Recent papers:
A pharmacological organization of G protein-coupled receptors.
Lin H, Sassano MF, Roth BL, Shoichet BK.
Nat Methods. 2013 Feb;10(2):140-6. doi: 10.1038/nmeth.2324. Epub 2013 Jan 6.
Conformational ensembles in GPCR activation.
Vardy E, Roth BL.
Cell. 2013 Jan 31;152(3):385-6. doi: 10.1016/j.cell.2013.01.025.
Automated design of ligands to polypharmacological profiles.
Besnard J, Ruda GF, Setola V, Abecassis K, Rodriguiz RM, Huang XP, Norval S, Sassano MF, Shin AI, Webster LA, Simeons FR, Stojanovski L, Prat A, Seidah NG, Constam DB, Bickerton GR, Read KD, Wetsel WC, Gilbert IH, Roth BL, Hopkins AL.
Nature. 2012 Dec 13;492(7428):215-20. doi: 10.1038/nature11691.
NOBEL 2012 Chemistry: Studies of a ubiquitous receptor family.
Roth BL, Marshall FH.
Nature. 2012 Dec 6;492(7427):57. doi: 10.1038/492057a.
Identifying mechanism-of-action targets for drugs and probes.
Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK.
Proc Natl Acad Sci U S A. 2012 Jun 18. [Epub ahead of print]
Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic.
Thompson AA, Liu W, Chun E, Katritch V, Huixian Wu H, Vardy E, Huang X, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V & Stevens RC.
Nature. 2012 May 17;485(7398):395-99. doi:10.1038/nature11085
Structure of the human κ-opioid receptor in complex with JDTic.
Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA,
Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL,
Cherezov V, Stevens RC.
Nature. 2012 Mar 21;485(7398):327-32. doi: 10.1038/nature10939.
Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons.
Huang HS, Allen JA, Mabb AM, King IF, Miriyala J, Taylor-Blake B, Sciaky N, Dutton JW, Lee HM, Chen X, Jin J, Bridges AS, Zylka MJ, Roth BL, Philpot BD.
Nature. 2011 Dec 21;481(7380):185-9. doi: 10.1038/nature10726.
Ligand discovery from a dopamine D(3) receptor homology model and crystal structure.
Carlsson J, Coleman RG, Setola V, Irwin JJ, Fan H, Schlessinger A, Sali A, Roth BL, Shoichet BK.
Nat Chem Biol. 2011 Sep 18;7(11):769-78. doi: 10.1038/nchembio.662.
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Vedadi M, Barsyte-Lovejoy D, Liu F, Rival-Gervier S, Allali-Hassani A, Labrie V, Wigle TJ,
Dimaggio PA, Wasney GA, Siarheyeva A, Dong A, Tempel W, Wang SC, Chen X, Chau I, Mangano TJ,
Huang XP, Simpson CD, Pattenden SG, Norris JL, Kireev DB, Tripathy A, Edwards A, Roth BL,
Janzen WP, Garcia BA, Petronis A, Ellis J, Brown PJ, Frye SV, Arrowsmith CH, Jin J.
Nat Chem Biol. 2011 Jul 10;7(8):566-74. doi: 10.1038/nchembio.599.
Vision and olfaction say UNC-le to G proteins.
Vardy E, Roth BL.
Nat Neurosci. 2011 Jun 27;14(7):805-6. doi: 10.1038/nn.2863.
Design, synthesis, and validation of a β-turn mimetic library targeting
protein-protein and peptide-receptor interactions.
Whitby LR, Ando Y, Setola V, Vogt PK, Roth BL, Boger DL.
J Am Chem Soc. 2011 Jul 6;133(26):10184-94.
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.
Endocrine Regulation of Male Fertility by the Skeleton.
Oury F, Sumara G, Sumara O, Ferron M, Chang H, Smith CE, Hermo L, Suarez S, Roth BL, Ducy P, Karsenty G.
