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Discovery of β-arrestin-biased β2-adrenoceptor agonists from 2-amino-2-phenylethanol derivatives.

Woo AY, Ge XY, Pan L, Xing G, Mo YM, Xing RJ, Li XR, Zhang YY, Wainer IW, Cheng MS, Xiao RP.

Acta Pharmacol Sin. 2019 Aug;40(8):1095-1105. doi: 10.1038/s41401-018-0200-x. Epub 2019 Jan 14.


d-Serine is a potential biomarker for clinical response in treatment of post-traumatic stress disorder using (R,S)-ketamine infusion and TIMBER psychotherapy: A pilot study.

Pradhan B, Mitrev L, Moaddell R, Wainer IW.

Biochim Biophys Acta Proteins Proteom. 2018 Jul;1866(7):831-839. doi: 10.1016/j.bbapap.2018.03.006. Epub 2018 Mar 18.


Stereochemical and structural effects of (2R,6R)-hydroxynorketamine on the mitochondrial metabolome in PC-12 cells.

Faccio AT, Ruperez FJ, Singh NS, Angulo S, Tavares MFM, Bernier M, Barbas C, Wainer IW.

Biochim Biophys Acta Gen Subj. 2018 Jun;1862(6):1505-1515. doi: 10.1016/j.bbagen.2018.03.008. Epub 2018 Mar 9.


GPR55 receptor antagonist decreases glycolytic activity in PANC-1 pancreatic cancer cell line and tumor xenografts.

Bernier M, Catazaro J, Singh NS, Wnorowski A, Boguszewska-Czubara A, Jozwiak K, Powers R, Wainer IW.

Int J Cancer. 2017 Nov 15;141(10):2131-2142. doi: 10.1002/ijc.30904. Epub 2017 Aug 7.


Concurrent activation of β2-adrenergic receptor and blockage of GPR55 disrupts pro-oncogenic signaling in glioma cells.

Wnorowski A, Such J, Paul RK, Wersto RP, Indig FE, Jozwiak K, Bernier M, Wainer IW.

Cell Signal. 2017 Aug;36:176-188. doi: 10.1016/j.cellsig.2017.05.006. Epub 2017 May 8.


Reply to: Antidepressant Actions of Ketamine Versus Hydroxynorketamine.

Zanos P, Moaddel R, Morris PJ, Wainer IW, Albuquerque EX, Thompson SM, Thomas CJ, Zarate CA Jr, Gould TD.

Biol Psychiatry. 2017 Apr 15;81(8):e69-e71. doi: 10.1016/j.biopsych.2016.08.039. Epub 2016 Sep 30. No abstract available.


Effects of Ketamine and Ketamine Metabolites on Evoked Striatal Dopamine Release, Dopamine Receptors, and Monoamine Transporters.

Can A, Zanos P, Moaddel R, Kang HJ, Dossou KS, Wainer IW, Cheer JF, Frost DO, Huang XP, Gould TD.

J Pharmacol Exp Ther. 2016 Oct;359(1):159-70. doi: 10.1124/jpet.116.235838. Epub 2016 Jul 28.


Selective GPR55 antagonism reduces chemoresistance in cancer cells.

Singh NS, Bernier M, Wainer IW.

Pharmacol Res. 2016 Sep;111:757-766. doi: 10.1016/j.phrs.2016.07.013. Epub 2016 Jul 14.


NMDAR inhibition-independent antidepressant actions of ketamine metabolites.

Zanos P, Moaddel R, Morris PJ, Georgiou P, Fischell J, Elmer GI, Alkondon M, Yuan P, Pribut HJ, Singh NS, Dossou KS, Fang Y, Huang XP, Mayo CL, Wainer IW, Albuquerque EX, Thompson SM, Thomas CJ, Zarate CA Jr, Gould TD.

Nature. 2016 May 26;533(7604):481-6. doi: 10.1038/nature17998. Epub 2016 May 4.


Ketamine Metabolites Enantioselectively Decrease Intracellular D-Serine Concentrations in PC-12 Cells.

