Lawrence Toll

Summary

Affiliation: Torrey Pines Institute for Molecular Studies
Country: USA

Publications

  1. ncbi request reprint The Use of Bifunctional NOP/Mu and NOP Receptor Selective Compounds for the Treatment of Pain, Drug Abuse, and Psychiatric Disorders
    Lawrence Toll
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    Curr Pharm Des 19:7451-60. 2013
  2. pmc AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats
    Lawrence Toll
    SRI International, Menlo Park, CA, USA
    Neuropsychopharmacology 37:1367-76. 2012
  3. pmc Thermodynamics and docking of agonists to the β(2)-adrenoceptor determined using [(3)H](R,R')-4-methoxyfenoterol as the marker ligand
    Lawrence Toll
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    Mol Pharmacol 81:846-54. 2012
  4. pmc Peptides derived from the prohormone proNPQ/spexin are potent central modulators of cardiovascular and renal function and nociception
    Lawrence Toll
    SRI International, Menlo Park, California, USA
    FASEB J 26:947-54. 2012
  5. pmc Comparison of the antinociceptive and antirewarding profiles of novel bifunctional nociceptin receptor/mu-opioid receptor ligands: implications for therapeutic applications
    Lawrence Toll
    Neuropharmacology Program, SRI International, Menlo Park, California, USA
    J Pharmacol Exp Ther 331:954-64. 2009
  6. pmc Nociceptin/orphanin FQ receptor activation attenuates antinociception induced by mixed nociceptin/orphanin FQ/mu-opioid receptor agonists
    Taline V Khroyan
    Policy Division, SRI International, Menlo Park, California 94025, USA
    J Pharmacol Exp Ther 331:946-53. 2009
  7. pmc Activity of new NOP receptor ligands in a rat peripheral mononeuropathy model: potentiation of morphine anti-allodynic activity by NOP receptor antagonists
    Taline V Khroyan
    Center for Health Sciences, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    Eur J Pharmacol 610:49-54. 2009
  8. pmc Differential effects of nociceptin/orphanin FQ (NOP) receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation chronic pain model in mice
    Taline V Khroyan
    SRI International, Menlo Park, California, USA
    J Pharmacol Exp Ther 339:687-93. 2011
  9. pmc The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mouse mode
    Taline V Khroyan
    SRI International, Menlo Park, CA 94025, USA
    J Pharmacol Exp Ther 336:952-61. 2011
  10. pmc Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation
    Nurulain Zaveri
    Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, California 94025, USA
    J Med Chem 53:8187-91. 2010

