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PHARMACOLOGYPHARMACOLOGYThe Journal of
And Experimental Therapeutics
A Publication of the American Society for
Pharmacology and Experimental Therapeutics
Edited for the Society by Rick G. Schnellmann
Volume 324 ■ Number 3 ■ March 2008 ■ ISSN 0022-3565
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PERSPECTIVES IN PHARMACOLOGYNAD� and Vitamin B3: From Metabolism to Therapies Anthony A. Sauve 883
CARDIOVASCULAR□S Functional Antagonism between Endogenous Neuropeptide Y
and Calcitonin Gene-Related Peptide in Mesenteric ResistanceArteries
Jo G. R. De Mey, Remco Megens, andGregorio E. Fazzi
930
□S Characterization of Epoxyeicosatrienoic Acid Binding Site inU937 Membranes Using a Novel Radiolabeled Agonist, 20-125I-14,15-Epoxyeicosa-8(Z)-Enoic Acid
Wenqi Yang, Venugopal Raju Tuniki,Siddam Anjaiah, J. R. Falck,Cecilia J. Hillard, and William B. Campbell
1019
Inhibiting Protease-Activated Receptor 4 Limits MyocardialIschemia/Reperfusion Injury in Rat Hearts by UnmaskingAdenosine Signaling
Jennifer L. Strande, Anna Hsu, Jidong Su,Xiangping Fu, Garrett J. Gross, andJohn E. Baker
1045
Characterization of the Molecular Fragment That IsResponsible for Agonism of Pergolide at Serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A Receptors
Tilo Görnemann, Harald Hübner,Peter Gmeiner, Reinhard Horowski,Klaus Peter Latté, Miroslav Flieger, andHeinz H. Pertz
1136
Doxycycline Attenuates Isoproterenol- and Transverse AorticBanding-Induced Cardiac Hypertrophy in Mice
Mounir Errami, Cristi L. Galindo,Amina T. Tassa, John M. DiMaio,Joseph A. Hill, and Harold R. Garner
1196
Mechanism-Based Pharmacodynamic Modeling ofS(�)-Atenolol: Estimation of in Vivo Affinity for the �1-Adrenoceptor with an Agonist-Antagonist Interaction Model
Tamara J. van Steeg, Jan Freijer,Meindert Danhof, andElizabeth C. M. de Lange
1234
CELLULAR AND MOLECULAR7-Chloro-5-(4-hydroxyphenyl)-1-methyl-3-(naphthalen-2-ylmethyl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one (Bz-423), a Benzodiazepine, Suppresses Keratinocyte Proliferationand Has Antipsoriatic Activity in the Human Skin-Severe,Combined Immunodeficient Mouse Transplant Model
Narasimharao Bhagavathula,Kamalakar C. Nerusu, Andrew Hanosh,Muhammad N. Aslam, Thomas B. Sundberg,Anthony W. Opipari, Jr., Kent Johnson,Sewon Kang, Gary D. Glick, andJames Varani
938
Inhibition of the Cardiac L-Type Calcium Channel Currentby Antidepressant Drugs
Ivan Zahradnı́k, Igor Minarovič, andAlexandra Zahradnı́ková
977
Inhibition of Geranylgeranyl Diphosphate Synthase InducesApoptosis through Multiple Mechanisms and DisplaysSynergy with Inhibition of Other Isoprenoid BiosyntheticEnzymes
Amel Dudakovic, Andrew J. Wiemer,Kimberly M. Lamb, Laura A. Vonnahme,Sara E. Dietz, and Raymond J. Hohl
1028
The Journal of
PHARMACOLOGYAnd Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
March 2008 Vol. 324, No. 3
Contents
The Journal of Pharmacology and Experimental Therapeutics (ISSN0022-3565) is published monthly by the American Society for Pharma-cology and Experimental Therapeutics, 9650 Rockville Pike,Bethesda, MD 20814-3995; email: [email protected]; web site:www.aspet.org. Periodicals postage paid at Bethesda, MD, and at addi-tional mailing offices. POSTMASTER: Send address changes to The Jour-nal of Pharmacology and Experimental Therapeutics, 9650 RockvillePike, Bethesda, MD 20814-3995. Subscription rates: U.S.: $893.00 forinstitutions and $389.00 for non-ASPET members. Outside the U.S.:$1,049.00 for institutions and $545.00 for non-ASPET members.
