Search Results - "Jacobson, Arthur E"

Structure–Activity Relationships of (+)-Naltrexone-Inspired Toll-like Receptor 4 (TLR4) Antagonists by Selfridge, Brandon R, Wang, Xiaohui, Zhang, Yingning, Yin, Hang, Grace, Peter M, Watkins, Linda R, Jacobson, Arthur E, Rice, Kenner C

“…Activation of Toll-like receptors has been linked to neuropathic pain and opioid dependence. (+)-Naltrexone acts as a Toll-like receptor 4 (TLR4) antagonist…”
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Functional Activity of Enantiomeric Oximes and Diastereomeric Amines and Cyano Substituents at C9 in 3-Hydroxy- N -phenethyl-5-phenylmorphans by Roth, Hudson G, Das, Madhurima, Sulima, Agnieszka, Luo, Dan, Kaska, Sophia, Prisinzano, Thomas E, Kerr, Andrew T, Jacobson, Arthur E, Rice, Kenner C

“…The synthesis of stereochemically pure oximes, amines, saturated and unsaturated cyanomethyl compounds, and methylaminomethyl compounds at the C9 position in…”
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Potent MOR Agonists from 2'-Hydroxy-5,9-dimethyl- N -phenethyl Substituted-6,7-benzomorphans and from C8-Hydroxy, Methylene and Methyl Derivatives of N -Phenethylnormetazocine by Das, Madhurima, Ward, George W, Sulima, Agnieszka, Luo, Dan, Prisinzano, Thomas Edward, Imler, Gregory H, Kerr, Andrew T, Jacobson, Arthur E, Rice, Kenner C

“…(-)-5,9-Dimethyl-6,7-benzomorphan (normetazocine) derivatives with a -OH or -F substituent in the aromatic ring of the -phenethyl moiety were synthesized and…”
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A MOR Antagonist with High Potency and Antagonist Efficacy among Diastereomeric C9-Alkyl-Substituted N -Phenethyl-5-(3-hydroxy)phenylmorphans by Chambers, Dana R, Sulima, Agnieszka, Luo, Dan, Prisinzano, Thomas E, Jacobson, Arthur E, Rice, Kenner C

“…The 5-(3-hydroxy)phenylmorphan structural class of compounds are unlike the classical morphinans, 4,5-epoxymorphinans, and 6,7-benzomorphans, in that they have…”
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Discovery of a Potent Highly Biased MOR Partial Agonist among Diastereomeric C9-Hydroxyalkyl-5-phenylmorphans by Lutz, Joshua A, Sulima, Agnieszka, Gutman, Eugene S, Bow, Eric W, Luo, Dan, Kaska, Sophia, Prisinzano, Thomas E, Paronis, Carol A, Bergman, Jack, Imler, Gregory H, Kerr, Andrew T, Jacobson, Arthur E, Rice, Kenner C

“…All possible diastereomeric C9-hydroxymethyl-, hydroxyethyl-, and hydroxypropyl-substituted 5-phenylmorphans were synthesized to explore the three-dimensional…”
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Synthesis and Pharmacological Evaluation of Enantiopure N-Substituted Ortho-c Oxide-Bridged 5-Phenylmorphans by Li, Fuying, Kopajtic, Theresa A, Katz, Jonathan L, Luo, Dan, Prisinzano, Thomas E, Imler, Gregory H, Deschamps, Jeffrey R, Jacobson, Arthur E, Rice, Kenner C

“…The design of enantiopure stereoisomers of N-2-phenylcyclopropylmethyl-substituted ortho-c oxide-bridged phenylmorphans, the E and Z isomers of an N-cinnamyl…”
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A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists by Chambers, Dana R, Sulima, Agnieszka, Luo, Dan, Prisinzano, Thomas E, Goldberg, Alexander, Xie, Bing, Shi, Lei, Paronis, Carol A, Bergman, Jack, Nassehi, Nima, Selley, Dana E, Imler, Gregory H, Jacobson, Arthur E, Rice, Kenner C