Singh NS, Rutkowska E, Plazinska A, Khadeer M, Moaddel R, Jozwiak K, Bernier M, Wainer IW.

PLoS One. 2016 Apr 20;11(4):e0149499. doi: 10.1371/journal.pone.0149499. eCollection 2016.


Subchronic administration of (R,S)-ketamine induces ketamine ring hydroxylation in Wistar rats.

Moaddel R, Sanghvi M, Ramamoorthy A, Jozwiak K, Singh N, Green C, O'Loughlin K, Torjman M, Wainer IW.

J Pharm Biomed Anal. 2016 Aug 5;127:3-8. doi: 10.1016/j.jpba.2016.03.030. Epub 2016 Mar 14.


Development and characterization of the α3β4α5 nicotinic receptor cellular membrane affinity chromatography column and its application for on line screening of plant extracts.

Ciesla L, Okine M, Rosenberg A, Dossou KSS, Toll L, Wainer IW, Moaddel R.

J Chromatogr A. 2016 Jan 29;1431:138-144. doi: 10.1016/j.chroma.2015.12.065. Epub 2015 Dec 29.


Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.

Littmann T, Göttle M, Reinartz MT, Kälble S, Wainer IW, Ozawa T, Seifert R.

J Pharmacol Exp Ther. 2015 Nov;355(2):183-90. doi: 10.1124/jpet.115.227959. Epub 2015 Aug 25.


The distribution and clearance of (2S,6S)-hydroxynorketamine, an active ketamine metabolite, in Wistar rats.

Moaddel R, Sanghvi M, Dossou KS, Ramamoorthy A, Green C, Bupp J, Swezey R, O'Loughlin K, Wainer IW.

Pharmacol Res Perspect. 2015 Aug;3(4):e00157. doi: 10.1002/prp2.157. Epub 2015 Jun 22.


Enantioselective inhibition of d-serine transport by (S)-ketamine.

Singh NS, Bernier M, Camandola S, Khadeer MA, Moaddel R, Mattson MP, Wainer IW.

Br J Pharmacol. 2015 Sep;172(18):4546-4559. doi: 10.1111/bph.13239. Epub 2015 Jul 31.


The development of mitochondrial membrane affinity chromatography columns for the study of mitochondrial transmembrane proteins.

Habicht KL, Singh NS, Indig FE, Wainer IW, Moaddel R, Shimmo R.

Anal Biochem. 2015 Sep 1;484:154-61. doi: 10.1016/j.ab.2015.05.018. Epub 2015 Jun 4.


Activation of β2-adrenergic receptor by (R,R')-4'-methoxy-1-naphthylfenoterol inhibits proliferation and motility of melanoma cells.

Wnorowski A, Sadowska M, Paul RK, Singh NS, Boguszewska-Czubara A, Jimenez L, Abdelmohsen K, Toll L, Jozwiak K, Bernier M, Wainer IW.

Cell Signal. 2015 May;27(5):997-1007. doi: 10.1016/j.cellsig.2015.02.012. Epub 2015 Feb 20.


Interaction of fenoterol stereoisomers with β2-adrenoceptor-G sα fusion proteins: antagonist and agonist competition binding.

Reinartz MT, Kälble S, Wainer IW, Seifert R.

Naunyn Schmiedebergs Arch Pharmacol. 2015 May;388(5):517-24. doi: 10.1007/s00210-015-1086-5. Epub 2015 Jan 31.


Antitumor activity of (R,R')-4-methoxy-1-naphthylfenoterol in a rat C6 glioma xenograft model in the mouse.

Bernier M, Paul RK, Dossou KS, Wnorowski A, Ramamoorthy A, Paris A, Moaddel R, Cloix JF, Wainer IW.

Pharmacol Res Perspect. 2013 Dec;1(2):e00010. doi: 10.1002/prp2.10. Epub 2013 Dec 5.


Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.

Jozwiak K, Targowska-Duda KM, Kaczor AA, Kozak J, Ligeza A, Szacon E, Wrobel TM, Budzynska B, Biala G, Fornal E, Poso A, Wainer IW, Matosiuk D.