Single copy: $79.00. GST Tax Number for Canadian subscribers: BN:13489 2330 RT. Indexed or abstracted by Biochemistry & BiophysicsCitation Index®, Biological Abstracts, BIOSIS Previews Database, Bio-Sciences Information Services, Current Awareness in Biological Sci-ences, Current Contents®/Life Sciences, EMBASE/Excerpta Medica,Index Medicus, Medical Documentation Service®, PsycINFO, Refer-ence Update®, Research Alert®, Science Citation Index®, SciSearch®,and SIIC Data Bases. Copyright © 2008 by the American Society forPharmacology and Experimental Therapeutics. All rights reserved.Printed in the U.S.A.
Involvement of P2Y1 and P2Y11 Purinoceptors inParasympathetic Inhibition of Colonic Smooth Muscle
Brian F. King andAndrea Townsend-Nicholson
1055
A Conservative, Single-Amino Acid Substitution in the SecondCytoplasmic Domain of the Human Serotonin2C ReceptorAlters Both Ligand-Dependent and -Independent ReceptorSignaling
Kelly A. Berg, John Dunlop,Teresa Sanchez, Michelle Silva, andWilliam P. Clarke
1084
Plitidepsin Has a Dual Effect Inhibiting Cell Cycle andInducing Apoptosis via Rac1/c-Jun NH2-Terminal KinaseActivation in Human Melanoma Cells
Marı́a J. Muñoz-Alonso,Laura González-Santiago, Natasha Zarich,Teresa Martı́nez, Enrique Alvarez,José Marı́a Rojas, and Alberto Muñoz
1093
Statins Decrease Expression of the ProinflammatoryNeuropeptides Calcitonin Gene-Related Peptide and SubstanceP in Sensory Neurons
Robert C. Bucelli, Eugene A. Gonsiorek,Woo-Yang Kim, Donald Bruun,Richard A. Rabin, Dennis Higgins, andPamela J. Lein
1172
Estrogen Receptor-Independent Neuroprotection via ProteinPhosphatase Preservation and Attenuation of PersistentExtracellular Signal-Regulated Kinase 1/2 Activation
Kun Don Yi, Zu Yun Cai,Douglas F. Covey, and James W. Simpkins
1188
Erythropoietin Stimulates Cancer Cell Migration andActivates RhoA Protein through a Mitogen-Activated ProteinKinase/Extracellular Signal-Regulated Kinase-DependentMechanism
Sumaya N. Hamadmad andRaymond J. Hohl
1227
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPYThe Effects of Cyclooxygenase-2 Expression in ProstateCancer Cells: Modulation of Response to Cytotoxic Agents
Ayaz Mehar, Patricia Macanas-Pirard,Atsushi Mizokami, Yutaka Takahashi,Georges E. N. Kass, and Helen M. Coley
1181
ENDOCRINE AND DIABETESStudies with an Orally Bioavailable �V Integrin Antagonist inAnimal Models of Ocular Vasculopathy: RetinalNeovascularization in Mice and Retinal Vascular Permeabilityin Diabetic Rats
Rosemary J. Santulli, William A. Kinney,Shyamali Ghosh, Bart L. DeCorte, Li Liu,Robert W. A. Tuman, Zhao Zhou,Norman Huebert, Sven E. Bursell,Alan C. Clermont, Maria B. Grant,Lynn C. Shaw, Shaker A. Mousa,Robert A. Galemmo, Jr., Dana L. Johnson,Bruce E. Maryanoff, and Bruce P. Damiano
894
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENALCellular Targeting of the Apoptosis-Inducing CompoundGliotoxin to Fibrotic Rat Livers
W. I. Hagens, L. Beljaars, D.A. Mann,M. C. Wright, B. Julien, S. Lotersztajn,C. Reker-Smit, and K. Poelstra
902
INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMAReduction of Peroxisome Proliferation-Activated Receptor �Expression by �-Irradiation as a Mechanism Contributing toInflammatory Response in Rat Colon: Modulation by the 5-Aminosalicylic Acid Agonist
Christine Linard, Olivier Grémy, andMarc Benderitter
911
p38�-Selective Mitogen-Activated Protein Kinase InhibitorSD-282 Reduces Inflammation in a Subchronic Model ofTobacco Smoke-Induced Airway Inflammation
