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Synthetic Cathinone Analogues Structurally Related to the Central Stimulant Methylphenidate as Dopamine Reuptake Inhibitors.

Yadav-Samudrala BJ, Eltit JM, Glennon RA.

ACS Chem Neurosci. 2019 Aug 15. doi: 10.1021/acschemneuro.9b00284. [Epub ahead of print]


Revised Pharmacophore Model for 5-HT2A Receptor Antagonists Derived from the Atypical Antipsychotic Agent Risperidone.

Shah UH, Gaitonde SA, Moreno JL, Glennon RA, Dukat M, González-Maeso J.

ACS Chem Neurosci. 2019 May 15;10(5):2318-2331. doi: 10.1021/acschemneuro.8b00637. Epub 2019 Jan 16.


Systematic Structure-Activity Studies on Selected 2-, 3-, and 4-Monosubstituted Synthetic Methcathinone Analogs as Monoamine Transporter Releasing Agents.

Walther D, Shalabi AR, Baumann MH, Glennon RA.

ACS Chem Neurosci. 2019 Jan 16;10(1):740-745. doi: 10.1021/acschemneuro.8b00524. Epub 2018 Nov 7.


des-Formylflustrabromine (dFBr): A Structure-Activity Study on Its Ability To Potentiate the Action of Acetylcholine at α4β2 Nicotinic Acetylcholine Receptors.

Dukat M, Jain A, German N, Ferrara-Pontoriero R, Huang Y, Ma Y, Schulte MK, Glennon RA.

ACS Chem Neurosci. 2018 Dec 19;9(12):2984-2996. doi: 10.1021/acschemneuro.8b00156. Epub 2018 Aug 2.


Effects of N-Alkyl-4-Methylamphetamine Optical Isomers on Plasma Membrane Monoamine Transporters and Abuse-Related Behavior.

Battisti UM, Sitta R, Harris A, Sakloth F, Walther D, Ruchala I, Negus SS, Baumann MH, Glennon RA, Eltit JM.

ACS Chem Neurosci. 2018 Jul 18;9(7):1829-1839. doi: 10.1021/acschemneuro.8b00138. Epub 2018 May 14.


N-Alkylated Analogs of 4-Methylamphetamine (4-MA) Differentially Affect Monoamine Transporters and Abuse Liability.

Solis E Jr, Partilla JS, Sakloth F, Ruchala I, Schwienteck KL, De Felice LJ, Eltit JM, Glennon RA, Negus SS, Baumann MH.

Neuropsychopharmacology. 2017 Sep;42(10):1950-1961. doi: 10.1038/npp.2017.98. Epub 2017 May 22.


The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.

Glennon RA.

J Med Chem. 2017 Apr 13;60(7):2605-2628. doi: 10.1021/acs.jmedchem.7b00085. Epub 2017 Mar 15.


Deconstructed Analogues of Bupropion Reveal Structural Requirements for Transporter Inhibition versus Substrate-Induced Neurotransmitter Release.

Shalabi AR, Walther D, Baumann MH, Glennon RA.

ACS Chem Neurosci. 2017 Jun 21;8(6):1397-1403. doi: 10.1021/acschemneuro.7b00055. Epub 2017 Feb 27.


Synthetic Cathinones: A Brief Overview of Overviews with Applications to the Forensic Sciences.

Glennon RA, Dukat M.

Ann Forensic Res Anal. 2017;4(2). pii: 1040. Epub 2017 Mar 21.


Structure-Activity Relationships of Synthetic Cathinones.

Glennon RA, Dukat M.

Curr Top Behav Neurosci. 2017;32:19-47. doi: 10.1007/7854_2016_41.


Reformulating a Pharmacophore for 5-HT2A Serotonin Receptor Antagonists.

Younkin J, Gaitonde SA, Ellaithy A, Vekariya R, Baki L, Moreno JL, Shah S, Drossopoulos P, Hideshima KS, Eltit JM, González-Maeso J, Logothetis DE, Dukat M, Glennon RA.

ACS Chem Neurosci. 2016 Sep 21;7(9):1292-9. doi: 10.1021/acschemneuro.6b00162. Epub 2016 Jul 19.


Neurobiology of 3,4-methylenedioxypyrovalerone (MDPV) and α-pyrrolidinovalerophenone (α-PVP).