Cell. 2011 Mar 4;144(5):796-809. Epub 2011 Feb 17.
Transient neuronal inhibition reveals opposing roles of indirect and direct pathways in sensitization.
Ferguson SM, Eskenazi D, Ishikawa M, Wanat MJ, Phillips PE, Dong Y, Roth BL, Neumaier JF.
Nat Neurosci. 2011 Jan;14(1):22-4. Epub 2010 Dec 5.
Rapid modulation of spine morphology by the 5-HT2A serotonin receptor through kalirin-7 signaling.
Jones KA, Srivastava DP, Allen JA, Strachan RT, Roth BL, Penzes P.
Proc Natl Acad Sci U S A. 2009 Nov 17;106(46):19575-80. Epub 2009 Nov 4.
A chemical-genetic approach to study G protein regulation of β cell function in vivo
Guettier JM, Gautam D, Scarselli M, Ruiz de Azua I, Li JH, Rosemond E, Ma X, Gonzalez FJ,
Armbruster BN, Lu H, Roth BL, Wess J.
Proc Natl Acad Sci U S A. 2009 Nov 10;106(45):19197-202. Epub 2009 Oct 26.
Remote control of neuronal activity in transgenic mice expressing evolved G protein-coupled receptors.
Alexander GM, Rogan SC, Abbas AI, Armbruster BN, Pei Y, Allen JA, Nonneman RJ, Hartmann J, Moy SS,
Nicolelis MA, McNamara JO, Roth BL.
Neuron. 2009 Jul 16;63(1):27-39.
Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine
2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling.
Strachan RT, Sheffler DJ, Willard B, Kinter M, Kiselar JG, Roth BL.
J Biol Chem. 2009 Feb 27;284(9):5557-73. Epub 2008 Dec 22.
The Expanded Biology of Serotonin
Berger M, Gray JA, Roth BL.
Annu Rev Med. 2009;60:355-66.
Protein engineering: electrifying cell receptors.
Abbas A, Roth BL.
Nat Nanotechnol. 2008 Oct;3(10):587-8.
Engineering GPCR signaling pathways with RASSLs.
Conklin BR, Hsiao EC, Claeysen S, Dumuis A, Srinivasan S, Forsayeth JR, Guettier JM, Chang WC, Pei Y, McCarthy KD, Nissenson RA, Wess J, Bockaert J, Roth BL.
Nat Methods. 2008 Aug;5(8):673-8.
Arresting serotonin.
Abbas A, Roth BL.
Proc Natl Acad Sci U S A. 2008 Jan 22;105(3):831-2. Epub 2008 Jan 14.
Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand.
Armbruster BN, Li X, Pausch MH, Herlitze S, Roth BL.
Proc Natl Acad Sci U S A. 2007 Mar 20;104(12):5163-8. Epub 2007 Mar 2.
Relating protein pharmacology by ligand chemistry.
Keiser MJ, Roth BL, Armbruster BN, Ernsberger P, Irwin JJ, Shoichet BK.
Nat Biotechnol. 2007 Feb;25(2):197-206.
Drugs and valvular heart disease.
Roth BL
N Engl J Med. 2007 Jan 4;356(1):6-9.
Why Academic Drug Discovery Makes Sense
Kozikowski AP, Roth B, Tropsha A
Science. 2006 Sep 1;313(5791):1235-6
p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling
Sheffler DJ, Kroeze WK, Garcia BG, Deutch AY, Hufeisen SJ, Leahy P, Brüning JC, Roth BL.
Proc Natl Acad Sci U S A. 2006 Mar 21;103(12):4717-22. Epub 2006 Mar 10.
Nigrostriatal Dopaminergic Deficits and Hypokinesia Caused by Inactivation of the Familial Parkinsonism-Linked Gene DJ-1.
Goldberg MS, Pisani A, Haburcak M, Vortherms TA, Kitada T, Costa C,
Tong Y, Martella G, Tscherter A, Martins A, Bernardi G, Roth BL, Pothos EN, Calabresi P, Shen J.
