Research Topics
| Cecile BeguinSummaryAffiliation: Harvard University Country: USA Publications
| Collaborators |
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Publications
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analoguesCecile 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...- Effects of the anticonvulsant lacosamide compared to valproate and lamotrigine on cocaine-enhanced reward in ratsCecile 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... 
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptorCecile 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...
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...- N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacyCecile Beguin
Department of Psychiatry, McLean Hospital, MRC 322A, 115 Mill Street, Belmont, MA 02478, USA
J Pharmacol Exp Ther 324:188-95. 2008.... - Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analoguesDavid 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... - 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... - Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethersThomas 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... - Depressive-like effects of the kappa-opioid receptor agonist salvinorin A on behavior and neurochemistry in ratsWilliam A Carlezon
Department of Psychiatry, McLean Hospital, MRC 217, 115 Mill Street, Belmont, MA 02478
J Pharmacol Exp Ther 316:440-7. 2006.... - Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analoguesDavid 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... - Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicityThomas 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... - Role of kappa-opioid receptors in the effects of salvinorin A and ketamine on attention in ratsChristina 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... - Kappa-opioid ligands in the study and treatment of mood disordersWilliam 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...