Glennon RA, Young R.

Brain Res Bull. 2016 Sep;126(Pt 1):111-126. doi: 10.1016/j.brainresbull.2016.04.011. Epub 2016 Apr 29. Review.


Abuse-related neurochemical and behavioral effects of cathinone and 4-methylcathinone stereoisomers in rats.

Hutsell BA, Baumann MH, Partilla JS, Banks ML, Vekariya R, Glennon RA, Negus SS.

Eur Neuropsychopharmacol. 2016 Feb;26(2):288-297. doi: 10.1016/j.euroneuro.2015.12.010. Epub 2015 Dec 11.


Abuse-Related Neurochemical Effects of Para-Substituted Methcathinone Analogs in Rats: Microdialysis Studies of Nucleus Accumbens Dopamine and Serotonin.

Suyama JA, Sakloth F, Kolanos R, Glennon RA, Lazenka MF, Negus SS, Banks ML.

J Pharmacol Exp Ther. 2016 Jan;356(1):182-90. doi: 10.1124/jpet.115.229559. Epub 2015 Oct 15.


Ocular Hypotensive Response in Nonhuman Primates of (8R)-1-[(2S)-2-Aminopropyl]-8,9-dihydro-7H-pyrano[2,3-g]indazol-8-ol a Selective 5-HT2 Receptor Agonist.

May JA, Sharif NA, McLaughlin MA, Chen HH, Severns BS, Kelly CR, Holt WF, Young R, Glennon RA, Hellberg MR, Dean TR.

J Med Chem. 2015 Nov 25;58(22):8818-33. doi: 10.1021/acs.jmedchem.5b00857. Epub 2015 Nov 9.


Structural Modification of the Designer Stimulant α-Pyrrolidinovalerophenone (α-PVP) Influences Potency at Dopamine Transporters.

Kolanos R, Sakloth F, Jain AD, Partilla JS, Baumann MH, Glennon RA.

ACS Chem Neurosci. 2015 Oct 21;6(10):1726-31. doi: 10.1021/acschemneuro.5b00160. Epub 2015 Aug 11.


Desformylflustrabromine (dFBr) and [3H]dFBr-Labeled Binding Sites in a Nicotinic Acetylcholine Receptor.

Hamouda AK, Wang ZJ, Stewart DS, Jain AD, Glennon RA, Cohen JB.

Mol Pharmacol. 2015 Jul;88(1):1-11. doi: 10.1124/mol.115.098913. Epub 2015 Apr 13. Erratum in: Mol Pharmacol. 2016 Jan;89(1):141.


Stereoselective Actions of Methylenedioxypyrovalerone (MDPV) To Inhibit Dopamine and Norepinephrine Transporters and Facilitate Intracranial Self-Stimulation in Rats.

Kolanos R, Partilla JS, Baumann MH, Hutsell BA, Banks ML, Negus SS, Glennon RA.

ACS Chem Neurosci. 2015 May 20;6(5):771-7. doi: 10.1021/acschemneuro.5b00006. Epub 2015 Mar 3.


Structural analysis of dopamine- and amphetamine-induced depolarization currents in the human dopamine transporter.

Tang QY, Kolanos R, De Felice LJ, Glennon RA.

ACS Chem Neurosci. 2015 Apr 15;6(4):551-8. doi: 10.1021/cn500282f. Epub 2015 Feb 23.


Steric parameters, molecular modeling and hydropathic interaction analysis of the pharmacology of para-substituted methcathinone analogues.

Sakloth F, Kolanos R, Mosier PD, Bonano JS, Banks ML, Partilla JS, Baumann MH, Negus SS, Glennon RA.

Br J Pharmacol. 2015 May;172(9):2210-8. doi: 10.1111/bph.13043. Epub 2015 Feb 27.


Quantitative structure-activity relationship analysis of the pharmacology of para-substituted methcathinone analogues.

Bonano JS, Banks ML, Kolanos R, Sakloth F, Barnier ML, Glennon RA, Cozzi NV, Partilla JS, Baumann MH, Negus SS.

Br J Pharmacol. 2015 May;172(10):2433-44. doi: 10.1111/bph.13030. Epub 2015 Apr 10.