Neuron. 2005 Feb 17;45(4):489-96
Finding new tricks for old drugs: an efficient route for public-sector drug discovery.
O'connor KA, Roth BL.
Nat Rev Drug Discov. 2005 Dec;4(12):1005-14
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Gobbi G, Bambico FR, Mangieri R, Bortolato M, Campolongo P, Solinas M, Cassano T, Morgese MG, Debonnel G, Duranti A,
Tontini A, Tarzia G, Mor M, Trezza V, Goldberg SR, Cuomo V, Piomelli D.
Proc Natl Acad Sci U S A. 2005 Dec 20;102(51):18620-5. Epub 2005 Dec 13.
The human polyomavirus, JCV, uses serotonin receptors to infect cells.
Elphick GF, Querbes W, Jordan JA, Gee GV, Eash S, Manley K, Dugan A, Stanifer M, Bhatnagar A, Kroeze WK, Roth BL, Atwood WJ.
Science. 2004 Nov 19;306(5700):1380-3.
Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia.
Roth BL, Sheffler DJ, Kroeze WK.
Nat Rev Drug Discov. 2004 Apr;3(4):353-9.
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Roth BL, Baner K, Westkaemper R, Siebert D, Rice KC, Steinberg S, Ernsberger P, Rothman RB.
Proc Natl Acad Sci U S A 2002 Sep 3;99(18):11934-9
Others:
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
Kulkarni SS, Newman AH.
Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91. Epub 2007 Mar 24.
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.
Kulkarni SS, Newman AH.
Bioorg Med Chem Lett. 2007 Apr 1;17(7):2074-9. Epub 2007 Jan 4
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II:
Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors
Carato P, Graulich A, Jensen N, Roth BL, Liegeois JF.
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1570-4. Epub 2007 Jan 8.
Synthesis and in vitro binding studies of substituted piperidine naphthamides.
Part I: Influence of the substitution on the basic nitrogen and the position of the
amide on the affinity for D2L, D4.2, and 5-HT2A receptors.
Carato P, Graulich A, Jensen N, Roth BL, Liegeois JF.
Bioorg Med Chem Lett. Mar 15;17(6):1565-9. Epub 2007 Jan 8.
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Kulkarni SS, Nightingale B, Dersch CM, Rothman RB, Newman AH.
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. Epub 2006 May 5.
Synthesis and Structure-Activity Relationships of 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine Analogues as Potent,
Noncompetitive Metabotropic Glutamate Receptor Subtype 5 Antagonists; Search for Cocaine Medications.
Iso Y, Grajkowska E, Wroblewski JT, Davis J, Goeders NE, Johnson KM, Sanker S, Roth BL, Tueckmantel W, Kozikowski AP.
J Med Chem. 2006 Feb 9;49(3):1080-100
Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors.
Pullagurla M, Siripurapu U, Kolanos R, Bondarev ML, Dukat M, Setola V, Roth BL, Glennon RA
Bioorg Med Chem Lett. 2005 Dec 1;15(23):5298-302. Epub 2005 Sep 23.
Synthesis of a Library of Complex Macrodiolides Employing Cyclodimerization of Hydroxy Esters.
Beeler AB, Acquilano DE, Su Q, Yan F, Roth BL, Panek JS, Porco JA Jr.
J Comb Chem. 2005 Sep-Oct;7(5):673-81
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Huang Y, Bae SA, Roth BL, Laruelle M
Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9
SAR of psilocybin analogs: Discovery of a selective 5-HT2C agonist.
Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, Shuster L
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.
Evidence for the Preferential Involvement of 5-HT2A Serotonin Receptors in Stress- and Drug-Induced Dopamine
Release in the Rat Medial Prefrontal Cortex.
Pehek EA, Nocjar C, Roth BL, Byrd TA, Mabrouk OS.