Satyanarayana Medicherla,Mary F. Fitzgerald, Dianne Spicer,Paul Woodman, Jing Y. Ma,Ann M. Kapoun, Sarvajit Chakravarty,Sundeep Dugar, Andrew A. Protter, andLinda S. Higgins
921
Thionamides Inhibit the Transcription Factor Nuclear Factor-�B by Suppression of Rac1 and Inhibitor of �B Kinase �
Matjaz Humar, Hannah Dohrmann,Philipp Stein, Nikolaos Andriopoulos,Ulrich Goebel, Martin Roesslein,Rene Schmidt, Christian I. Schwer,Torsten Loop, Klaus K. Geiger,Heike L. Pahl, and Benedikt H.J. Pannen
1037
METABOLISM, TRANSPORT, AND PHARMACOGENOMICSInhibitor Binding in the Human Renal Low- and High-Affinity Na�/Glucose Cotransporters
Ana M. Pajor, Kathleen M. Randolph,Sandy A. Kerner, and Chari D. Smith
985
Selegiline Is a Mechanism-Based Inactivator of CYP2A6Inhibiting Nicotine Metabolism in Humans and Mice
Eric C.K. Siu and Rachel F. Tyndale 992
Identification and Design of Peptides as a New Drug DeliverySystem for the Brain
Michel Demeule, Anthony Régina,Christian Ché, Julie Poirier, Tran Nguyen,Reinhard Gabathuler, Jean-Paul Castaigne,and Richard Béliveau
1064
Age-Dependent Kinetics and Metabolism of Dichloroacetate:Possible Relevance to Toxicity
Albert L. Shroads, Xu Guo, Vaishali Dixit,Hui-Ping Liu, Margaret O. James, andPeter W. Stacpoole
1163
Extracting Global System Dynamics of CorticosteroidGenomic Effects in Rat Liver
E. Yang, R. R. Almon, D. C. DuBois,W. J. Jusko, and I. P. Androulakis
1243
NEUROPHARMACOLOGY□S Trace Amine-Associated Receptor 1 Modulates Dopaminergic
ActivityLothar Lindemann, Claas Aiko Meyer,Karine Jeanneau, Amyaouch Bradaia,Laurence Ozmen, Horst Bluethmann,Bernhard Bettler, Joseph G. Wettstein,Edilio Borroni, Jean-Luc Moreau, andMarius C. Hoener
948
□S In Vivo �-Secretase 1 Inhibition Leads to Brain A� Loweringand Increased �-Secretase Processing of Amyloid PrecursorProtein without Effect on Neuregulin-1
Sethu Sankaranarayanan, Eric A. Price,Guoxin Wu, Ming-Chih Crouthamel,Xiao-Ping Shi, Katherine Tugusheva,Keala X. Tyler, Jason Kahana,Joan Ellis, Lixia Jin, Thomas Steele,Shawn Stachel, Craig Coburn, andAdam J. Simon
957
Increased C-Fiber Nociceptive Input Potentiates InhibitoryGlycinergic Transmission in the Spinal Dorsal Horn
Hong-Yi Zhou, Hong-Mei Zhang,Shao-Rui Chen, and Hui-Lin Pan
1000
Arginine 246 of the Pretransmembrane Domain 1 RegionAlters 2,2,2-Trichloroethanol Action in the 5-Hydroxytryptamine3A Receptor
Xiang-Qun Hu and Robert W. Peoples 1011
2-Methoxymethyl-Salvinorin B Is a Potent � Opioid ReceptorAgonist with Longer Lasting Action in Vivo Than SalvinorinA
Yulin Wang, Yong Chen, Wei Xu,David Y.W. Lee, Zhongze Ma,Scott M. Rawls, Alan Cowan, andLee-Yuan Liu-Chen
1073
The Triple Uptake Inhibitor (1R,5S)-(�)-1-(3,4-Dichlorophenyl)-3-azabicyclo[3.1.0] Hexane Hydrochloride(DOV 21947) Reduces Body Weight and Plasma Triglyceridesin Rodent Models of Diet-Induced Obesity
Joseph P. Tizzano, D. Sloan Stribling,Diego Perez-Tilve, Alison Strack,Andrea Frassetto, Richard Z. Chen,Tung M. Fong, Lauren Shearman,Philip A. Krieter, Matthias H. Tschöp,Phil Skolnick, and Anthony S. Basile
1111
Isoflurane Is a Potent Modulator of Extrasynaptic GABAAReceptors in the Thalamus
Fan Jia, Minerva Yue, Dev Chandra,Gregg E. Homanics, Peter A. Goldstein, andNeil L. Harrison
1127
A Selective Nav1.8 Sodium Channel Blocker, A-803467 [5-(4-Chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide],Attenuates Spinal Neuronal Activity in Neuropathic Rats
Steve McGaraughty, Katharine L. Chu,Marc J. C. Scanio, Michael E. Kort,Connie R. Faltynek, and Michael F. Jarvis
