5 November 2009

Takato Hiranita, Paul L Soto, Gianluigi Tanda, and Jonathan L. Katz

Reinforcing Effects of -Receptor Agonists in Rats Trained to Self-Administer Cocaine
Published November 5, 2009; doi:10.1124/jpet.109.159236 [Abstract] [PDF]  

Mei Hong, Shanshan Li, Fanfan Zhou, Paul E Thomas, and Guofeng You

Putative Transmembrane Domain 12 of the Human Organic Anion Transporter hOAT1 Determines Transporter Stability and Maturation Efficiency
Published November 5, 2009; doi:10.1124/jpet.109.160515 [Abstract] [PDF]  

4 November 2009

Francois Chavant, Julie Deguil, Stephanie Pain, Isabelle Ingrand, Serge Milin, Bernard Fauconneau, Marie-Christine Perault, and Claire LAFAY-CHEBASSIER

Imipramine, in part through TNF- inhibition, prevents cognitive decline and Aβ accumulation in a mouse model of Alzheimer's disease
Published November 4, 2009; doi:10.1124/jpet.109.162164 [Abstract] [PDF]  

Jennifer R Paulson, Tianzhi Yang, Pradeep K Selvaraj, Alexander Mdzinarishvili, Cornelis J Van der Schyf, Jochen Klein, Ulrich Bickel, and Thomas J Abbruscato

Nicotine Exacerbates Brain Edema during in vitro and in vivo Focal Ischemic Conditions
Published November 4, 2009; doi:10.1124/jpet.109.157776 [Abstract] [PDF]  

Nadine Freimuth, Robert Ramer, and Burkhard Hinz

Antitumorigenic effects of cannabinoids beyond apoptosis
Published November 4, 2009; doi:10.1124/jpet.109.157735 [Abstract] [PDF]  

Yoshiaki Kitamura, Hiroyuki Kusuhara, and Yuichi Sugiyama

Functional characterization of multidrug resistance-associated protein 3 (Mrp3/Abcc3) in the basolateral efflux of glucuronide conjugates in the mouse small intestine
Published November 4, 2009; doi:10.1124/jpet.109.156943 [Abstract] [PDF]  

Chuang Lu, Suresh K. Balani, Mark G. Qian, Shimoga R. Prakash, Patricia S. Ducray, and Lisa L. von Moltke

QUANTITATIVE PREDICTION AND CLINICAL OBSERVATION OF A CYP3A INHIBITOR-BASED DRUG - DRUG INTERACTIONS WITH MLN3897, A POTENT CCR1 ANTAGONIST
Published November 4, 2009; doi:10.1124/jpet.109.161893 [Abstract] [PDF]  

Feng Han, Ying-mei Lu, Hideyuki Hasegawa, Hiroshi Kanai, Erika Hachimura, Yasufumi Shirasaki, and Kohji Fukunaga

Inhibition of dystrophin breakdown and endothelial nitric oxide synthase uncoupling accounts for cytoprotection by 3-[2-[4-(3-Chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole Dihydrochloride 3.5 Hydrate (DY-9760e) in left ventricular hypertrophied mice
Published November 4, 2009; doi:10.1124/jpet.109.161646 [Abstract] [PDF]  

29 October 2009

Kyle Rasbach, Jason A. Funk, Tamilselvan Jayavelu, Peter T. Green, and Rick G. Schnellmann

5-Hydroxytryptamine Receptor Stimulation of Mitochondrial Biogenesis
Published October 29, 2009; doi:10.1124/jpet.109.159947 [Abstract] [PDF]  

28 October 2009

Aruna R. Natarajan, Guichun Han, Shi-you Chen, Peiying Yu, Richard E. White, and Pedro A. Jose

The D₅ dopamine receptor mediates BK_Ca channel activation in human coronary artery smooth muscle cells
Published October 28, 2009; doi:10.1124/jpet.109.159871 [Abstract] [PDF]  

Shikha Snigdha, Masakuni Horiguchi, Zhu Li, Mei Huang, Mo Shahid, Joanna C. Neill, and Herbert Y. Meltzer