Neuropsychopharmacology. 2006 Feb;31(2):265-77.
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship
study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.
Huang Y, Bae SA, Zhu Z, Guo N, Roth BL, Laruelle M.
J Med Chem. 2005 Apr 7;48(7):2559-70
Development of a rationally designed, low abuse potential, biogenic amine releaser that suppresses cocaine self-administration.
Rothman RB, Blough BE, Woolverton WL, Anderson KG, Negus SS, Mello NK, Roth BL, Baumann MH
J Pharmacol Exp Ther. 2005 Jun;313(3):1361-9. Epub 2005 Mar 10.
A PHYTOCHEMICAL STUDY OF SALVIA DIVINORUM
Jeremy Stewart, Franck E. Dayan, Bryan L. Roth, and Jordan K. Zjawiony
in press
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands
Lee M, Rangisetty JB, Pullagurla MR, Dukat M, Setola V, Roth BL, Glennon RA.
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1707-11
Studies toward the Pharmacophore of Salvinorin A, a
Potent k Opioid Receptor Agonist
Munro TA, Rizzacasa MA, Roth BL, Toth BA, Yan F.
J Med Chem. 2005 Jan 27;48(2):345-8.
Haloperidol: towards further understanding of the structural contributions of its pharmacophoric
elements at D2-like receptors.
Sikazwe DM, Li S, Mardenborough L, Cody V, Roth BL, Ablordeppey SY
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5739-42.
A PET imaging agent with fast kinetics: synthesis and in vivo evaluation of the serotonin transporter ligand
[11C]2-[2-dimethylaminomethylphenylthio)]-5-fluorophenylamine ([11C]AFA).
Huang Y, Narendran R, Bae SA, Erritzoe D, Guo N, Zhu Z, Hwang DR, Laruelle M.
Nucl Med Biol. 2004 Aug;31(6):727-38.
Three putative N-glycosylation sites within the murine 5-HT3A receptor sequence affect plasma
membrane targeting, ligand binding, and calcium influx in heterologous mammalian cells.
Quirk PL, Rao S, Roth BL, Siegel RE.
J Neurosci Res. 2004 Aug 15;77(4):498-506.
A new positron emission tomography imaging agent for the serotonin transporter: synthesis, pharmacological
characterization, and kinetic analysis of [11C]2-[2-(dimethylaminomethyl)phenylthio]-5-fluoromethylphenylamine
([11C]AFM).
Huang Y, Hwang DR, Bae SA, Sudo Y, Guo N, Zhu Z, Narendran R, Laruelle M.
Nucl Med Biol. 2004 Jul;31(5):543-56.
Serotonin receptors represent highly favorable molecular targets for cognitive enhancement in
schizophrenia and other disorders.
Roth BL, Hanizavareh SM, Blum AE.
Psychopharmacology (Berl). 2004 Jun;174(1):17-24. Epub 2003 Dec 02.
Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds:
a novel approach for CNS drug discovery.
Roth BL, Lopez E, Beischel S, Westkaemper RB, Evans JM.
Pharmacol Ther. 2004 May;102(2):99-110.
The Neurotensin Agonist PD149163 Increases Fos Expression in the Prefrontal Cortex of the Rat.
Petrie KA, Bubser M, Casey CD, Davis MD, Roth BL, Deutch AY.
Neuropsychopharmacology. 2004 Oct;29(10):1878-88.
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-
pyrrolidine (SpAMDA).
Peddi S, Roth BL, Glennon RA, Westkaemper RB.
Bioorg Med Chem Lett. 2004 May 3;14(9):2279-83.
Salvinorin A, an active component of the hallucinogenic sage salvia divinorum is a highly efficacious
kappa-opioid receptor agonist: structural and functional considerations.
Chavkin C, Sud S, Jin W, Stewart J, Zjawiony JK, Siebert DJ, Toth BA, Hufeisen SJ, Roth BL.