Bioorg Med Chem. 2014 Dec 15;22(24):6846-56. doi: 10.1016/j.bmc.2014.10.036. Epub 2014 Oct 31.


Structure-bias relationships for fenoterol stereoisomers in six molecular and cellular assays at the β2-adrenoceptor.

Reinartz MT, Kälble S, Littmann T, Ozawa T, Dove S, Kaever V, Wainer IW, Seifert R.

Naunyn Schmiedebergs Arch Pharmacol. 2015 Jan;388(1):51-65. doi: 10.1007/s00210-014-1054-5. Epub 2014 Oct 24.


What is hydroxynorketamine and what can it bring to neurotherapeutics?

Singh NS, Zarate CA Jr, Moaddel R, Bernier M, Wainer IW.

Expert Rev Neurother. 2014 Nov;14(11):1239-42. doi: 10.1586/14737175.2014.971760.


Are basal D-serine plasma levels a predictive biomarker for the rapid antidepressant effects of ketamine and ketamine metabolites?

Wainer IW.

Psychopharmacology (Berl). 2014 Oct;231(20):4083-4. doi: 10.1007/s00213-014-3736-6. Epub 2014 Sep 11. No abstract available.


D-serine plasma concentration is a potential biomarker of (R,S)-ketamine antidepressant response in subjects with treatment-resistant depression.

Moaddel R, Luckenbaugh DA, Xie Y, Villaseñor A, Brutsche NE, Machado-Vieira R, Ramamoorthy A, Lorenzo MP, Garcia A, Bernier M, Torjman MC, Barbas C, Zarate CA Jr, Wainer IW.

Psychopharmacology (Berl). 2015 Jan;232(2):399-409. doi: 10.1007/s00213-014-3669-0. Epub 2014 Jul 24.


(R,S)-Ketamine metabolites (R,S)-norketamine and (2S,6S)-hydroxynorketamine increase the mammalian target of rapamycin function.

Paul RK, Singh NS, Khadeer M, Moaddel R, Sanghvi M, Green CE, O'Loughlin K, Torjman MC, Bernier M, Wainer IW.

Anesthesiology. 2014 Jul;121(1):149-59. doi: 10.1097/ALN.0000000000000285.


Tyrosine 308 is necessary for ligand-directed Gs protein-biased signaling of β2-adrenoceptor.

Woo AY, Jozwiak K, Toll L, Tanga MJ, Kozocas JA, Jimenez L, Huang Y, Song Y, Plazinska A, Pajak K, Paul RK, Bernier M, Wainer IW, Xiao RP.

J Biol Chem. 2014 Jul 11;289(28):19351-63. doi: 10.1074/jbc.M114.558882. Epub 2014 May 15.


Multiple protein stationary phases: a review.

Singh NS, Habicht KL, Dossou KS, Shimmo R, Wainer IW, Moaddel R.

J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Oct 1;968:64-8. doi: 10.1016/j.jchromb.2014.04.005. Epub 2014 Apr 13. Review.


A pilot study of plasma metabolomic patterns from patients treated with ketamine for bipolar depression: evidence for a response-related difference in mitochondrial networks.

Villaseñor A, Ramamoorthy A, Silva dos Santos M, Lorenzo MP, Laje G, Zarate C Jr, Barbas C, Wainer IW.

Br J Pharmacol. 2014 Apr;171(8):2230-42. doi: 10.1111/bph.12494.


Characterization of a multiple endogenously expressed adenosine triphosphate-binding cassette transporters using nuclear and cellular membrane affinity chromatography columns.

Habicht KL, Singh NS, Khadeer MA, Shimmo R, Wainer IW, Moaddel R.

J Chromatogr A. 2014 Apr 25;1339:80-85. doi: 10.1016/j.chroma.2014.02.076. Epub 2014 Mar 5.


Stereochemical and conformational study on fenoterol by ECD spectroscopy and TD-DFT calculations.