Collaborators

Detail Information

Publications26

  1. ncbi request reprint The Use of Bifunctional NOP/Mu and NOP Receptor Selective Compounds for the Treatment of Pain, Drug Abuse, and Psychiatric Disorders
    Lawrence Toll
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    Curr Pharm Des 19:7451-60. 2013
    ....
  2. pmc AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats
    Lawrence Toll
    SRI International, Menlo Park, CA, USA
    Neuropsychopharmacology 37:1367-76. 2012
    ..These findings suggest the utility of this receptor as a target for smoking cessation medications, and highlight the potential of AT-1001 and congeners as clinically useful compounds...
  3. pmc Thermodynamics and docking of agonists to the β(2)-adrenoceptor determined using [(3)H](R,R')-4-methoxyfenoterol as the marker ligand
    Lawrence Toll
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    Mol Pharmacol 81:846-54. 2012
    ..The study underlines the possibility of using defined radioligand structure to probe a specific conformation of such shape-shifting system as the β(2)-adrenoceptor...
  4. pmc Peptides derived from the prohormone proNPQ/spexin are potent central modulators of cardiovascular and renal function and nociception
    Lawrence Toll
    SRI International, Menlo Park, California, USA
    FASEB J 26:947-54. 2012
    ..We conclude that newly identified peptides derived from the NPQ/spexin precursor contribute to CNS-mediated control of arterial blood pressure and salt and water balance and modulate nociceptive responses...
  5. pmc Comparison of the antinociceptive and antirewarding profiles of novel bifunctional nociceptin receptor/mu-opioid receptor ligands: implications for therapeutic applications
    Lawrence Toll
    Neuropharmacology Program, SRI International, Menlo Park, California, USA
    J Pharmacol Exp Ther 331:954-64. 2009
    ..The opioid-modulating effects of the NOPr ligands may be used effectively to produce better medications for treatment of drug abuse and pain...
  6. pmc Nociceptin/orphanin FQ receptor activation attenuates antinociception induced by mixed nociceptin/orphanin FQ/mu-opioid receptor agonists
    Taline V Khroyan
    Policy Division, SRI International, Menlo Park, California 94025, USA
    J Pharmacol Exp Ther 331:946-53. 2009
    ....
  7. pmc Activity of new NOP receptor ligands in a rat peripheral mononeuropathy model: potentiation of morphine anti-allodynic activity by NOP receptor antagonists
    Taline V Khroyan
    Center for Health Sciences, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    Eur J Pharmacol 610:49-54. 2009
    ..Increased levels of the NOP receptor are implicated in the reduced efficacy of morphine in neuropathic pain. Our results suggest the utility of NOP receptor antagonists for potentiating opioid efficacy in chronic pain...
  8. pmc Differential effects of nociceptin/orphanin FQ (NOP) receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation chronic pain model in mice
    Taline V Khroyan
    SRI International, Menlo Park, California, USA
    J Pharmacol Exp Ther 339:687-93. 2011
    ..Thus, although neither NOP agonists nor antagonists are effective as analgesics in acute pain, they may have efficacy as analgesics, either alone or in combination with morphine, for treatment of chronic pain...
  9. pmc The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mouse mode
    Taline V Khroyan
    SRI International, Menlo Park, CA 94025, USA
    J Pharmacol Exp Ther 336:952-61. 2011
    ..Thus, it is possible that a different buprenorphine analog that is a universal high-affinity opioid ligand but with "full agonist" activity at NOP may counteract traditional opioid-mediated effects such as antinociception and reward...
  10. pmc Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation
    Nurulain Zaveri
    Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, California 94025, USA
    J Med Chem 53:8187-91. 2010
    ..In functional assays the lead compound antagonized epibatidine-induced Ca(2+) flux in α3β4-transfected cells in a noncompetitive manner...
  11. pmc Retrodialysis of N/OFQ into the nucleus accumbens shell blocks cocaine-induced increases in extracellular dopamine and locomotor activity
    Jacqueline Vazquez-Derose
    SRI International, Menlo Park, CA 94025, USA
    Eur J Pharmacol 699:200-6. 2013
    ..These studies confirm the widespread involvement of NOP receptors in drug addiction and further validate the utility of an NOP receptor agonist as a medication for treatment of drug addiction...
  12. pmc Evolutionary sequence modeling for discovery of peptide hormones
    Kemal Sonmez
    SRI International, Menlo Park, California, United States of America
    PLoS Comput Biol 5:e1000258. 2009
    ..The success of this approach will have a great impact on our understanding of GPCRs and associated pathways and help to identify new targets for drug development...
  13. pmc Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): ligand-based analysis of structural factors influencing intrinsic activity at NOP
    Nurulain Zaveri
    Biosciences Division, SRI International, Menlo Park, CA 94025, USA
    AAPS J 7:E345-52. 2005
    ....
  14. pmc Hypocretin/orexin and nociceptin/orphanin FQ coordinately regulate analgesia in a mouse model of stress-induced analgesia
    Xinmin Xie
    Biosciences Division, SRI International, Menlo Park, California 94025, USA