Effects of the neuropeptide S receptor antagonist RTI-118 on abuse-related facilitation of intracranial self-stimulation produced by cocaine and methylenedioxypyrovalerone (MDPV) in rats.

Bonano JS, Runyon SP, Hassler C, Glennon RA, Stevens Negus S.

Eur J Pharmacol. 2014 Nov 15;743:98-105. doi: 10.1016/j.ejphar.2014.09.006. Epub 2014 Sep 16.


Receptor-ligand interaction at 5-HT3 serotonin receptors: a cluster approach.

Rao BK, Samanta D, Joshi S, Basu K, Baldwin SD, Jha A, Dukat M, Glennon RA, Jena P.

J Phys Chem A. 2014 Sep 18;118(37):8471-6. doi: 10.1021/jp5017906. Epub 2014 Jun 10.


Electrical coupling between the human serotonin transporter and voltage-gated Ca(2+) channels.

Ruchala I, Cabra V, Solis E Jr, Glennon RA, De Felice LJ, Eltit JM.

Cell Calcium. 2014 Jul;56(1):25-33. doi: 10.1016/j.ceca.2014.04.003. Epub 2014 Apr 27.


Synthetic cathinones: chemical phylogeny, physiology, and neuropharmacology.

De Felice LJ, Glennon RA, Negus SS.

Life Sci. 2014 Feb 27;97(1):20-6. doi: 10.1016/j.lfs.2013.10.029. Epub 2013 Nov 11. Review.


"Deconstruction" of the abused synthetic cathinone methylenedioxypyrovalerone (MDPV) and an examination of effects at the human dopamine transporter.

Kolanos R, Solis E Jr, Sakloth F, De Felice LJ, Glennon RA.

ACS Chem Neurosci. 2013 Dec 18;4(12):1524-9. doi: 10.1021/cn4001236. Epub 2013 Oct 31.


Abuse-related and abuse-limiting effects of methcathinone and the synthetic "bath salts" cathinone analogs methylenedioxypyrovalerone (MDPV), methylone and mephedrone on intracranial self-stimulation in rats.

Bonano JS, Glennon RA, De Felice LJ, Banks ML, Negus SS.

Psychopharmacology (Berl). 2014 Jan;231(1):199-207. doi: 10.1007/s00213-013-3223-5. Epub 2013 Aug 15.


Mephedrone and methylenedioxypyrovalerone (MDPV), major constituents of "bath salts," produce opposite effects at the human dopamine transporter.

Cameron K, Kolanos R, Vekariya R, De Felice L, Glennon RA.

Psychopharmacology (Berl). 2013 Jun;227(3):493-9. doi: 10.1007/s00213-013-2967-2. Epub 2013 Jan 31. Erratum in: Psychopharmacology (Berl). 2013 Jun;227(3):447. Verkariya, Rakesh [corrected to Vekariya, Rakesh].


Bath salts components mephedrone and methylenedioxypyrovalerone (MDPV) act synergistically at the human dopamine transporter.

Cameron KN, Kolanos R, Solis E Jr, Glennon RA, De Felice LJ.

Br J Pharmacol. 2013 Apr;168(7):1750-7. doi: 10.1111/bph.12061.


Deconstruction of the α4β2 nicotinic acetylcholine receptor positive allosteric modulator desformylflustrabromine.

German N, Kim JS, Jain A, Dukat M, Pandya A, Ma Y, Weltzin M, Schulte MK, Glennon RA.

J Med Chem. 2011 Oct 27;54(20):7259-67. doi: 10.1021/jm200834x. Epub 2011 Oct 3.


Distribution, level, pharmacology, regulation, and signaling of 5-HT6 receptors in rats and marmosets with special reference to an experimental model of parkinsonism.

Zhang X, Andren PE, Glennon RA, Svenningsson P.

J Comp Neurol. 2011 Jun 15;519(9):1816-27. doi: 10.1002/cne.22605.


Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships.

Klein MT, Dukat M, Glennon RA, Teitler M.

J Pharmacol Exp Ther. 2011 Jun;337(3):860-7. doi: 10.1124/jpet.111.179606. Epub 2011 Mar 21.


MD-354 selectively antagonizes the antinociceptive effects of (-)nicotine in the mouse tail-flick assay.

Dukat M, Wesołowska A, Alley G, Young S, Abdrakhmanova GR, Navarro HA, Young R, Glennon RA.