Tedesco D, Zanasi R, Wainer IW, Bertucci C.

J Pharm Biomed Anal. 2014 Mar;91:92-6. doi: 10.1016/j.jpba.2013.12.018. Epub 2013 Dec 30.


(R,R')-4'-methoxy-1-naphthylfenoterol targets GPR55-mediated ligand internalization and impairs cancer cell motility.

Paul RK, Wnorowski A, Gonzalez-Mariscal I, Nayak SK, Pajak K, Moaddel R, Indig FE, Bernier M, Wainer IW.

Biochem Pharmacol. 2014 Feb 15;87(4):547-61. doi: 10.1016/j.bcp.2013.11.020. Epub 2013 Dec 16.


Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor.

Plazinska A, Pajak K, Rutkowska E, Jimenez L, Kozocas J, Koolpe G, Tanga M, Toll L, Wainer IW, Jozwiak K.

Bioorg Med Chem. 2014 Jan 1;22(1):234-46. doi: 10.1016/j.bmc.2013.11.030. Epub 2013 Nov 23.


Development and validation of a sensitive LC-MS/MS method for the determination of D-serine in human plasma.

Xie Y, Alexander GM, Schwartzman RJ, N Singh, Torjman MC, Goldberg ME, Wainer IW, Moaddel R.

J Pharm Biomed Anal. 2014 Feb;89:1-5. doi: 10.1016/j.jpba.2013.10.028. Epub 2013 Oct 30.


Molecular interactions between fenoterol stereoisomers and derivatives and the β₂-adrenergic receptor binding site studied by docking and molecular dynamics simulations.

Plazinska A, Kolinski M, Wainer IW, Jozwiak K.

J Mol Model. 2013 Nov;19(11):4919-30. doi: 10.1007/s00894-013-1981-y. Epub 2013 Sep 17.


Nicotinic acetylcholine receptor antagonists alter the function and expression of serine racemase in PC-12 and 1321N1 cells.

Singh NS, Paul RK, Ramamoorthy A, Torjman MC, Moaddel R, Bernier M, Wainer IW.

Cell Signal. 2013 Dec;25(12):2634-45. doi: 10.1016/j.cellsig.2013.08.025. Epub 2013 Sep 4.


Interview with Irving W Wainer.

Wainer IW.

Bioanalysis. 2013 Aug;5(16):1949-52. doi: 10.4155/bio.13.135.


Development and validation of a sensitive LC-MS/MS method for the determination of fenoterol in human plasma and urine samples.

Sanghvi M, Ramamoorthy A, Strait J, Wainer IW, Moaddel R.

J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Aug 15;933:37-43. doi: 10.1016/j.jchromb.2013.06.020. Epub 2013 Jun 26.


Gabapentin and (S)-pregabalin decrease intracellular D-serine concentrations in PC-12 cells.

Singh NS, Paul RK, Torjman MC, Wainer IW.

Neurosci Lett. 2013 Feb 22;535:90-4. doi: 10.1016/j.neulet.2012.12.024. Epub 2012 Dec 27.


Sub-anesthetic concentrations of (R,S)-ketamine metabolites inhibit acetylcholine-evoked currents in α7 nicotinic acetylcholine receptors.

Moaddel R, Abdrakhmanova G, Kozak J, Jozwiak K, Toll L, Jimenez L, Rosenberg A, Tran T, Xiao Y, Zarate CA, Wainer IW.

Eur J Pharmacol. 2013 Jan 5;698(1-3):228-34. doi: 10.1016/j.ejphar.2012.11.023. Epub 2012 Nov 23.


The synthesis and characterization of a nuclear membrane affinity chromatography column for the study of human breast cancer resistant protein (BCRP) using nuclear membranes obtained from the LN-229 cells.

Habicht KL, Frazier C, Singh N, Shimmo R, Wainer IW, Moaddel R.

J Pharm Biomed Anal. 2013 Jan;72:159-62. doi: 10.1016/j.jpba.2012.10.001. Epub 2012 Oct 8.


