Jean Bidlack

Summary

Affiliation: University of Rochester
Country: USA

Publications

  1. doi request reprint Mixed kappa/mu partial opioid agonists as potential treatments for cocaine dependence
    Jean M Bidlack
    School of Medicine and Dentistry, University of Rochester, Rochester, New York, USA Electronic address
    Adv Pharmacol 69:387-418. 2014
  2. pmc Phenobarbital withdrawal seizures may occur over several weeks before remitting: human data and hypothetical mechanism
    Jean M Bidlack
    Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, P O Box 711, 601 Elmwood Avenue, Rochester, NY 14642 8711, USA
    Seizure 18:79-81. 2009
  3. ncbi request reprint Opioid receptors and signaling on cells from the immune system
    Jean M Bidlack
    Department of Pharmacology and Physiology, School of Medicine and Dentistry, University of Rochester, P O Box 711, 601 Elmwood Ave, Rochester, NY 14642 8711, USA
    J Neuroimmune Pharmacol 1:260-9. 2006
  4. ncbi request reprint 8-Carboxamidocyclazocine: a long-acting, novel benzomorphan
    Jean M Bidlack
    Department of Pharmacology and Physiology, School of Medicine and Dentistry, University of Rochester, 601 Elmwood Avenue, Rochester, NY 14642 8711, USA
    J Pharmacol Exp Ther 302:374-80. 2002
  5. ncbi request reprint Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties
    Jennifer L Mathews
    Department of Pharmacology and Physiology, University of Rochester School of Medicine and Dentistry, NY 14642 8711, USA
    J Pharmacol Exp Ther 315:821-7. 2005
  6. pmc A novel Gbetagamma-subunit inhibitor selectively modulates mu-opioid-dependent antinociception and attenuates acute morphine-induced antinociceptive tolerance and dependence
    Jennifer L Mathews
    Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, Rochester, New York 14642 8711, USA
    J Neurosci 28:12183-9. 2008
  7. ncbi request reprint Differential targeting of Gbetagamma-subunit signaling with small molecules
    Tabetha M Bonacci
    Department of Pharmacology and Physiology, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA
    Science 312:443-6. 2006
  8. pmc In vivo characterization of (-)(-)MCL-144 and (+)(-)MCL-193: isomeric, bivalent ligands with mu/kappa agonist properties
    Jennifer L Mathews
    Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, P O Box 711, 601 Elmwood Ave, Rochester, NY, 14642 8711, USA
    Neurochem Res 33:2142-50. 2008
  9. ncbi request reprint Assay of G protein-coupled receptor activation of G proteins in native cell membranes using [35S]GTP gamma S binding
    Jean M Bidlack
    Department of Pharmacology and Physiology, University of Rochester School of Medicine, NY, USA
    Methods Mol Biol 237:135-43. 2004
  10. ncbi request reprint Reduction of lipopolysaccharide-induced interleukin-6 production by the kappa opioid U50,488 in a mouse monocyte-like cell line
    Amy L Parkhill
    Department of Pharmacology and Physiology, P O Box 711, University of Rochester, School of Medicine and Dentistry, 601 Elmwood Avenue, Rochester, NY 14642 8711, USA
    Int Immunopharmacol 6:1013-9. 2006

Research Grants

  1. MOLECULAR ASPECTS OF THE MULTIPLE OPIOID RECEPTOR
    Jean Bidlack; Fiscal Year: 1992
  2. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1992
  3. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1990
  4. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1991
  5. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1993
  6. PARTIAL OPIOIDS--POTENTIAL TREATMENTS FOR COCAINE ABUSE
    Jean Bidlack; Fiscal Year: 2000
  7. PARTIAL OPIOIDS--POTENTIAL TREATMENTS FOR COCAINE ABUSE
    Jean Bidlack; Fiscal Year: 2001
  8. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 2001
  9. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 2002
  10. Opioid Binding to U51: A Human herpes Virus Protein
    Jean Bidlack; Fiscal Year: 2002