Attenuation of phencyclidine-induced object recognition deficits by the combination of atypical antipsychotic drugs with pimavanserin (ACP 103), a 5-hydroxytryptamine_2A receptor inverse agonist
Published October 28, 2009; doi:10.1124/jpet.109.156349 [Abstract] [PDF]  

Anibal Garza, Omar Lopez-Ramirez, Rosario Vega, and Enrique Soto

The aminoglycosides modulate the acid-sensing ionic-channel (ASIC) currents in dorsal-root ganglion neurons from the rat
Published October 28, 2009; doi:10.1124/jpet.109.152884 [Abstract] [PDF] [Data Supplement]  

Tai ning Lam and C. Anthony Hunt

Mechanistic Insight from In Silico Pharmacokinetic Experiments: Roles of P-glycoprotein, CYP3A4 Enzymes, and Microenvironments
Published October 28, 2009; doi:10.1124/jpet.109.160739 [Abstract] [PDF] [Data Supplement]  

Feng Liu, Amber Frick, Xing Yuan, and Leaf Huang

Dysopsonin Activity of Serum DNA-Binding Proteins Favorable for Gene Delivery
Published October 28, 2009; doi:10.1124/jpet.109.159541 [Abstract] [PDF]  

27 October 2009

Rong Zhou, Richard V. Mazurchuk, Judith H. Tamburlin, John M. Harrold, Donald E. Mager, and Robert M. Straubinger

Differential pharmacodynamic effects of paclitaxel formulations in an intracranial rat brain tumor model
Published October 27, 2009; doi:10.1124/jpet.109.160044 [Abstract] [PDF]  

23 October 2009

Amarjit S. Chaudhry, Thomas J. Urban, Jatinder K. Lamba, Angela K. Birnbaum, Rory P. Remmel, Murali Subramanian, Stephen Strom, Joyce H. You, Dalia Kasperaviciute, Claudia B. Catarino, Rodney A. Radtke, Sanjay M. Sisodiya, David B. Goldstein, and Erin G. Schuetz

CYP2C9*1B promoter polymorphisms, in linkage with CYP2C19*2, affect phenytoin auto-induction of clearance and maintenance dose
Published October 23, 2009; doi:10.1124/jpet.109.161026 [Abstract] [PDF] [Data Supplement]  

Johann Meunier and Teruo Hayashi

Sigma-1 receptors regulate Bcl-2 expression by ROS-dependent transcriptional regulation of NF-B
Published October 23, 2009; doi:10.1124/jpet.109.160960 [Abstract] [PDF]  

Justin Robert Nickell, Sairam Krishnamurthy, Seth Norrholm, Gabriela Deaciuc, Kiran B. Siripurapu, Guangrong Zheng, Peter A. Crooks, and Linda P. Dwoskin

Lobelane Inhibits Methamphetamine-Evoked Dopamine Release via Inhibition of the Vesicular Monoamine Transporter-2
Published October 23, 2009; doi:10.1124/jpet.109.160275 [Abstract] [PDF] [Data Supplement]  

Ai Ogawa, Hideru Obinata, Tomoyasu Hattori, Mikiko Kishi, Kazuaki Tatei, Osamu Ishikawa, and Takashi Izumi

Identification and analysis of two splice variants of human G2A generated by alternative splicing
Published October 23, 2009; doi:10.1124/jpet.109.158758 [Abstract] [PDF]  

21 October 2009

Joachim Hartmann, Cornelia Kiewert, and Jochen Klein

Neurotransmitters and Energy Metabolites in Amyloid-bearing APP_SWE x PSEN1dE9 Mouse Brain
Published October 21, 2009; doi:10.1124/jpet.109.161091 [Abstract] [PDF]  

Jose M. Escandell, Maria Carmen Recio, Rosa M. Giner, Salvador Manez, Miguel Cerda-Nicolas, Irmgard Merfort, and Jose Luis Rios