J Pharmacol Exp Ther. 2004 Mar;308(3):1197-203. Epub 2004 Jan 08.
SK&F; 83822 distinguishes adenylyl cyclase from phospholipase C-coupled dopamine D1-like receptors:
behavioural topography.
O'Sullivan GJ, Roth BL, Kinsella A, Waddington JL.
Eur J Pharmacol. 2004 Feb 23;486(3):273-80.
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist.
Peddi S, Roth BL, Glennon RA, Westkaemper RB.
Eur J Pharmacol. 2003 Dec 15;482(1-3):335-7.
IRAS splice variants.
Piletz JE, Deleersnijder W, Roth BL, Ernsberger P, Zhu H, Ziegler D.
Ann N Y Acad Sci. 2003 Dec;1009:419-26.
L-homocysteine sulfinic acid and L-homocysteic acid stimulate phosphoinositide hydrolysis in rat
cortical neurons.
Shi Q, Hufeisen SJ, Wroblewski JT, Nadeau JH, Roth BL.
Ann N Y Acad Sci. 2003 Nov;1003:461-3.
Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.
De Amici M, Conti P, Fasoli E, Barocelli E, Ballabeni V, Bertoni S, Impicciatore M, Roth BL,
Ernsberger P, De Micheli C.
Farmaco. 2003 Sep;58(9):739-48.
In Vitro Characterization of Ephedrine-Related Stereoisomers at Biogenic
Amine Transporters and the Receptorome Reveals Selective Actions as
Norepinephrine Transporter Substrates.
Rothman RB, Vu N, Partilla JS, Roth BL, Hufeisen SJ, Compton-Toth BA, Birkes J, Young R, Glennon RA.
J Pharmacol Exp Ther. 2003 Oct;307(1):138-45. Epub 2003 Sep 3.
Behavioral and biochemical investigations of bupropion metabolites
Bondarev ML, Bondareva TS, Young R, Glennon RA.
Eur J Pharmacol. 2003 Aug 1;474(1):85-93.
Ring Substituted Analogues of 5-Aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH):
Potential Modes of Binding to the 5-HT2A Receptor
Peddi S, Roth BL, Glennon RA, Westkaemper RB.
Bioorg Med Chem Lett. 2003 Aug 4;13(15):2565-8.
3,4-Methylenedioxymethamphetamine (MDMA, "Ecstasy") Induces Fenfluramine-Like Proliferative
Actions on Human Cardiac Valvular Interstitial Cells in Vitro.
Setola V, Hufeisen SJ, Grande-Allen KJ, Vesely I, Glennon RA, Blough B, Rothman RB, Roth BL.
Mol Pharmacol 2003 Jun;63(6):1223-9
L-homocysteine sulfinic acid and other acidic homocysteine derivatives
are potent and selective metabotropic glutamate receptor agonists.
Shi Q, Savage J, Hufesein S, Rauser L, Grajkowski E, Ernsberger P, Wroblewski J, Nadeau J,Roth BL.
J Pharmacol Exp Ther. 2003 Apr;305(1):131-42
Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor
Sheffler DJ, Roth BL.
Trends Pharmacol Sci. 2003 Mar;24(3):107-9.
Novel diketopiperazine enhances motor and cognitive recovery after traumatic brain injury in
rats and shows neuroprotection in vitro and in vivo.
Faden AI, Knoblach SM, Cernak I, Fan L, Vink R, Araldi GL, Fricke ST, Roth BL, Kozikowski AP.
J Cereb Blood Flow Metab. 2003 Mar;23(3):342-54
The binding of 2-(4'-methylaminophenyl)benzothiazole to postmortem brain
homogenates is dominated by the amyloid component.
Klunk WE, Wang Y, Huang GF, Debnath ML, Holt DP, Shao L, Hamilton RL, Ikonomovic MD,
DeKosky ST, Mathis CA.
J Neurosci 2003 Mar 15;23(6):2086-92
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of
constrained epibatidine analogues.