Collaborators

  • Stevens S Negus
  • J L Neumeyer
  • Alan Smrcka
  • Mark Wentland
  • Mary Kreek
  • Qun Zhou
  • Jennifer L Mathews
  • Xuemei Peng
  • Brian I Knapp
  • Melissa A VanAlstine
  • John J Lowery
  • Amy L Parkhill
  • Tabetha M Bonacci
  • Gavin Bart
  • Ao Zhang
  • Glenn W Stevenson
  • Zhu Zhen
  • Csaba Csutoras
  • Martin E Kuehne
  • Brian S Fulton
  • Robin Polt
  • Frank Porreca
  • Edward J Bilsky
  • Larisa Yeomans
  • Charles M Keyari
  • Peg Davis
  • Dana J Cohen
  • David M Lehmann
  • Sundeep Malik
  • Chujun Yuan
  • Jose L Font
  • Dianqing Wu
  • Wennan Xiong
  • Ann Ho
  • Lisa Borg
  • James H Schluger
  • Birgit G Bradel-Tretheway
  • Stephen Dewhurst
  • Nancy K Mello
  • M W Fleck
  • Liwen He
  • C J Pace
  • I M Maisonneuve
  • Patrick A Jokiel
  • Stanley D Glick

Detail Information

Publications27

  1. doi request reprint Mixed kappa/mu partial opioid agonists as potential treatments for cocaine dependence
    Jean M Bidlack
    School of Medicine and Dentistry, University of Rochester, Rochester, New York, USA Electronic address
    Adv Pharmacol 69:387-418. 2014
    ..Preclinical strategies and successes will lay the groundwork for the further development of mixed μ/κ opioid receptor agonists to treat cocaine dependence. ..
  2. pmc Phenobarbital withdrawal seizures may occur over several weeks before remitting: human data and hypothetical mechanism
    Jean M Bidlack
    Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, P O Box 711, 601 Elmwood Avenue, Rochester, NY 14642 8711, USA
    Seizure 18:79-81. 2009
    ..As suggested by animal studies, the PB withdrawal seizures and increase in aura frequency in this patient may be explained by changes in her levels of GABA(A) receptor subunits...
  3. ncbi request reprint Opioid receptors and signaling on cells from the immune system
    Jean M Bidlack
    Department of Pharmacology and Physiology, School of Medicine and Dentistry, University of Rochester, P O Box 711, 601 Elmwood Ave, Rochester, NY 14642 8711, USA
    J Neuroimmune Pharmacol 1:260-9. 2006
    ..In transfected systems, opioid receptors have been shown to dimerize with chemokine and cannabinoid receptors, resulting in crosstalk between different types of receptors...
  4. ncbi request reprint 8-Carboxamidocyclazocine: a long-acting, novel benzomorphan
    Jean M Bidlack
    Department of Pharmacology and Physiology, School of Medicine and Dentistry, University of Rochester, 601 Elmwood Avenue, Rochester, NY 14642 8711, USA
    J Pharmacol Exp Ther 302:374-80. 2002
    ..8-Carboxamidocyclazocine is a novel, long-acting benzomorphan, which possesses pharmacological properties that are distinct from the properties of cyclazocine...
  5. ncbi request reprint Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties
    Jennifer L Mathews
    Department of Pharmacology and Physiology, University of Rochester School of Medicine and Dentistry, NY 14642 8711, USA
    J Pharmacol Exp Ther 315:821-7. 2005
    ..MCL-145 also acted as a mu antagonist, as measured by the inhibition of morphine-induced antinociception...
  6. pmc A novel Gbetagamma-subunit inhibitor selectively modulates mu-opioid-dependent antinociception and attenuates acute morphine-induced antinociceptive tolerance and dependence
    Jennifer L Mathews
    Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, Rochester, New York 14642 8711, USA
    J Neurosci 28:12183-9. 2008
    ....
  7. ncbi request reprint Differential targeting of Gbetagamma-subunit signaling with small molecules
    Tabetha M Bonacci
    Department of Pharmacology and Physiology, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA
    Science 312:443-6. 2006
    ..These data demonstrate an approach for modulation of G protein-coupled receptor signaling that may represent an important therapeutic strategy...
  8. pmc In vivo characterization of (-)(-)MCL-144 and (+)(-)MCL-193: isomeric, bivalent ligands with mu/kappa agonist properties