“…Four sets of diastereomeric C9-alkenyl 5-phenylmorphans, varying in the length of the C9-alkenyl chain, were designed to examine the effect of these spatially…”
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Design, Synthesis, and In Vivo Evaluation of C1-Linked 4,5-Epoxymorphinan Haptens for Heroin Vaccines by Sulima, Agnieszka, Li, Fuying, Morgan, Jeffrey Brian, Truong, Phong, Antoline, Joshua F G, Oertel, Therese, Barrientos, Rodell C, Torres, Oscar B, Beck, Zoltan, Imler, Gregory H, Deschamps, Jeffrey R, Matyas, Gary R, Jacobson, Arthur E, Rice, Kenner C

“…In our continuing effort to develop effective anti-heroin vaccines as potential medications for the treatment of opioid use disorder, herein we present the…”
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Novel chimeric monoclonal antibodies that block fentanyl effects and alter fentanyl biodistribution in mice by Ban, Bhupal, Barrientos, Rodell C., Oertel, Therese, Komla, Essie, Whalen, Connor, Sopko, Megan, You, Yingjian, Banerjee, Partha, Sulima, Agnieszka, Jacobson, Arthur E., Rice, Kenner C., Matyas, Gary R., Yusibov, Vidadi

“…The prevalence and societal impact of opioid use disorder (OUD) is an acknowledged public health crisis that is further aggravated by the current pandemic. One…”
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The Intriguing Effects of Substituents in the N -Phenethyl Moiety of Norhydromorphone: A Bifunctional Opioid from a Set of "Tail Wags Dog" Experiments by Wang, Meining, Irvin, Thomas C, Herdman, Christine A, Hanna, Ramsey D, Hassan, Sergio A, Lee, Yong-Sok, Kaska, Sophia, Crowley, Rachel Saylor, Prisinzano, Thomas E, Withey, Sarah L, Paronis, Carol A, Bergman, Jack, Inan, Saadet, Geller, Ellen B, Adler, Martin W, Kopajtic, Theresa A, Katz, Jonathan L, Chadderdon, Aaron M, Traynor, John R, Jacobson, Arthur E, Rice, Kenner C

“…(-)- -Phenethyl analogs of optically pure -norhydromorphone were synthesized and pharmacologically evaluated in several in vitro assays (opioid receptor…”
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Role of efficacy as a determinant of locomotor activation by mu‐opioid receptor (MOR) ligands in female and male mice. II. Effects of novel MOR‐selective phenylmorphans with high‐to‐low MOR efficacy by Santos, Edna J., Nassehi, Nima, Bow, Eric W., Chambers, Dana R., Gutman, Eugene S., Jacobson, Arthur E., Lutz, Joshua A., Marsh, Samuel A., Rice, Kenner C., Sulima, Agnieszka, Selley, Dana E., Negus, S. Stevens

“…Low‐efficacy mu‐opioid receptor (MOR) agonists represent promising therapeutics, but existing compounds (e.g., buprenorphine, nalbuphine) span a limited range…”
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Heroin-HIV-1 (H2) vaccine: induction of dual immunologic effects with a heroin hapten-conjugate and an HIV-1 envelope V2 peptide with liposomal lipid A as an adjuvant by Torres, Oscar B., Matyas, Gary R., Rao, Mangala, Peachman, Kristina K., Jalah, Rashmi, Beck, Zoltan, Michael, Nelson L., Rice, Kenner C., Jacobson, Arthur E., Alving, Carl R.

“…A synthetic heroin analog (MorHap) and a synthetic 42 amino acid V2 loop peptide from A/E strain of HIV-1 gp120 envelope protein that was previously used in a…”
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Effect of Preexisting Immunity to Tetanus Toxoid on the Efficacy of Tetanus Toxoid-Conjugated Heroin Vaccine in Mice by Komla, Essie, Torres, Oscar B., Jalah, Rashmi, Sulima, Agnieszka, Beck, Zoltan, Alving, Carl R., Jacobson, Arthur E., Rice, Kenner C., Matyas, Gary R.

