Molecular dynamics
Membranes
75 Citations (Scopus)

Interaction of bivalent ligand KDN21 with heterodimeric δ-κ opioid receptors in human embryonic kidney 293 cells

Xie, Z., Bhushan, R. G., Daniels, D. J. & Portoghese, P. S., Oct 1 2005, In : Molecular Pharmacology. 68, 4, p. 1079-1086 8 p.

Research output: Contribution to journalArticle

Opioid Receptors
naltrindole
Ligands
Kidney
Mitogen-Activated Protein Kinase 3
212 Citations (Scopus)

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

Daniels, D. J., Lenard, N. R., Etienne, C. L., Law, P-Y., Roerig, S. C. & Portoghese, P. S., Dec 27 2005, In : Proceedings of the National Academy of Sciences of the United States of America. 102, 52, p. 19208-19213 6 p.

Research output: Contribution to journalArticle

naltrindole
Opioid Receptors
Opioid Analgesics
Ligands
Morphine
7 Citations (Scopus)

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

Zhang, Y., McCurdy, C. R., Metzger, T. G. & Portoghese, P. S., Feb 22 2005, In : Biochemistry. 44, 7, p. 2271-2275 5 p.

Research output: Contribution to journalArticle

Affinity Labels
mu Opioid Receptor
Opioid Receptors
Isoindoles
Fluorophores
2004
116 Citations (Scopus)

A bivalent ligand (KDN-21) reveals spinal δ and κ opioid receptors are organized as heterodimers that give rise to δ1 and δ2 phenotypes. Selective targeting of δ-κ heterodimers

Bhushan, R. G., Sharma, S. K., Xie, Z., Daniels, D. J. & Portoghese, P. S., Jun 3 2004, In : Journal of Medicinal Chemistry. 47, 12, p. 2969-2972 4 p.

Research output: Contribution to journalArticle

Opioid Receptors
Pharmacology
Ligands
Phenotype
Spinal Cord
9 Citations (Scopus)
Myenteric Plexus
Opioid Receptors
Opioid Analgesics
Small Intestine
Diprenorphine
191 Citations (Scopus)

Effects of κ-opioid receptor ligands on intracranial self-stimulation in rats

Todtenkopf, M. S., Marcus, J. F., Portoghese, P. S. & Carlezon, W. A., Apr 1 2004, In : Psychopharmacology. 172, 4, p. 463-470 8 p.

Research output: Contribution to journalArticle

Self Stimulation
Opioid Receptors
Reward
Ligands
Cyclic AMP Response Element-Binding Protein
22 Citations (Scopus)

Safety evaluation of natural flavour complexes

Smith, R. L., Adams, T. B., Cohen, S. M., Doull, J., Feron, V. J., Goodman, J. I., Hall, R. L., Marnett, L. J., Portoghese, P. S., Waddell, W. J. & Wagner, B. M., Apr 1 2004, In : Toxicology Letters. 149, 1-3, p. 197-207 11 p.

Research output: Contribution to journalArticle

Flavors
Safety
Toxicology
Poisons
Metabolic Networks and Pathways
2003
345 Citations (Scopus)

Antidepressant-like effects of κ-opioid receptor antagonists in the forced swim test in rats

Mague, S. D., Pliakas, A. M., Todtenkopf, M. S., Tomasiewicz, H. C., Zhang, Y., Stevens, W. C., Jones, R. M., Portoghese, P. S. & Carlezon, W. A., Apr 1 2003, In : Journal of Pharmacology and Experimental Therapeutics. 305, 1, p. 323-330 8 p.

Research output: Contribution to journalArticle

Narcotic Antagonists
Cyclic AMP Response Element-Binding Protein
Antidepressive Agents
Nucleus Accumbens
Dynorphins