Cecile Beguin

Summary

Affiliation: Harvard University
Country: USA

Publications

  1. ncbi request reprint Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues
    Cecile Beguin
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA Department of Psychiatry, Harvard Medical School, Boston, MA 02215, USA
    Bioorg Med Chem Lett 22:1023-6. 2012
  2. doi request reprint Effects of the anticonvulsant lacosamide compared to valproate and lamotrigine on cocaine-enhanced reward in rats
    Cecile Beguin
    Mailman Research Center, McLean Hospital, 115 Mill Street, Belmont, MA 02478, USA
    Brain Res 1479:44-51. 2012
  3. pmc Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor
    Cecile Beguin
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem 17:1370-80. 2009
  4. ncbi request reprint Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 16:4679-85. 2006
  5. ncbi request reprint N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy
    Cecile Beguin
    Department of Psychiatry, McLean Hospital, MRC 322A, 115 Mill Street, Belmont, MA 02478, USA
    J Pharmacol Exp Ther 324:188-95. 2008
  6. pmc Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters
    Thomas A Munro
    McLean Hospital, Belmont, Massachusetts, United States of America Department of Psychiatry, Harvard Medical School, Boston, Massachusetts, United States of America School of Chemistry and Bio21 Institute, University of Melbourne, Parkville, Australia
    PLoS ONE 8:e70701. 2013
  7. ncbi request reprint Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues
    David Y W Lee
    Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:4169-73. 2005
  8. ncbi request reprint Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:2761-5. 2005
  9. pmc Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers
    Thomas A Munro
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem 16:1279-86. 2008
  10. ncbi request reprint Depressive-like effects of the kappa-opioid receptor agonist salvinorin A on behavior and neurochemistry in rats
    William A Carlezon
    Department of Psychiatry, McLean Hospital, MRC 217, 115 Mill Street, Belmont, MA 02478
    J Pharmacol Exp Ther 316:440-7. 2006

Detail Information

Publications14

  1. ncbi request reprint Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues
    Cecile Beguin
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA Department of Psychiatry, Harvard Medical School, Boston, MA 02215, USA
    Bioorg Med Chem Lett 22:1023-6. 2012
    ..By comparison, the non-selective opioid ligand nalbuphine, known to be a partial agonist for G-protein activation, was also a partial agonist for the β-arrestin mediated signaling pathway activated through KOPR...
  2. doi request reprint Effects of the anticonvulsant lacosamide compared to valproate and lamotrigine on cocaine-enhanced reward in rats
    Cecile Beguin
    Mailman Research Center, McLean Hospital, 115 Mill Street, Belmont, MA 02478, USA
    Brain Res 1479:44-51. 2012
    ..Abnormalities of mood and reward are common in psychiatric disorders, and these results suggest that lacosamide deserves further study in models of these disorders...
  3. pmc Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor
    Cecile Beguin
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem 17:1370-80. 2009
    ..Finally, substitution of oxadiazoles for the furan ring abolished affinity for the KOPR. None of the compounds displayed any KOPR antagonism or any affinity for mu or delta opioid receptors...
  4. ncbi request reprint Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 16:4679-85. 2006
    ..Our preliminary SAR study at C(18) suggested that this part of the molecule interacts with a tight lipophilic pocket of the kappa-receptor...
  5. ncbi request reprint N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy
    Cecile Beguin
    Department of Psychiatry, McLean Hospital, MRC 322A, 115 Mill Street, Belmont, MA 02478, USA
    J Pharmacol Exp Ther 324:188-95. 2008
    ....
  6. pmc Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters
    Thomas A Munro
    McLean Hospital, Belmont, Massachusetts, United States of America Department of Psychiatry, Harvard Medical School, Boston, Massachusetts, United States of America School of Chemistry and Bio21 Institute, University of Melbourne, Parkville, Australia
    PLoS ONE 8:e70701. 2013
    ..The transient effects of these compounds differ, suggesting that some of them may be mediated by other targets...
  7. ncbi request reprint Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues
    David Y W Lee
    Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:4169-73. 2005
    ..These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human kappa-opioid receptor and several potent new agonists have been identified...
  8. ncbi request reprint Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:2761-5. 2005
    ..Compound 10, containing an N-methyl carbamate at C(2), showed partial agonist activity with 81% efficacy when compared with the full agonist U50,488H. No antagonist ligands were observed...
  9. pmc Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers
    Thomas A Munro
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem 16:1279-86. 2008
    ..These protecting groups may prove useful in related work not only by enabling the use of harsher synthetic conditions, but potentially by optimizing the potency of the products...
  10. ncbi request reprint Depressive-like effects of the kappa-opioid receptor agonist salvinorin A on behavior and neurochemistry in rats
    William A Carlezon
    Department of Psychiatry, McLean Hospital, MRC 217, 115 Mill Street, Belmont, MA 02478
    J Pharmacol Exp Ther 316:440-7. 2006
    ....
  11. pmc Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
    Thomas A Munro
    McLean Hospital, Belmont, MA and Department of Psychiatry, Harvard Medical School, Boston, MA, USA
    BMC Pharmacol 12:5. 2012
    ..Recent evidence suggests, instead, that they induce prolonged desensitization of the κ opioid receptor...
  12. ncbi request reprint Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues
    David Y W Lee
    Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 15:3744-7. 2005
    ..Compound 4, containing a methoxymethyl group at the 2-position, was a full kappa-agonist with an EC50 value at 0.6 nM, which is about 7 times more potent than salvinorin A...
  13. pmc Role of kappa-opioid receptors in the effects of salvinorin A and ketamine on attention in rats
    Christina L Nemeth
    Behavioral Genetics Laboratory, Department of Psychiatry, Harvard Medical School, McLean Hospital, Belmont, MA 02478, USA
    Psychopharmacology (Berl) 210:263-74. 2010
    ..One way to study these states in rodents is with tests that require attention and visual perception for correct performance...
  14. pmc Kappa-opioid ligands in the study and treatment of mood disorders
    William A Carlezon
    Behavioral Genetics Laboratory, Department of Psychiatry, Harvard Medical School, McLean Hospital, Belmont, MA 02478, USA
    Pharmacol Ther 123:334-43. 2009
    ..The development of KOR-selective agents with improved drug-like characteristics would facilitate preclinical and clinical studies designed to evaluate the possibility that KORs are a feasible target for new medications...