“…Opioid use disorder (OUD) is a serious health problem that has dramatically increased over the last decade. Although current therapies for the management of…”
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Reversal of pancreatitis-induced pain by an orally available, small molecule interleukin-6 receptor antagonist by Vardanyan, Marina, Melemedjian, Ohannes K., Price, Theodore J., Ossipov, Michael H., Lai, Josephine, Roberts, Ed, Boos, Terrence L., Deschamps, Jeffrey R., Jacobson, Arthur E., Rice, Kenner C., Porreca, Frank

“…Pancreatic pain resulting from chronic inflammation of the pancreas is often intractable and clinically difficult to manage with available analgesics…”
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Low-Efficacy Mu Opioid Agonists as Candidate Analgesics: Effects of Novel C-9 Substituted Phenylmorphans on Pain-Depressed Behavior in Mice by Santos, Edna J, Akbarali, Hamid I, Bow, Eric W, Chambers, Dana R, Gutman, Eugene S, Jacobson, Arthur E, Kang, Minho, Lee, Young K, Lutz, Joshua A, Rice, Kenner C, Sulima, Agnieszka, Negus, S Stevens

“…Low-efficacy mu opioid receptor (MOR) agonists may serve as novel candidate analgesics with improved safety relative to high-efficacy opioids. This study used…”
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Search for novel TLR4 antagonists for the treatment of neuropathic pain and drug abuse by Wang, Meining, Jacobson, Arthur E

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Bivalent Conjugate Vaccine Induces Dual Immunogenic Response That Attenuates Heroin and Fentanyl Effects in Mice by Barrientos, Rodell C, Whalen, Connor, Torres, Oscar B, Sulima, Agnieszka, Bow, Eric W, Komla, Essie, Beck, Zoltan, Jacobson, Arthur E, Rice, Kenner C, Matyas, Gary R

“…Opioid use disorders and fatal overdose due to consumption of fentanyl-laced heroin remain a major public health menace in the United States. Vaccination may…”
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Enhancing Protective Antibodies against Opioids through Antigen Display on Virus-like Particles by Shafieichaharberoud, Fatemeh, Lang, Shuyao, Whalen, Connor, Rivera Quiles, Cristina, Purcell, Lillie, Talbot, Cameron, Wang, Pengfei, Norton, Elizabeth B., Mazei-Robison, Michelle, Sulima, Agnieszka, Jacobson, Arthur E., Rice, Kenner C., Matyas, Gary R., Huang, Xuefei

“…Opioid use disorder (OUD) has become a public health crisis, with recent significant increases in the number of deaths due to overdose. Vaccination can provide…”
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Novel Vaccine That Blunts Fentanyl Effects and Sequesters Ultrapotent Fentanyl Analogues by Barrientos, Rodell C, Bow, Eric W, Whalen, Connor, Torres, Oscar B, Sulima, Agnieszka, Beck, Zoltan, Jacobson, Arthur E, Rice, Kenner C, Matyas, Gary R

“…Active immunization is an emerging potential modality to combat fatal overdose amid the opioid epidemic. In this study, we described the design, synthesis,…”
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Opioid-galanin receptor heteromers mediate the dopaminergic effects of opioids by Cai, Ning-Sheng, Quiroz, César, Bonaventura, Jordi, Bonifazi, Alessandro, Cole, Thomas O, Purks, Julia, Billing, Amy S, Massey, Ebonie, Wagner, Michael, Wish, Eric D, Guitart, Xavier, Rea, William, Lam, Sherry, Moreno, Estefanía, Casadó-Anguera, Verònica, Greenblatt, Aaron D, Jacobson, Arthur E, Rice, Kenner C, Casadó, Vicent, Newman, Amy H, Winkelman, John W, Michaelides, Michael, Weintraub, Eric, Volkow, Nora D, Belcher, Annabelle M, Ferré, Sergi

“…Identifying non-addictive opioid medications is a high priority in medical sciences, but μ-opioid receptors mediate both the analgesic and addictive effects of…”
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