Inhibition of Delayed-Type Hypersensitivity by Cucurbitacin R Through the Curbing of Lymphocyte Proliferation and Cytokine Expression by Means of NFAT Translocation to the Nucleus
Published October 21, 2009; doi:10.1124/jpet.109.159327 [Abstract] [PDF]  

Izumi Kure, Shin Nishiumi, Yosuke Nishitani, Takeshi Tanoue, Tsukasa Ishida, Masashi Mizuno, Tsuyoshi Fujita, Hiromu Kutsumi, Makoto Arita, Takeshi Azuma, and Masaru Yoshida

Lipoxin A4 reduces lipopolysaccharide-induced inflammation in macrophages and intestinal epithelial cells through inhibition of NF-B activation
Published October 21, 2009; doi:10.1124/jpet.109.159046 [Abstract] [PDF]  

20 October 2009

Mae M. Huang, David H. Overtstreet, Darin J. Knapp, Robert Angel, Tiffany A. Wills, Montserrat Navarro, Jean Rivier, Wylie Vale, and George R. Breese

Corticotropin Releasing Factor (CRF) Sensitization of Ethanol Withdrawal-Induced Anxiety-like Behavior is Brain Site Specific and Mediated by CRF-1 Receptors: Relation to Stress-Induced Sensitization
Published October 20, 2009; doi:10.1124/jpet.109.159186 [Abstract] [PDF] [Data Supplement]  

Kathrin Mandery, Krystyna Bujok, Ingrid Schmidt, Thomas Wex, Gerhard Treiber, Peter Malfertheiner, Tilman T. Rau, Kerstin U. Amann, Kay Brune, Martin F. Fromm, and Hartmut Glaeser

Influence of cyclooxygenase inhibitors on the function of the prostaglandin transporter OATP2A1 expressed in human gastroduodenal mucosa
Published October 20, 2009; doi:10.1124/jpet.109.154518 [Abstract] [PDF]  

Stacey N. Williams and Ashiwel S. Undieh

Brain-derived neurotrophic factor signaling modulates cocaine induction of reward-associated ultrasonic vocalization in rats
Published October 20, 2009; doi:10.1124/jpet.109.158535 [Abstract] [PDF]  

19 October 2009

Paolo Spallarossa, Paola Altieri, Paolo Pronzato, Concetta Aloi, Giorgio Ghigliotti, Antonio Barsotti, and Claudio Brunelli

Sub-lethal doses of an anti-erbB2 antibody leads to death by apoptosis in cardiomyocytes sensitized by low pro-senescent doses of epirubicin: the protective role of dexrazoxane
Published October 19, 2009; doi:10.1124/jpet.109.159525 [Abstract] [PDF]  

Mias Pretorius and Nancy J Brown

Endogenous Nitric Oxide Contributes to Bradykinin-Stimulated Glucose Uptake but Attenuates Vascular t-PA Release
Published October 19, 2009; doi:10.1124/jpet.109.160168 [Abstract] [PDF]  

Jennifer Cheng, Cheng-Chia Wu, Katherine H Gotlinger, Frank Zhang, Dubasi Narsimhaswamy, John R Falck, and Michal Laniado Schwartzman

20-HETE MEDIATES ENDOTHELIAL DYSFUNCTION VIA IKK-DEPENDENT ENOS UNCOUPLING
Published October 19, 2009; doi:10.1124/jpet.109.159863 [Abstract] [PDF]  

Lu Zhang, Li Li, Heather W Leavesley, Xun Zhang, Joseph L Borowitz, and Gary E Isom

Cyanide-induced Apoptosis of Dopaminergic Cells is Promoted by BNIP3 and Bax Modulation of Endoplasmic Reticulum-Mitochondrial Ca²⁺ Levels
Published October 19, 2009; doi:10.1124/jpet.109.159103 [Abstract] [PDF] [Data Supplement]  

Hussien A Al-Shamma, Christen Anderson, Emil Chuang, Remy Luthringer, Andrew J Grottick, Erin Hauser, Michael Morgan, William Shanahan, Bradley R Teegarden, William J Thomsen, and Dominic Behan

Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine_2A Inverse Agonist for the Treatment of Insomnia
Published October 19, 2009; doi:10.1124/jpet.109.160994 [Abstract] [PDF] [Data Supplement]  

Gregory William Sawyer, Frederick J. Ehlert, and Crystal A. Shults

A Conserved Motif in the Membrane Proximal C-Terminal Tail of Human Muscarinic M₁ Acetylcholine Receptors Affects Plasma Membrane Expression
Published October 19, 2009; doi:10.1124/jpet.109.160986 [Abstract] [PDF]  

Jean-Philippe Fortin, Jonathan C. Schroeder, Yuantee Zhu, Martin Beinborn, and Alan S. Kopin

Pharmacological Characterization of Human Incretin Receptor Missense Variants
Published October 19, 2009; doi:10.1124/jpet.109.160531 [Abstract] [PDF] [Data Supplement]  

14 October 2009

Georgia E Hodes, Tiffany E Hill-Smith, Raymond F Suckow, Thomas B Cooper, and Irwin Lucki

Sex Specific Effects of Chronic Fluoxetine Treatment on Neuroplasticity and Pharmacokinetics in Mice
Published October 14, 2009; doi:10.1124/jpet.109.158717 [Abstract] [PDF]  

Julie A. Brennan, Radka Graf, Steven M. Grauer, Rachel L. Navarra, Claudine M. Pulicicchio, Zoe A. Hughes, Qian Lin, Caitlin Wantuch, Sharon Rosenzweig-Lipson, Farhana Pruthi, Margaret Lai, Deborah Smith, Wouter Goutier, Martina van de Neut, Albert J. Robichaud, David Rotella, Rolf W. Feenstra, Chris Kruse, Pierre Broqua, Chad E. Beyer, Andrew C. McCreary, Mark H. Pausch, and Karen L. Marquis

WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: A Novel Dopamine D₂ Receptor Partial Agonist / Serotonin Reuptake Inhibitor with Preclinical Antipsychotic-Like and Antidepressant-Like Activity
Published October 14, 2009; doi:10.1124/jpet.109.157388 [Abstract] [PDF]  

Pierluigi Onali, Simona Dedoni, and Maria C Olianas

Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes
Published October 14, 2009; doi:10.1124/jpet.109.159939 [Abstract] [PDF]  

Wen-Juan Zhao, Zhen-Yu Gao, Hong Wei, Hui-Zhen Nie, Qian Zhao, Xiang-Jun Zhou, and Yong-Xiang Wang

Spinal D-Amino Acid Oxidase Contributes to Neuropathic Pain in Rats
Published October 14, 2009; doi:10.1124/jpet.109.158816 [Abstract] [PDF]  

Iain A. Murray, Colin A. Flaveny, Brett C. DiNatale, Chris R. Chairo, Jennifer C. Schroeder, Ann Kusnadi, and Gary H. Perdew

Antagonism of aryl hydrocarbon receptor signaling by 6, 2', 4'-trimethoxyflavone
Published October 14, 2009; doi:10.1124/jpet.109.158261 [Abstract] [PDF] [Data Supplement]  

Xiao-dong Peng, Xiao-hua Wu, Li-juan Chen, Zhen-ling Wang, Xiao-hong Hu, Li-fang Song, Chun-mei He, You-fu Luo, Zhi-zhi Chen, Ke Jin, Xiao-lei Li, Hong-gang Lin, Yong-sheng Wang, and Yu-quan Wei

Inhibition of Phosphoinositide 3-Kinase Ameliorates Dextran Sodium Sulfate-Induced Colitis in Mice
Published October 14, 2009; doi:10.1124/jpet.109.153494 [Abstract] [PDF] [Data Supplement]  

9 October 2009

Tao Chen, Leslie M Tompkins, Linhao Li, Haishan Li, Gregory Kim, Yuxin Zheng, and Hongbing Wang

A Single Amino Acid Controls the Functional Switch of Human CAR1 to the Xenobiotic Sensitive Splicing Variant CAR3
Published October 9, 2009; doi:10.1124/jpet.109.159210 [Abstract] [PDF]  