Wei ZL, Petukhov PA, Xiao Y, Tuckmantel W, George C, Kellar KJ, Kozikowski AP.
J Med Chem 2003 Mar 13;46(6):921-4
Lysergamides of Isomeric 2,4-Dimethylazetidines Map the Binding Orientation of the
Diethylamide Moiety in the Potent Hallucinogenic Agent N,N-Diethyllysergamide (LSD).
Nichols DE, Frescas S, Marona-Lewicka D, Kurrasch-Orbaugh DM.
J Med Chem 2002 Sep 12;45(19):4344-9
A Last GASP for GPCRs?
Gray JA, Roth BL.
Science. 2002 Jul 26;297(5581):529-31.
Substituted Diphenyl Sulfides as Selective Serotonin Transporter Ligands:
Synthesis and In Vitro Evaluation
Emond P, Vercouillie J, Innis R, Chalon S, Mavel S, Frangin Y, Halldin C, Besnard JC, Guilloteau D.
J Med Chem. 2002 Mar 14;45(6):1253-8.
Geometry-Affinity Relationships of the Selective Serotonin Receptor Ligand
9-(Aminomethyl)-9,10-Dihydroanthracene
Runyon SP, Peddi S, Savage JE, Roth BL, Glennon RA, and Westkaemper RB
J Med Chem. 2002 Apr 11;45(8):1656-64.
Synthesis of Potent and Selective Dopamine D4 Antagonists as Candidate Radioligands.
Huang Y, Kegeles LS, Bae S, Hwang D, Roth BL, Savage JE, Laruelle M.
Bioorg Med Chem Lett 2001 Jun 4;11(11):1375-7
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors
of prostate cancer cell growth.
Qiao L, Zhao LY, Rong SB, Wu XW, Wang S, Fujii T, Kazanietz MG, Rauser L, Savage J, Roth BL,
Flippen-Anderson J, Kozikowski AP.
Bioorg Med Chem Lett. 2001 Apr 23;11(8):955-9.
Discovery of a Novel Member of the Histamine Receptor Family.
Nguyen T, Shapiro DA,
George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF.
Mol Pharmacol. 2001 Mar;59(3):427-33.
Influence of Chain Length and N-alkylation on the Selective Serotonin Receptor Ligand
9-(aminomethyl)-9,10-dihydroanthracene.
Runyon SP, Savage JE, Taroua M, Roth BL, Glennon RA, Westkaemper RB.
Bioorg Med Chem Lett 2001 Mar 12;11(5):655-8.
Exploring the Relationship between Binding Modes of 9-(aminomethyl)-9,10-dihydroanthracene
and Cyproheptadine Analogs at the 5-HT2A Serotonin Receptor.
Westkaemper RB, Runyon SP, Savage JE, Roth BL, Glennon RA.
Bioorg Med Chem Lett, 2001 Feb 26;11(4):563-6
Derivation of 5-HT transporter parameters with [11C]DASB and [11C]ADAM in baboons: Comparison with [11C]McN5652..
Huang Y, Hwang DR, Sudo Y, Lombardo I, Kegeles L, Chatterjee R, Ali M, Bae SA, Kung H, Wilson AA,
Laruelle M (2001)
Journal of Nuclear Medicine 42:105p
Synthesis and characterization of a new PET ligand for the serotonin transporter:
[11C]5-Bromo-2-{2-[(dimethylamino)methyl]phenylsulfanyl}phenylamine.
Huang Y, Bae SA, Zhu Z, Guo N, Hwang DR, Sudo Y, Ngo K, Kegeles L, Laruelle M (2001)
Journal of Nuclear Medicine 42:112p
Fluorinated analogues of ADAM as new PET radioligands for the serotonin transporter: Synthesis
and pharmacological evaluation.
