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Items: 25


Benzimidazolone-based selective σ2 receptor ligands: Synthesis and pharmacological evaluation.

Intagliata S, Alsharif WF, Mesangeau C, Fazio N, Seminerio M, Xu YT, Matsumoto RR, McCurdy CR.

Eur J Med Chem. 2019 Mar 1;165:250-257. doi: 10.1016/j.ejmech.2019.01.019. Epub 2019 Jan 9.


Divergent Cytotoxic and Metabolically Stimulative Functions of Sigma-2 Receptors: Structure-Activity Relationships of 6-Acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79) Derivatives.

Nicholson HE, Alsharif WF, Comeau AB, Mesangeau C, Intagliata S, Mottinelli M, McCurdy CR, Bowen WD.

J Pharmacol Exp Ther. 2019 Feb;368(2):272-281. doi: 10.1124/jpet.118.253484. Epub 2018 Dec 7.


Quantification of highly selective sigma-1 receptor antagonist CM304 using liquid chromatography tandem mass spectrometry and its application to a pre-clinical pharmacokinetic study.

Avery BA, Vuppala PK, Jamalapuram S, Sharma A, Mesangeau C, Chin FT, McCurdy CR.

Drug Test Anal. 2017 Aug;9(8):1236-1242. doi: 10.1002/dta.2156. Epub 2017 Apr 11.


Blockade of Cocaine or σ Receptor Agonist Self Administration by Subtype-Selective σ Receptor Antagonists.

Katz JL, Hiranita T, Kopajtic TA, Rice KC, Mesangeau C, Narayanan S, Abdelazeem AH, McCurdy CR.

J Pharmacol Exp Ther. 2016 Jul;358(1):109-24. doi: 10.1124/jpet.116.232728. Epub 2016 Apr 21.


The Sigma-2 Receptor and Progesterone Receptor Membrane Component 1 are Different Binding Sites Derived From Independent Genes.

Chu UB, Mavlyutov TA, Chu ML, Yang H, Schulman A, Mesangeau C, McCurdy CR, Guo LW, Ruoho AE.

EBioMedicine. 2015 Oct 19;2(11):1806-13. doi: 10.1016/j.ebiom.2015.10.017. eCollection 2015 Nov.


Sigma-2 Receptors Play a Role in Cellular Metabolism: Stimulation of Glycolytic Hallmarks by CM764 in Human SK-N-SH Neuroblastoma.

Nicholson H, Mesangeau C, McCurdy CR, Bowen WD.

J Pharmacol Exp Ther. 2016 Feb;356(2):232-43. doi: 10.1124/jpet.115.228387. Epub 2015 Nov 16.


Characterization of CM572, a Selective Irreversible Partial Agonist of the Sigma-2 Receptor with Antitumor Activity.

Nicholson H, Comeau A, Mesangeau C, McCurdy CR, Bowen WD.

J Pharmacol Exp Ther. 2015 Aug;354(2):203-12. doi: 10.1124/jpet.115.224105. Epub 2015 Jun 1.


Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.

Journigan VB, Mésangeau C, Vyas N, Eans SO, Cutler SJ, McLaughlin JP, Mollereau C, McCurdy CR.

J Med Chem. 2014 Nov 13;57(21):8903-27. doi: 10.1021/jm500989n. Epub 2014 Oct 21.


Evaluation of σ-1 receptor radioligand 18F-FTC-146 in rats and squirrel monkeys using PET.

James ML, Shen B, Nielsen CH, Behera D, Buckmaster CL, Mesangeau C, Zavaleta C, Vuppala PK, Jamalapuram S, Avery BA, Lyons DM, McCurdy CR, Biswal S, Gambhir SS, Chin FT.

J Nucl Med. 2014 Jan;55(1):147-53. doi: 10.2967/jnumed.113.120261. Epub 2013 Dec 12.


New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.

James ML, Shen B, Zavaleta CL, Nielsen CH, Mesangeau C, Vuppala PK, Chan C, Avery BA, Fishback JA, Matsumoto RR, Gambhir SS, McCurdy CR, Chin FT.

J Med Chem. 2012 Oct 11;55(19):8272-8282. doi: 10.1021/jm300371c. Epub 2012 Sep 20.


Determination of a highly selective mixed-affinity sigma receptor ligand, in rat plasma by ultra performance liquid chromatography mass spectrometry and its application to a pharmacokinetic study.

Jamalapuram S, Vuppala PK, Mesangeau C, McCurdy CR, Avery BA.

J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Apr 1;891-892:1-6. doi: 10.1016/j.jchromb.2011.12.013. Epub 2011 Dec 20.


Synthesis and pharmacological characterization of a novel sigma receptor ligand with improved metabolic stability and antagonistic effects against methamphetamine.