Scott J. Fisher, Peter W. Swaan, and Natalie D. Eddington

The Ethanol Metabolite Acetaldehyde Increases Paracellular Drug Permeability In Vitro and Oral Bioavailability In Vivo
Published October 9, 2009; doi:10.1124/jpet.109.158642 [Abstract] [PDF]  

8 October 2009

Patrizia Giannoni, Andrew D. Medhurst, Maria-Beatrice Passani, Mariagrazia Giovannini, Chiara Ballini, Laura Della Corte, and Patrizio Blandina

Regional differential effects of the novel histamine H₃ receptor antagonist GSK189254 on histamine release in the CNS of freely moving rats
Published October 8, 2009; doi:10.1124/jpet.109.158444 [Abstract] [PDF]  

Moahmmed A. Abdelsaid, Bindu A. Pillai, Suraporn Matragoon, Roshini Prakash, Mohamed Al-Shabrawey, and Azza B. El-Remessy

Early Intervention of Tyrosine Nitration Prevents Vaso-obliteration and Neovascularization in Ischemic Retinopathy
Published October 8, 2009; doi:10.1124/jpet.109.157941 [Abstract] [PDF]  

Sabine Meis, Alexandra Hamacher, Darunee Hongwiset, Claudia Marzian, Michael Wiese, Niels Eckstein, Hans-Dieter Royer, Didier Communi, Jean-Marie Boeynaems, Ralf Hausmann, Gunther Schmalzing, and Matthias U. Kassack

NF546 [4,4'-(carbonylbis(imino-3,1-phenylene-carbonylimino-3,1 (4-methyl-phenylene)-carbonylimino))-bis(1,3-xylene-,'-diphosphonic acid) tetrasodium salt] is a non-nucleotide P2Y₁₁ agonist and stimulates release of IL-8 from human monocyte-derived dendritic cells
Published October 8, 2009; doi:10.1124/jpet.109.157750 [Abstract] [PDF] [Data Supplement]  

Maja T. Tomicic, Markus Christmann, and Bernd Kaina

Topotecan triggers apoptosis in p53-deficient cells by forcing degradation of XIAP and survivin thereby activating caspase-3 mediated Bid cleavage
Published October 8, 2009; doi:10.1124/jpet.109.159962 [Abstract] [PDF] [Data Supplement]  

6 October 2009

Kevin J Freise, John A Widness, and Peter Veng-Pedersen

Erythropoietic response to endogenous erythropoietin in premature very low birth weight infants
Published October 6, 2009; doi:10.1124/jpet.109.159905 [Abstract] [PDF] [Data Supplement]  

Xiaoqing He and Qiang Ma

Critical Cysteine Residues of Kelch-Like ECH-Associated Protein 1 in Arsenic-Sensing and Suppression of Nuclear Factor Erythroid 2-Related Factor 2
Published October 6, 2009; doi:10.1124/jpet.109.160465 [Abstract] [PDF]  

2 October 2009

Jin Kyung Lee, Tracy Marion, Koji Abe, Changwon Lim, Gary M Pollack, and Kim L. R. Brouwer

Hepatobiliary Disposition of Troglitazone and Metabolites in Rat and Human Sandwich-Cultured Hepatocytes: Use of Monte Carlo Simulations to Assess the Impact of Changes in Biliary Excretion on Troglitazone Sulfate Accumulation
Published October 2, 2009; doi:10.1124/jpet.109.156653 [Abstract] [PDF]  

1 October 2009

M Carla Zimmermann, Syreeta L Tilghman, Stephen M Boue, Virgilio A Salvo, Steven Elliott, K Y Williams, Elena V Skripnikova, Hasina Ashe, Florastina Payton-Stewart, Lyndsay Vanhoy-Rhodes, Juan Pablo Fonseca, Cynthia Corbitt, Bridgette M Collins-Burow, Melanie H Howell, Michelle Lacey, Betty Y Shih, Carol Carter-Wientjes, Thomas E Cleveland, John A McLachlan, Thomas E Wiese, Barbara S Beckman, and Matthew E Burow