Cannabinoid receptor activation correlates with the proapoptotic action of the β2-adrenergic agonist (R,R')-4-methoxy-1-naphthylfenoterol in HepG2 hepatocarcinoma cells.

Paul RK, Ramamoorthy A, Scheers J, Wersto RP, Toll L, Jimenez L, Bernier M, Wainer IW.

J Pharmacol Exp Ther. 2012 Oct;343(1):157-66. doi: 10.1124/jpet.112.195206. Epub 2012 Jul 9.


The stereoselective sulfate conjugation of 4'-methoxyfenoterol stereoisomers by sulfotransferase enzymes.

Iyer LV, Ramamoorthy A, Rutkowska E, Furimsky AM, Tang L, Catz P, Green CE, Jozwiak K, Wainer IW.

Chirality. 2012 Oct;24(10):796-803. doi: 10.1002/chir.22072. Epub 2012 Jun 29.


Stereoselective and regiospecific hydroxylation of ketamine and norketamine.

Desta Z, Moaddel R, Ogburn ET, Xu C, Ramamoorthy A, Venkata SL, Sanghvi M, Goldberg ME, Torjman MC, Wainer IW.

Xenobiotica. 2012 Nov;42(11):1076-87. doi: 10.3109/00498254.2012.685777. Epub 2012 May 21.


Relationship of ketamine's plasma metabolites with response, diagnosis, and side effects in major depression.

Zarate CA Jr, Brutsche N, Laje G, Luckenbaugh DA, Venkata SL, Ramamoorthy A, Moaddel R, Wainer IW.

Biol Psychiatry. 2012 Aug 15;72(4):331-8. doi: 10.1016/j.biopsych.2012.03.004. Epub 2012 Apr 18.


The rapid and direct determination of ATPase activity by ion exchange chromatography and the application to the activity of heat shock protein-90.

Bartolini M, Wainer IW, Bertucci C, Andrisano V.

J Pharm Biomed Anal. 2013 Jan 25;73:77-81. doi: 10.1016/j.jpba.2012.03.021. Epub 2012 Mar 21.


Thermodynamics and docking of agonists to the β(2)-adrenoceptor determined using [(3)H](R,R')-4-methoxyfenoterol as the marker ligand.

Toll L, Pajak K, Plazinska A, Jozwiak K, Jimenez L, Kozocas JA, Tanga MJ, Bupp JE, Wainer IW.

Mol Pharmacol. 2012 Jun;81(6):846-54. doi: 10.1124/mol.111.077347. Epub 2012 Mar 20.


Breast cancer resistance protein (BCRP/ABCG2) localises to the nucleus in glioblastoma multiforme cells.

Bhatia P, Bernier M, Sanghvi M, Moaddel R, Schwarting R, Ramamoorthy A, Wainer IW.

Xenobiotica. 2012 Aug;42(8):748-55. doi: 10.3109/00498254.2012.662726. Epub 2012 Mar 8.


Simultaneous population pharmacokinetic modelling of ketamine and three major metabolites in patients with treatment-resistant bipolar depression.

Zhao X, Venkata SL, Moaddel R, Luckenbaugh DA, Brutsche NE, Ibrahim L, Zarate CA Jr, Mager DE, Wainer IW.

Br J Clin Pharmacol. 2012 Aug;74(2):304-14. doi: 10.1111/j.1365-2125.2012.04198.x.


Capillary electrophoresis-laser-induced fluorescence (CE-LIF) assay for measurement of intracellular D-serine and serine racemase activity.

Singh NS, Paul RK, Sichler M, Moaddel R, Bernier M, Wainer IW.

Anal Biochem. 2012 Feb 15;421(2):460-6. doi: 10.1016/j.ab.2011.10.003. Epub 2011 Oct 10.


The development and characterization of protein-based stationary phases for studying drug-protein and protein-protein interactions.

Sanghvi M, Moaddel R, Wainer IW.

J Chromatogr A. 2011 Dec 9;1218(49):8791-8. doi: 10.1016/j.chroma.2011.05.067. Epub 2011 May 27. Review.

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