Seminerio MJ, Robson MJ, Abdelazeem AH, Mesangeau C, Jamalapuram S, Avery BA, McCurdy CR, Matsumoto RR.

AAPS J. 2012 Mar;14(1):43-51. doi: 10.1208/s12248-011-9311-8. Epub 2011 Dec 20.


Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.

Mésangeau C, Amata E, Alsharif W, Seminerio MJ, Robson MJ, Matsumoto RR, Poupaert JH, McCurdy CR.

Eur J Med Chem. 2011 Oct;46(10):5154-61. doi: 10.1016/j.ejmech.2011.08.031. Epub 2011 Aug 29.


CM156, a high affinity sigma ligand, attenuates the stimulant and neurotoxic effects of methamphetamine in mice.

Kaushal N, Seminerio MJ, Shaikh J, Medina MA, Mesangeau C, Wilson LL, McCurdy CR, Matsumoto RR.

Neuropharmacology. 2011 Oct-Nov;61(5-6):992-1000. doi: 10.1016/j.neuropharm.2011.06.028. Epub 2011 Jul 7.


Early development of sigma-receptor ligands.

Narayanan S, Bhat R, Mesangeau C, Poupaert JH, McCurdy CR.

Future Med Chem. 2011 Jan;3(1):79-94. doi: 10.4155/fmc.10.279. Review.


Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands.

Mésangeau C, Fraise M, Delagrange P, Caignard DH, Boutin JA, Berthelot P, Yous S.

Eur J Med Chem. 2011 May;46(5):1835-40. doi: 10.1016/j.ejmech.2011.02.044. Epub 2011 Feb 23.


Synthesis and characterization of [³H]-SN56, a novel radioligand for the σ₁ receptor.

Fishback JA, Mesangeau C, Poupaert JH, McCurdy CR, Matsumoto RR.

Eur J Pharmacol. 2011 Feb 25;653(1-3):1-7. doi: 10.1016/j.ejphar.2010.10.099. Epub 2010 Dec 2.


Sigma receptors and cocaine abuse.

Narayanan S, Mesangeau C, Poupaert JH, McCurdy CR.

Curr Top Med Chem. 2011;11(9):1128-50. Review.


Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis.

Garcés-Ramírez L, Green JL, Hiranita T, Kopajtic TA, Mereu M, Thomas AM, Mesangeau C, Narayanan S, McCurdy CR, Katz JL, Tanda G.

Biol Psychiatry. 2011 Feb 1;69(3):208-17. doi: 10.1016/j.biopsych.2010.07.026. Epub 2010 Oct 15.


Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.

Mésangeau C, Pérès B, Descamps-François C, Chavatte P, Audinot V, Coumailleau S, Boutin JA, Delagrange P, Bennejean C, Renard P, Caignard DH, Berthelot P, Yous S.

Bioorg Med Chem. 2010 May 15;18(10):3426-36. doi: 10.1016/j.bmc.2010.04.008. Epub 2010 Apr 7.


A novel substituted piperazine, CM156, attenuates the stimulant and toxic effects of cocaine in mice.

Xu YT, Kaushal N, Shaikh J, Wilson LL, Mésangeau C, McCurdy CR, Matsumoto RR.

J Pharmacol Exp Ther. 2010 May;333(2):491-500. doi: 10.1124/jpet.109.161398. Epub 2010 Jan 25.


Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.

Mésangeau C, Narayanan S, Green AM, Shaikh J, Kaushal N, Viard E, Xu YT, Fishback JA, Poupaert JH, Matsumoto RR, McCurdy CR.

J Med Chem. 2008 Mar 13;51(5):1482-6. doi: 10.1021/jm701357m. Epub 2008 Feb 16.


Design, synthesis and in vitro evaluation of novel benzo[b]thiophene derivatives as serotonin N-acetyltransferase (AANAT) inhibitors.

Mesangeau C, Yous S, Chavatte P, Ferry G, Audinot V, Boutin JA, Delagrange P, Bennejean C, Renard P, Lesieur D.

J Enzyme Inhib Med Chem. 2003 Apr;18(2):119-25.


Design, synthesis and in vitro evaluation of novel derivatives as serotonin N-acetyltransferase inhibitors.

Beaurain N, Mésangeau C, Chavatte P, Ferry G, Audinot V, Boutin JA, Delagrange P, Bennejean C, Yous S.

J Enzyme Inhib Med Chem. 2002 Dec;17(6):409-14.


Characterization and regulation of a CHO cell line stably expressing human serotonin N-acetyltransferase (EC

Ferry G, Mozo J, Ubeaud C, Berger S, Bertrand M, Try A, Beauverger P, Mesangeau C, Delagrange P, Boutin JA.

Cell Mol Life Sci. 2002 Aug;59(8):1395-405.


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