Glyceollin I, a novel antiestrogenic phytoalexin isolated from activated soy
Published October 1, 2009; doi:10.1124/jpet.109.160382 [Abstract] [PDF]  

Benon E. Mugabe, Fariborz A. Yaghini, Chi Young Song, Cuneyt K. Buharalioglu, Christopher M. Waters, and Kafait U. Malik

Angiotensin II-Induced Migration of Vascular Smooth Muscle Cells is Mediated by p38-MAPK Activated c-Src Through Spleen Tyrosine Kinase and EGFR Transactivation
Published October 1, 2009; doi:10.1124/jpet.109.157552 [Abstract] [PDF]  

Michelle G Baladi, Amy H Newman, and Charles P. France

Dopamine D3 receptors mediate the discriminative stimulus effects of quinpirole in free-feeding rats
Published October 1, 2009; doi:10.1124/jpet.109.158394 [Abstract] [PDF]  

30 September 2009

Chiara Cervetto, Guido Maura, and Manuela Marcoli

Inhibition of Presynaptic Release-Facilitatory Kainate Autoreceptors by Extracellular Cyclic GMP
Published September 30, 2009; doi:10.1124/jpet.109.154955 [Abstract] [PDF]  

29 September 2009

Nancy A. Ator, John R. Atack, Richard J. Hargreaves, H. Donald Burns, and Gerard R. Dawson

Reducing Abuse Liability of GABA_A/Benzodiazepine Ligands via Selective Partial-Agonist Efficacy at ₁ and _2/3 Subtypes
Published September 29, 2009; doi:10.1124/jpet.109.158303 [Abstract] [PDF]  

Paula A Pousinha, Alexandra M Correia, Ana M Sebastiao, and Joaquim A Ribeiro

Predominance of adenosine excitatory over inhibitory effects on transmission at the neuromuscular junction of infant rats
Published September 29, 2009; doi:10.1124/jpet.109.157255 [Abstract] [PDF]  

Catriona M.H. Anderson, Mark Jevons, Muthusamy Thangaraju, Noel Edwards, Nichola J. Conlon, Steven Woods, Vadivel Ganapathy, and David T. Thwaites

Transport of the Photodynamic Therapy Agent 5-Aminolevulinic Acid by Distinct H⁺-Coupled Nutrient Carriers Co-expressed in the Small Intestine
Published September 29, 2009; doi:10.1124/jpet.109.159822 [Abstract] [PDF]  

28 September 2009

Mario B. Marrero, Rudolph Lucas, Christina Salet, Terry A. Hauser, Anatoly Mazurov, Patrick M. Lippiello, and Merouane Bencherif

An Alpha7 Nicotinic Acetylcholine Receptor-Selective Agonist Reduces Weight Gain and Metabolic Changes in a Mouse Model of Diabetes
Published September 28, 2009; doi:10.1124/jpet.109.154633 [Abstract] [PDF] [Data Supplement]  

Jeannette Zinggeler Berg, Jesse Mason, Angela J Boettcher, Dorothy K Hatsukami, and Sharon E Murphy

Nicotine metabolism in African Americans and European Americans: variation in glucuronidation by ethnicity and UGT2B10 haplotype
Published September 28, 2009; doi:10.1124/jpet.109.159855 [Abstract] [PDF]  

24 September 2009

Dean Y. Maeda, Mark T. Quinn, Igor A. Scheptekin, Liliya N. Kirpotina, and John A. Zebala

Nicotinamide glycolates antagonize CXCR2 activity through an intracellular mechanism
Published September 24, 2009; doi:10.1124/jpet.109.159020 [Abstract] [PDF] [Data Supplement]  

Yoshiyuki Shirasaka, Erika Kuraoka, Hildegard Spahn-Langguth, Takeo Nakanishi, Peter Langguth, and Ikumi Tamai