Huang Y, Bae SA, Zhu Z, Guo N. Hwang DR. Laruelle M (2001)
Journal of Labelled Compounds and Radiopharmaceuticals 44:S18-20
Inverse Agonist Actions of Typical and Atypical Antipsychotic Drugs at the
Human 5-Hydroxytryptamine2C Receptor
Rauser L, Savage JE, Meltzer HY, Roth BL.
J Pharmacol Exp Ther. 2001 Oct;299(1):83-9.
The in vitro pharmacology of the b-adrenergic receptor pet ligand
(s)-fluorocarazolol reveals high affinity for cloned b-adrenergic
receptors and moderate affinity for the human 5-HT1A receptor
Roth BL, Ernsberger P, Steinberg SA, Rao S, Rauser L, Savage J, Hufeisen S, Berridge MS, Muzic RF Jr.
Psychopharmacology (Berl). 2001 Aug;157(1):111-4.
Selective in vitro and in vivo binding of [(125)I]ADAM to serotonin transporters in rat brain.
Choi SR, Hou C, Oya S, Mu M, Kung MP, Siciliano M, Acton PD, Kung HF.
Synapse. 2000 Dec 15;38(4):403-12.
Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy
associated with fenfluramine and other serotonergic medications.
Rothman RB, Baumann MH, Savage JE, Rauser L, McBride A, Hufeisen SJ, Roth BL.
Circulation. 2000 Dec 5;102(23):2836-41.
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S,
Lee M, Glennon RA.
Bioorg Med Chem Lett. 2000 Oct 16;10(20):2295-9.
The Multiplicity of Serotonin Receptors: Uselessly diverse molecules or an embarrasment of
riches?
BL Roth, E Lopez, S Patel and WK Kroeze
Neuroscientist, Aug 2000; 6: 252 - 262.
Neuronal Signal Transduction Pathways: Wasteland or the Promised Land?
Roth BL.
Sci STKE. 2000 Aug 15;2000(45):pe1.
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L,
Hufeisen S, Lee DK.
J Med Chem. 2000 Mar 9;43(5):1011-8.
Pharmacokinetics unbound. Need to know how tightly your drug candidate binds to a
particular G-protein receptor, a class of proteins through which many pharmaceutical
agents exert their therapeutic effects? This new database from a psychoactive drug-screening
program offers thousands of affinity constants (k) for ligand binding to over 125 receptors.
Science 28 January 2000: Vol. 287 no. 5453 p. 543
Development of PET radioligand for the 5-HT1B receptor: synthesis and in vivo evaluation of
[C-11]GR127935.
Huang Y, Kent JM, Simpson N, Guo N, Bae SA, Mann JJ, Laruelle M (2000)
NeuroImage 11:S69
Development of candidate dopamine D4 receptor PET radiotracers.
Huang Y, Bae SA, Hwang DR, Kegeles LS, Roth BL, Savage JE, Rauser L, McBride A, Laruelle M (2000)
Journal of Nuclear Medicine 41:242p
A third life for burimamide. Discovery and characterization of a novel class of non-opioid analgesics derived from histamine antagonists.
Hough LB, Nalwalk JW, Barnes WG, Leurs R, Menge WM, Timmerman H, Wentland M.
Ann N Y Acad Sci. 2000;909:25-40.
LQ12, A Novel PKC Activator, Enhances sAPP Secretion in PC-12 Cells;
Lixin Qiao, Rene Etcheberrigaray, Alan P. Kozikowski and Bryan Roth
Proceedings of The Third International Electronic Conference on Synthetic Organic Chemistry,
http://www.mdpi.org/ecsoc-3.htm,
September 1-30, 1999 Editors: Esteban Pombo-Villar, Reinhard Neier and Shu-Kun Lin
Characterization of radioactive metabolites of 5-HT2A receptor PET ligand [18F]altanserin
in human and rodent.
Tan PZ, Baldwin RM, Van Dyck CH, Al-Tikriti M, Roth B, Khan N, Charney DS, Innis RB.
Nucl Med Biol. 1999 Aug;26(6):601-8.
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