    Jennifer L Mathews
    Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, P O Box 711, 601 Elmwood Ave, Rochester, NY, 14642 8711, USA
    Neurochem Res 33:2142-50. 2008
    ..3 nmol and 3.0 nmol, respectively)...
  9. ncbi request reprint Assay of G protein-coupled receptor activation of G proteins in native cell membranes using [35S]GTP gamma S binding
    Jean M Bidlack
    Department of Pharmacology and Physiology, University of Rochester School of Medicine, NY, USA
    Methods Mol Biol 237:135-43. 2004
    ....
  10. ncbi request reprint Reduction of lipopolysaccharide-induced interleukin-6 production by the kappa opioid U50,488 in a mouse monocyte-like cell line
    Amy L Parkhill
    Department of Pharmacology and Physiology, P O Box 711, University of Rochester, School of Medicine and Dentistry, 601 Elmwood Avenue, Rochester, NY 14642 8711, USA
    Int Immunopharmacol 6:1013-9. 2006
    ..Understanding the mechanism behind the reduction of proinflammatory cytokine production by opioids may lead to the development of more effective therapeutics for inflammatory diseases...
  11. ncbi request reprint Transient overexpression of kappa and mu opioid receptors using recombinant adenovirus vectors
    Zhu Zhen
    Department of Microbiology and Immunology, University of Rochester Medical Center, Rochester, NY 14642, USA
    J Neurosci Methods 136:133-9. 2004
    ..These findings demonstrate the feasibility of using rAd5 vectors to express opioid receptors at high densities, which may facilitate opioid receptor studies...
  12. ncbi request reprint Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine
    Mark P Wentland
    Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA
    Bioorg Med Chem Lett 15:2547-51. 2005
    ..High affinity for opioid receptors was observed for the 8-CSNH2 and 8-NHCHS analogues indicating that these groups are isosteric with not only the 8-OH but with the previously synthesized 8-CONH2 and 8-NHCHO cyclazocine derivatives...
  13. ncbi request reprint Synthesis and pharmacology of 8-amino-3-[(tetrahydro-2-furanyl)methyl] benzomorphan
    Qun Zhou
    Department of Chemistry, Rensselaer Polytechnic Institute, Troy, NY 12180, USA
    Yao Xue Xue Bao 38:748-53. 2003
    ..To design and synthesize new chiral 8-(substituted) amino-analogues of 3-[(tetrahydro-2-furanyl)methyl] benzomorphans, to expand knowledge of the structure-activity relationship (SAR) for 8-aminobenzomorphan...
  14. ncbi request reprint Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines
    Mark P Wentland
    Department of Chemistry, Rensselaer Polytechnic Institute, Troy, New York 12180, USA
    J Med Chem 46:838-49. 2003
    ..Several derivatives were shown to have intrinsic opioid-receptor-mediated activity in [(35)S]GTPgammaS assays...
  15. ncbi request reprint An investigation of the N-demethylation of 3-deoxymorphine and the affinity of the alkylation products to mu, delta, and kappa receptors
    Csaba Csutoras
    Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem 12:2687-90. 2004
    ..The mu, delta, and kappa receptor binding affinity of a series of N-substituted 3-deoxynormorphines 6 and 7 and N-substituted 3-deoxydihydronormorphines 8-11 was also determined...
  16. pmc Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine
    Mark P Wentland
    Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA
    Bioorg Med Chem 16:5653-64. 2008
    ..In addition to the results from this study strongly supporting this pharmacophore hypothesis, a number of novel compounds with high affinity to opioid receptors have been identified...
  17. ncbi request reprint Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues
    Mark P Wentland
    Department of Chemistry, Rensselaer Polytechnic Institute, Troy, NY 12180, USA
    Bioorg Med Chem Lett 13:1911-4. 2003
    ..A preliminary SAR revealed that affinity is very sensitive to substitution on the formamide appendage...