    J Clin Invest 118:2471-81. 2008
    ..These results establish what is, to our knowledge, a novel interaction between the N/OFQ and Hcrt systems in which the corticotropin-releasing factor and N/OFQ systems coordinately modulate the Hcrt neurons to regulate SIA...
  15. ncbi request reprint Anti-nociceptive and anti-allodynic effects of a high affinity NOP hexapeptide [Ac-RY(3-Cl)YRWR-NH2] (Syn 1020) in rodents
    Taline V Khroyan
    SRI International, Center for Health Sciences, 333 Ravenswood Ave, Menlo Park, CA 94025, USA
    Eur J Pharmacol 560:29-35. 2007
    ..p, injections of Syn 1020 produced anti-allodynic effects. Thus, Syn 1020, a NOP receptor directed peptide, administered systemically has anti-nociceptive activity in both acute and chronic pain models in mice and rats respectively...
  16. pmc SR 16435 [1-(1-(bicyclo[3.3.1]nonan-9-yl)piperidin-4-yl)indolin-2-one], a novel mixed nociceptin/orphanin FQ/mu-opioid receptor partial agonist: analgesic and rewarding properties in mice
    Taline V Khroyan
    Center for Health Sciences, SRI International, Menlo Park, CA 94025, USA
    J Pharmacol Exp Ther 320:934-43. 2007
    ..In summary, the mixed NOP/mu-opioid partial agonist SR 16435 exhibited both NOP and mu-opioid receptor-mediated behaviors...
  17. ncbi request reprint Regulation of the prepronociceptin gene and its effect on neuronal differentiation
    Naunihal T Zaveri
    SRI International, Biosciences Division, 333 Ravenswood Ave, LA214A, Menlo Park, CA 94025, USA
    Gene 384:27-36. 2006
    ..In rat progenitor and mouse neuroblastoma cell lines, agents that increase ppN/OFQ mRNA expression also induce neurite outgrowth, suggesting a close relationship between ppN/OFQ and cellular differentiation...
  18. pmc A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor
    Nurulain T Zaveri
    Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    J Med Chem 47:2973-6. 2004
    ..The SAR revealed in this new series will provide important insights for the development of pharmacophores for agonist and antagonist actions at the NOP receptor...
  19. pmc [(125)I]AT-1012, a new high affinity radioligand for the α3β4 nicotinic acetylcholine receptors
    Jinhua Wu
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA
    Neuropharmacology 77:193-9. 2014
    ..We demonstrate that [(125)I]AT-1012 is an excellent tool for labeling the α3β4 nAChR in the presence of other nAChR subtypes. ..
  20. doi request reprint Physical presence of nor-binaltorphimine in mouse brain over 21 days after a single administration corresponds to its long-lasting antagonistic effect on κ-opioid receptors
    Kshitij A Patkar
    Torrey Pines Institute for Molecular Studies, Port St Lucie, Florida 34987, USA
    J Pharmacol Exp Ther 346:545-54. 2013
    ..Overall, the physical presence of nor-BNI in the mouse brain paralleled its in vivo pharmacological profile, suggesting physicochemical and pharmacokinetic properties of nor-BNI may contribute to the prolonged KOR antagonism. ..
  21. doi request reprint Nociceptin/orphanin FQ inhibition with SB612111 ameliorates dextran sodium sulfate-induced colitis
    Carsten Alt
    SRI International, Biosciences Division, 333 Ravenswood Avenue, Menlo Park, CA 94025 3493, USA
    Eur J Pharmacol 683:285-93. 2012
    ..We conclude that inhibition of NOP receptors with small molecule inhibitors may constitute a novel, urgently needed approach for the treatment of inflammatory bowel diseases...
  22. ncbi request reprint Regulation of transcription of the human prepronociceptin gene by Sp1
    Naunihal T Zaveri
    Neurobiology Program, SRI International, LA 214A, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    Gene 290:45-52. 2002
    ..Combined with the data from the supershift EMSAs, it appears that Sp1 is the transcription factor binding to the GC region close to the intron to regulate transcription of the human ppN/OFQ gene...
  23. pmc The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands
    Ling Jong
    Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    Bioorg Med Chem Lett 14:181-5. 2004
    ..While the conformational rigidity will provide an improved understanding of the NOP and opioid receptor binding pockets, these compounds also provide a new template for the design of novel opiate and NOP ligands...
  24. ncbi request reprint Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors
    Peter B Madrid
    Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    Bioorg Med Chem Lett 17:3014-7. 2007
    ..The most active compounds showed MICs from 2 to 4 microg/mL and had overall reduced binding to the dopamine and serotonin receptors compared to chlorpromazine and trifluoperazine...
  25. doi request reprint Scaffold Ranking and Positional Scanning Utilized in the Discovery of nAChR-Selective Compounds Suitable for Optimization Studies
    Jinhua Wu
    Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, Florida 34987, United States
    J Med Chem 56:10103-17. 2013
    ....
  26. doi request reprint Rodent motor and neuropsychological behaviour measured in home cages using the integrated modular platform SmartCage™
    Taline V Khroyan
    SRI International, Menlo Park, CA, USA
    Clin Exp Pharmacol Physiol 39:614-22. 2012
    ..This system, combined with the validated testing protocols, offers powerful a tool kit for transgenic phenotyping and in vivo drug screening...