Recent papers:
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 1. [Epub ahead of print]
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 4. [Epub ahead of print]
A chemical-genetic approach to study G protein regulation of Β cell function in vivo
Jean-Marc Guettier, Dinesh Gautam, Marco Scarselli, Inigo Ruiz de Azua, Jian Hua Li, Erica Rosemond,
Xiaochao Ma, Frank J. Gonzalez, Blaine N. Armbruster, Huiyan Lu, Bryan L. Roth, and Jürgen Wess
PNAS published online before print October 26, 2009, doi:10.1073/pnas.0906593106
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.Click here to read
The Expanded Biology of Serotonin
Miles Berger, John A. Gray, and Bryan L. Roth
Annual Review of Medicine, Vol. 60: 355-366 (Volume publication date February 2009)
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):1079-84.
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
Douglas J. Sheffler, Wesley K. Kroeze, Bonnie G. Garcia, Ariel Y. Deutch, Sandra J. Hufeisen,
Patrick Leahy, Jens C. Brüning, and Bryan L. Roth
Proc. Natl. Acad. Sci. USA, 10.1073/pnas.0600585103
Nigrostriatal Dopaminergic Deficits and Hypokinesia Caused by Inactivation of the Familial Parkinsonism-Linked Gene DJ-1.
Matthew S. Goldberg, Antonio Pisani, Marian Haburcak, Timothy A. Vortherms, Tohru Kitada, Cinzia Costa, Youren Tong,
Giuseppina Martella, Anne Tscherter, Andrea Martins, Giorgio Bernardi, Bryan L. Roth, Emmanuel N. Pothos, Paolo Calabresi,
and Jie Shen
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 13; [Epub ahead of print]
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 D(2L), D(4.2), and 5-HT(2A) receptors
Carato P, Graulich A, Jensen N, Roth BL, Liegeois JF.
Bioorg Med Chem Lett. 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 D(2L), D(4.2), and 5-HT(2A) receptors.
Carato P, Graulich A, Jensen N, Roth BL, Liegeois JF.
Bioorg Med Chem Lett. 2007 Jan 8
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Kulkarni, S. S.; Nightingale, B.; Dersch, C. M.; Rothman, R. B.; Newman, A. H.
Bioorg. Med. Chem Lett. 2006, 16, 3371-3375
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):1080-1100
Binding of amine-substituted N(1)-benzenesulfonylindoles at human 5-HT(6) serotonin receptors.
Pullagurla M, Siripurapu U, Kolanos R, Bondarev ML, Dukat M, Setola V, Roth BL, Glennon RA
Bioorg Med Chem Lett. 2005 Sep 21; [Epub ahead of print]
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-HT(1B) 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-HT(2C) agonist.
Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, Shuster L
Bioorg Med Chem Lett. 2005 Jul 29; [Epub ahead of print]
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. 2005 Jul 6; [Epub ahead of print]
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 Mar 10; [Epub ahead of print]
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
Mase Lee, Jagadeesh B. Rangisetty, Manik R. Pullagurla, Malgorzata Dukat, Vince Setola, Bryan L. Roth, and Richard A. Glennon
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1707-11
Studies toward the Pharmacophore of Salvinorin A, a
Potent k Opioid Receptor Agonist
Thomas A. Munro, Mark A. Rizzacasa, Bryan L. Roth, Beth A. Toth, and Feng Yan
J. Med. Chem. 2005, 48, 345-348 DOI: 10.1021/jm049438q
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-HT3(A) 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 May 19
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 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
Srinivas Peddi,a Bryan L. Roth,b Richard A. Glennona and Richard B. Westkaempera,*
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, Douglas J.; Roth, Bryan L.
Trends Pharmacol Sci. 2003 Mar;24(3):107-9. Review
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?
John A. Gray and Bryan L. Roth
Science Jul 26 2002: 529-531
Substituted Diphenyl Sulfides as Selective Serotonin Transporter Ligands:
Synthesis and In Vitro Evaluation
Patrick Emond,* Johnny Vercouillie, Robert Innis, † Sylvie Chalon, Sylvie Mavel, Yves Frangin,
Christer Halldin, ‡ Jean-Claude Besnard, and Denis Guilloteau
J. Med. Chem. 2002, 45, 1253-1258
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 Westkaempera RB
J Med Chem 2002, 45, 1656-1664
Synthesis of Potent and Selective Dopamine D4 Antagonists as Candidate Radioligands.
Yiyun Huang,* Lawrence Kegeles, Sung-A Bae, Dah-ren Hwang, Bryan L. Roth, Jason E.
Savage and Marc Laruelle.
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):427-433.
Influence of Chain Length and N-alkylation on the Selective Serotonin Receptor Ligand
9-(aminomethyl)-9,10-dihydroanthracene.
Scott P. Runyon, Jason E. Savage, Mohamed Taroua, Bryan L. Roth, Richard A. Glennon,
Richard B. Westkaemper.
Bioorg Med Chem Lett 2001 Mar 12;11(5):655-8 PMID: 11266163
Exploring the Relationship between Binding Modes of 9-(aminomethyl)-9,10-dihydroanthracene
and Cyproheptadine Analogs at the 5-HT2a Serotonin Receptor.
Richard B. Westkaemper, Scott P. Runyon, Jason E. Savage, Bryan L. Roth,
Richard A. Glennon.
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
Laura Rauser, Jason E. Savage, Herbert Y. Meltzer, and Bryan L. Roth
J. Pharmacol. Exp. Ther. 2001 299(1): p. 83-89
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
Bryan L. Roth, Paul Ernsberg, SeAnna Steinberg, Suma Rao, Laura Rauser, Jason Savage,
Sandy Hufeisen, Marc S. Berridge, Raymond F. Muzic Jr
Psychopharmacology (2001) 157:111-114
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 antagonistst.
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?
Bryan L. Roth
Science's STKE Published 15 August 2000
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.
http://pdsp.med.unc.edu/pdsp.php.
Science Jan. 21, 2000; #278 (5452).
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. Review.
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
|