  18. pmc Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC
    Melissa A VanAlstine
    Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA
    Bioorg Med Chem Lett 17:6516-20. 2007
    ..High binding affinity to all three opioid receptors were observed for the N-(2-naphthylethyl) analogue of 8-CAC...
  19. pmc In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors
    Xuemei Peng
    Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, Belmont, MA 02478, USA
    Bioorg Med Chem 15:4106-12. 2007
    ..Functional activities of these compounds were measured in the [35S]GTPgammaS binding assay, illustrating that all of these ligands were kappa agonists. At the mu receptor, compounds 11 and 12 were mu agonist/antagonists...
  20. ncbi request reprint Glycosylation improves the central effects of DAMGO
    John J Lowery
    Department of Pharmacology, University of New England, 11 Hill Beach Rd, Biddeford, Maine 04005, USA
    Chem Biol Drug Des 69:41-7. 2007
    ..The optimal 'degree of glycosylation' for the DAMGO peptide message appears to be between 1.25 and 1.75 g.u. (hydrodynamic g.u.), or 0.75 and 0.90 in terms of the surface-derived amphipathicity values...
  21. pmc High-affinity carbamate analogues of morphinan at opioid receptors
    Xuemei Peng
    Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 17:1508-11. 2007
    ..At the mu receptor, compounds 1b, 1c, 2b, and 3b were agonists, while compounds 2c-e and 3c-e were mu agonists/antagonists...
  22. pmc New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores
    John L Neumeyer
    Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, Massachusetts 02478, USA
    J Med Chem 49:5640-3. 2006
    ..MCL 450 represents a useful starting point for the synthesis of other multiple opioid ligands endowed with analgesic properties with low tolerance and dependence...
  23. ncbi request reprint Effects of the mixed-action kappa/mu opioid agonist 8-carboxamidocyclazocine on cocaine- and food-maintained responding in rhesus monkeys
    Glenn W Stevenson
    Alcohol and Drug Abuse Research Center, McLean Hospital Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Eur J Pharmacol 506:133-41. 2004
    ..However, non-selective effects of 8-CAC on food-maintained responding and tolerance to 8-CAC effects on cocaine self-administration may limit its potential for the treatment of cocaine dependence...
  24. ncbi request reprint Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents
    Martin E Kuehne
    Department of Chemistry, University of Vermont, Burlington, Vermont 05405, USA
    J Med Chem 46:2716-30. 2003
    ..The opioid activities were relatively low, and the alpha3beta4 nicotinic acetylcholine receptor activities were found to correlate with in vivo antiaddictive activities...
  25. ncbi request reprint Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone
    Mark P Wentland
    Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA
    Bioorg Med Chem Lett 15:2107-10. 2005
    ..g., K(i)=0.052nM for mu) has been observed in the rationally designed naltrexone analogue 5. SAR and physical data supports the hypothesis that the 4-OH group of 5 stabilizes the 3-carboxamido group in the putative bioactive conformation...
  26. ncbi request reprint Nalmefene induced elevation in serum prolactin in normal human volunteers: partial kappa opioid agonist activity?
    Gavin Bart
    The Laboratory of the Biology of Addictive Diseases, The Rockefeller University, 1230 York Avenue, New York, NY 10021, USA
    Neuropsychopharmacology 30:2254-62. 2005
    ....
  27. ncbi request reprint Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine
    Mark P Wentland
    Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, New York 12180, USA
    J Med Chem 49:5635-9. 2006
    ..High binding affinity to mu, kappa, and delta opioid receptors was observed for the 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogue...