1204
S33138 (N-[4-[2-[(3aS,9bR)-8-cyano-1,3a,4,9b-tetrahydro[1]benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenyl-acetamide), aPreferential Dopamine D3 versus D2 Receptor Antagonist andPotential Antipsychotic Agent: III. Actions in Models ofTherapeutic Activity and Induction of Side Effects
Mark J. Millan, Florence Loiseau,Anne Dekeyne, Alain Gobert, Gunnar Flik,Thomas I. Cremers, Jean-Michel Rivet,Dorothée Sicard, Rodolphe Billiras, andMauricette Brocco
1212
TOXICOLOGYInhibition of Mitochondrial Hydrogen Peroxide Production byLipophilic Metalloporphyrins
Pablo R. Castello, Derek A. Drechsel,Brian J. Day, and Manisha Patel
970
Omeprazole Stimulates the Induction of Human Insulin-LikeGrowth Factor Binding Protein-1 through Aryl HydrocarbonReceptor Activation
Iain A. Murray and Gary H. Perdew 1102
The Butyrylcholinesterase Knockout Mouse as a Model forHuman Butyrylcholinesterase Deficiency
Bin Li, Ellen G. Duysen, Michaela Carlson,and Oksana Lockridge
1146
Succinate Ameliorates Energy Deficits and PreventsDysfunction of Complex I in Injured Renal Proximal TubularCells
Grażyna Nowak, Ginger L. Clifton, andDiana Bakajsova
1155
□S Supplemental material is available online at http://jpet.aspetjournals.org.
About the cover: The Trace amine-associated receptor 1 (TAAR1) is expressed in multiple areas of themouse brain, including the ventral tegmental area. Dopaminergic neurons in this region show anincreased firing frequency in TAAR1 knockout compared to wild-type mice. See the article by Lindemannet al. on page 948 of this issue.
Rick G. Schnellmann, EditorCraig C. Beeson, Assistant Editor
ASSOCIATE EDITORSDarrell R. AbernethyIan AdcockJerry J. BuccafuscoPhilip S. BurtonDavid B. BylundPaul Ernsberger
Mitchell P. FinkAlan R. GintzlerRonald N. HinesMyron K. JacobsonMichael F. Jarvis
Norbert E. KaminskiRaouf A. KhalilDaniel R. KnappLawrence H. LashRoberto Levi
Louis M. LuttrellDavid S. MillerRichard A. MorrisettA. Leslie MorrowMichael J. O’Neill
Bryan L. RothRobert A. RothRoland SeifertKenneth D. TewStephanie W. WattsAlice M. Young
EDITORIAL ADVISORY BOARDGeoffrey W. AbbottThomas J. AbbruscatoPeter AbelEdson X. AlbuquerqueThomas M. ArgentieriBork BalkanLeslie R. BallouWilliam A. BanksJack BergmanDaniel C. BertrandItalo BiaggioniC. Paul BianchiFloyd E. BloomJean-Marie BoeynaemsFranco BorsiniMarco BrottoNancy BrownJohn CharpieLucio G. CostaBrian M. CoxBryan F. CoxBruce N. CronsteinBrian CummingsM. Imad DamajWilliam C. deGroatRussell Delude
Patrick DoughertyFrederick J. EhlertJohn L. EvendenSteven J. FeinmarkGiora Z. FeuersteinStephen F. FlaimAnthony W. FoxCharles P. FranceAlan FrazerGert FrickerRyan FryerBernard W. FutscherJames J. GalliganVadivel GanapathyPatricia E. GaneyRichard A. GillisGary GintantJohn R. GlowaMurali GopalakrishnanSteven M. GrasslGarrett J. GrossPerry V. HalushkaGyorgy HaskoJ. Paul HiebleK. Roger HornbrookSusanna HouraniLeonard L. Howell
Dale G. HoytJohn ImigHarry IschiropoulosEdwin K. JacksonKenneth M. JohnsonWilliam J. JuskoPeter W. KalivasLaurence S. KaminskyJonathan L. KatzMark R. KelleyLewis B. KinterThomas KocarekGeorge F. KoobSuk-Hee LeeBenedict R. LucchesiJoseph J. LynchRosalinde MasereeuwPhilip R. MayeuxDonald E. McMillanMark J. MillanGary W. MillerHitoshi MorikawaHasan MukhtarL. Charles MurrinMichael NaderStanley NattelS. Stevens Negus III