Psychopharmacology (Berl). 2010 Jul;210(4):547-57. doi: 10.1007/s00213-010-1857-0. Epub 2010 Apr 30.


The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs.

Glennon RA, Siripurapu U, Roth BL, Kolanos R, Bondarev ML, Sikazwe D, Lee M, Dukat M.

Curr Top Med Chem. 2010;10(5):579-95. Review.


Design, synthesis, and preliminary pharmacological evaluation of new imidazolinones as L-DOPA prodrugs.

Giorgioni G, Claudi F, Ruggieri S, Ricciutelli M, Palmieri GF, Di Stefano A, Sozio P, Cerasa LS, Chiavaroli A, Ferrante C, Orlando G, Glennon RA.

Bioorg Med Chem. 2010 Mar 1;18(5):1834-43. doi: 10.1016/j.bmc.2010.01.041. Epub 2010 Jan 25.


Interaction of the sigma(2) receptor ligand PB28 with the human nucleosome: computational and experimental probes of interaction with the H2A/H2B dimer.

Abate C, Elenewski J, Niso M, Berardi F, Colabufo NA, Azzariti A, Perrone R, Glennon RA.

ChemMedChem. 2010 Feb 1;5(2):268-73. doi: 10.1002/cmdc.200900402.


A structure-affinity and comparative molecular field analysis of sigma-2 (sigma2) receptor ligands.

Abate C, Mosier PD, Berardi F, Glennon RA.

Cent Nerv Syst Agents Med Chem. 2009 Sep;9(3):246-57.


The enigmatic sigma receptors.

Glennon RA.

Cent Nerv Syst Agents Med Chem. 2009 Sep;9(3):159-60. No abstract available.


Predicting new molecular targets for known drugs.

Keiser MJ, Setola V, Irwin JJ, Laggner C, Abbas AI, Hufeisen SJ, Jensen NH, Kuijer MB, Matos RC, Tran TB, Whaley R, Glennon RA, Hert J, Thomas KL, Edwards DD, Shoichet BK, Roth BL.

Nature. 2009 Nov 12;462(7270):175-81. doi: 10.1038/nature08506. Epub 2009 Nov 1.


S(-)Propranolol as a discriminative stimulus and its comparison to the stimulus effects of cocaine in rats.

Young R, Glennon RA.

Psychopharmacology (Berl). 2009 Apr;203(2):369-82. doi: 10.1007/s00213-008-1317-2. Epub 2008 Sep 16.


Effect of 8-hydroxy-2-(N,N-di-n-propylamino)tetralin and MDMA on the discriminative stimulus effects of the classical hallucinogen DOM in rats.

Khorana N, Young R, Glennon RA.

Pharmacol Biochem Behav. 2009 Jan;91(3):385-92. doi: 10.1016/j.pbb.2008.08.013. Epub 2008 Aug 17.


Pharmacological properties and discriminative stimulus effects of a novel and selective 5-HT2 receptor agonist AL-38022A [(S)-2-(8,9-dihydro-7H-pyrano[2,3-g]indazol-1-yl)-1-methylethylamine].

May JA, Sharif NA, Chen HH, Liao JC, Kelly CR, Glennon RA, Young R, Li JX, Rice KC, France CP.

Pharmacol Biochem Behav. 2009 Jan;91(3):307-14. doi: 10.1016/j.pbb.2008.07.015. Epub 2008 Jul 30.


Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.

Dukat M, Mosier PD, Kolanos R, Roth BL, Glennon RA.

J Med Chem. 2008 Feb 14;51(3):603-11. doi: 10.1021/jm070910s. Epub 2008 Jan 18.


Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.

Kim JS, Padnya A, Weltzin M, Edmonds BW, Schulte MK, Glennon RA.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4855-60. Epub 2007 Jun 14.


The 5-HT3 receptor partial agonist MD-354 (meta-chlorophenylguanidine) enhances the discriminative stimulus actions of (+)amphetamine in rats.

Dukat M, Wesolowska A, Young R, Glennon RA.

Pharmacol Biochem Behav. 2007 Jun-Jul;87(2):203-7. Epub 2007 Mar 30.


MD-354: what is it good for?

Dukat M, Glennon RA, Young S.

CNS Drug Rev. 2007 Spring;13(1):1-20. Review.

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