Research Grants38

  1. MOLECULAR ASPECTS OF THE MULTIPLE OPIOID RECEPTOR
    Jean Bidlack; Fiscal Year: 1992
    ..Based on the amino acid sequences, oligonucleotide probes will be synthesized, and used to screen cDNA libraries, in order to ultimately clone the mu opioid receptor...
  2. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1992
    ..The experiments described in this proposal will result in an understanding of the high affinity binding sites and second messenger systems by which kappa opioids can influence immunocompetence...
  3. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1990
    ..These studies will results in a better understanding of how opiates modulate immunocompetence and may help explain why heroin addicts are very susceptible to viral infection...
  4. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1991
    ..These studies will results in a better understanding of how opiates modulate immunocompetence and may help explain why heroin addicts are very susceptible to viral infection...
  5. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 1993
    ..The experiments described in this proposal will result in an understanding of the high affinity binding sites and second messenger systems by which kappa opioids can influence immunocompetence...
  6. PARTIAL OPIOIDS--POTENTIAL TREATMENTS FOR COCAINE ABUSE
    Jean Bidlack; Fiscal Year: 2000
    ..The characterization of novel cyclazocine derivatives will identify potential medications for treating cocaine and heroin abuse and will suggest the basic mechanisms responsible for the drug's action. ..
  7. PARTIAL OPIOIDS--POTENTIAL TREATMENTS FOR COCAINE ABUSE
    Jean Bidlack; Fiscal Year: 2001
    ..The characterization of novel cyclazocine derivatives will identify potential medications for treating cocaine and heroin abuse and will suggest the basic mechanisms responsible for the drug's action. ..
  8. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 2001
    ..These studies will lay the foundation for determining the cellular mechanisms by which opioids alter immune function and immunological responses to viral infection, including AIDS. ..
  9. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 2002
    ..These studies will lay the foundation for determining the cellular mechanisms by which opioids alter immune function and immunological responses to viral infection, including AIDS. ..
  10. Opioid Binding to U51: A Human herpes Virus Protein
    Jean Bidlack; Fiscal Year: 2002
    ..In addition, because HHV-6 and -7 infect both T lymphocytes and cells of the human central nervous system, this could result in the expression of a novel opioid receptor that is only present in the human neurons and T lymphocytes. ..
  11. OPIOID MODULATION OF IMMUNOCOMPETENCE
    Jean Bidlack; Fiscal Year: 2003
    ..These studies will lay the foundation for determining the cellular mechanisms by which opioids alter immune function and immunological responses to viral infection, including AIDS. ..
  12. 36th Annual International Narcotics Research Conference
    Jean Bidlack; Fiscal Year: 2005
    ..We feel that participation by many pre- and postdoctoral trainees has resulted and is likely to continue to result in recruiting promising scientists to a career of drug abuse research. ..
  13. 37th Annual International Narcotics Research Conference
    Jean Bidlack; Fiscal Year: 2006
    ..We feel that participation by many pre- and post-doctoral trainees has resulted and is likely to continue to result in recruiting promising scientists to a career of drug abuse research. ..
  14. OPIOID RECEPTORS ON LYMPHOCYTES AND BRAIN
    Jean Bidlack; Fiscal Year: 2007
    ....
  15. PHARMACOLOGY OF DRUG ABUSE
    Jean Bidlack; Fiscal Year: 2007
    ..This Training Program has served and will continue to serve as the focus for the training and research activities in drug abuse within the University and surrounding community. ..
  16. PHARMACOLOGY OF DRUG ABUSE
    Jean Bidlack; Fiscal Year: 2006
    ..This Training Program has served and will continue to serve as the focus for the training and research activities in drug abuse within the University and surrounding community. ..
  17. 38th Annual International Narcotics Research Conference
    Jean Bidlack; Fiscal Year: 2007
    ..We feel that participation by many pre- and post- doctoral trainees is likely to continue to result in recruiting promising scientists to a career of drug abuse research. ..
  18. MOLECULAR ASPECTS OF THE MULTIPLE OPIOID RECEPTOR
    Jean Bidlack; Fiscal Year: 1993
    ..Based on the amino acid sequences, oligonucleotide probes will be synthesized, and used to screen cDNA libraries, in order to ultimately clone the mu opioid receptor...
  19. PARTIAL OPIOIDS--POTENTIAL TREATMENTS FOR COCAINE ABUSE
    Jean Bidlack; Fiscal Year: 1999
    ..The characterization of novel cyclazocine derivatives will identify potential medications for treating cocaine and heroin abuse and will suggest the basic mechanisms responsible for the drug's action. ..
  20. MOLECULAR ASPECTS OF THE MULTIPLE OPIOID RECEPTOR
    Jean Bidlack; Fiscal Year: 1991
    ..Based on the amino acid sequences, oligonucleotide probes will be synthesized, and used to screen cDNA libraries, in order to ultimately clone the mu opioid receptor...
  21. MOLECULAR ASPECTS OF THE MULTIPLE OPIOID RECEPTORS
    Jean Bidlack; Fiscal Year: 1990
    ..Second messenger effects such as adenylate cyclase and the Na+/H+ antiporter exchange will be studie to determine if PKC is exerting its effect through either of these second messenger systems...