Kim A. NeveYasuyuki NomuraJames S. NorrisGrazyna NowakJames M. O’DonnellPatricio O’DonnellMichael F. O’NeillMark OsinskiK. Sandy PangAchilles J. PappanoB. Kevin ParkSandra PfisterMichael T. PiascikRussell O. PieperJoseph W. PolliJohn B. PritchardRussell A. ProughRaymond M. QuockJ. Larry RenfroMichael C. SanguinettiJonathan G. ScammellMichal Laniado
SchwartzmanFederico SestiDavid R. SibleyTheodore A. SlotkinMark Smith
Philip C. SmithQuentin R. SmithNikolai M. SoldatovEdward E. SoltisPatricia K. SonsallaMichael D. SouthallRoger D. SpealmanFrancis G. SpinaleJohn L. SutkoDouglas SweetIstvan SzelenyiMilt TeitlerPaul F. TerranovaAlvin V. TerryMyron L. ToewsGeorge J. TrachteHiroshi UedaMichael R. VaskoSandra P. WelchDaniel WierdaMichael WilliamsRaymond J. WinquistJeffrey M. WitkinBryan K. Yamamoto
BOARD OF PUBLICATIONS TRUSTEESJames E. Barrett, Chair; P. Jeffrey Conn, Ross Feldman, Lorraine J. Gudas, Eric F. Johnson, John S. Lazo, Edward T. Morgan,
Richard R. Neubig, Rick G. Schnellmann, Darryle D. Schoepp, and Mary VoreASPET EXECUTIVE OFFICER: Christine K. Carrico
Journals Director: Richard Dodenhoff Managing Editor: Jill Filler Senior Editorial Coordinator: David D. Williams
Journal and ASPET Office: 9650 Rockville Pike, Bethesda, MD 20814-3995; telephone: 301-634-7060; fax: 301-634-7061; email: [email protected]; website: www.aspet.org.Correspondence regarding editorial matters should be addressed to Dr.Rick G. Schnellmann, Editor, The Journal of Pharmacology and ExperimentalTherapeutics, at the above address.Official version: The online version of The Journal of Pharmacology and Experi-mental Therapeutics contains all of the information and material contained in theprint version plus additional material that may not appear in print such as videosand large data sets. The online version may be more current than the print version.Where noted, the online version has been corrected in departure from the printversion. The online version of The Journal of Pharmacology and ExperimentalTherapeutics officially published by the American Society for Pharmacology andExperimental Therapeutics is the definitive version and, to the extent any differenceexists, will prevail over the print version.Instructions to Authors: See http://jpet.aspetjournals.org for the Instruc-tions to Authors and the ASPET Authorship Responsibility, Financial Disclo-sure, and Copyright Transfer form.Correspondence concerning subscriptions: Nonmember individual and insti-tutional subscriptions: ASPET Subscriptions Dept., Rm. L-2310, 9650 RockvillePike, Bethesda, MD 20814-3998; telephone: 301-634-7029; fax: 301-634-7099; email:[email protected]. ASPET Members: contact the ASPET office. For European sitelicenses and consortia, contact: David Charles, Institutional Sales & Licensing, 92avenue du General de Gaulle, 78600 Maisons-Laffitte, France: telephone: �33–1-39–12-29–29; fax: �33–1-39–12-47–45; email: [email protected] of address: ASPET must be notified 60 days in advance. Journalsundeliverable because of incorrect address will be destroyed. Duplicate copiesmay be obtained, if available, from ASPET at the single copy price. Sendaddress changes to the ASPET office.Issue Replacement Policy: Domestic Subscribers—Claims for nondeliv-ery of issues must be made within three (3) months of issue mail date.Foreign Subscribers—Claims for nondelivery of issues must be made
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The Journal of Pharmacology and Experimental TherapeuticsA Publication of the American Society for Pharmacology and Experimental Therapeutics
Founded by John J. Abel - 1908