Species Difference in the Effect of Grapefruit Juice on Intestinal Absorption of Talinolol between Human and Rat
Published September 24, 2009; doi:10.1124/jpet.109.159756 [Abstract] [PDF]  

John Atack, Dean Wong, Timothy Fryer, Christine Ryan, Sandra Sanabria, Yun Zhou, Robert Dannals, Wai-Si Eng, Raymond Gibson, Donald Burns, Jose Vega, Laura Vessy, Paul Scott-Stevens, John Beech, Jean-Claude Baron, Bindi Sohal, Mike Schrag, Franklin Aigbirhio, Ruth M. McKernan, and Richard J. Hargreaves

Benzodiazepine binding site occupancy by the novel GABA_A receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates and man
Published September 24, 2009; doi:10.1124/jpet.109.157909 [Abstract] [PDF]  

Lenka Hahnova Cygalova, Jakub Hofman, Martina Ceckova, and Frantisek Staud

Transplacental pharmacokinetics of glyburide, rhodamine 123 and BODIPY FL prazosin; effect of drug efflux transporters and lipid solubility
Published September 24, 2009; doi:10.1124/jpet.109.160564 [Abstract] [PDF]  

Johan Gabrielsson and Alfred R Green

Quantitative pharmacology or pharmacokinetic pharmacodynamic integration should be a vital component in integrative pharmacology
Published September 24, 2009; doi:10.1124/jpet.109.157172 [Abstract] [PDF]  

23 September 2009

Prakasha Kempaiah, Leslie Danielson, Marc Barry, and Walter Kisiel

Comparative Effects of Aprotinin and Human Recombinant R24K KD1 on Temporal Renal Function in Long-Evans Rats
Published September 23, 2009; doi:10.1124/jpet.109.161034 [Abstract] [PDF]  

Juan J. Moreno

Differential Effects of Arachidonic and Eicosapentaenoic Acid Derived Eicosanoids on Polymorphonuclear Transmigration Across Endothelial Cell Cultures
Published September 23, 2009; doi:10.1124/jpet.109.157891 [Abstract] [PDF]  

22 September 2009

Lawrence R. Toll, Taline V Khroyan, Willma Polgar, Faming Jiang, Cris Olsen, and Nurulain T. Zaveri

Comparison of the Anti-nociceptive and Anti-Rewarding Profiles of Novel Bifunctional Nociceptin/Orphanin FQ Receptor (NOPr)-Mu Opioid Receptor (MOPr) Ligands: Implications for Therapeutic Applications
Published September 22, 2009; doi:10.1124/jpet.109.157446 [Abstract] [PDF]  

Leonardo Guzman, Gustavo Moraga-Cid, Ariel Avila, Maximiliano Figueroa, Gonzalo Yevenes, Jorge Fuentealba, and Luis G. Aguayo

Blockade of Ethanol-Induced Potentiation of Glycine Receptors by a Peptide that Interferes with Gβ Binding
Published September 22, 2009; doi:10.1124/jpet.109.160440 [Abstract] [PDF]  

Lars Bellner, Lucia Martinelli, Adna Halilovic, Kiran A Patil, Nitin Puri, Michael W Dunn, Raymond F Regan, and Michal Laniado Schwartzman

HO-2 deletion causes endothelial cell activation marked by oxidative stress, inflammation and angiogenesis
Published September 22, 2009; doi:10.1124/jpet.109.158352 [Abstract] [PDF]  

Yu-Ching Lu, Chao-Wei Chen, Su-Yi Wang, and Fong-Sen Wu

17β-Estradiol Mediates the Sex Difference in Capsaicin-Induced Nociception in Rats
Published September 22, 2009; doi:10.1124/jpet.109.158402 [Abstract] [PDF]  

21 September 2009

Xianglu Rong, Yuhao Li, Ken Ebihara, Mingming Zhao, Wufuerjiang Aini, Toru Kusakabe, Masakazu Hirata, Licht Miyamoto, Michael Murray, and Kazuwa Nakao

An adipose tissue-independent insulin-sensitizing action of telmisartan: a study in lipodystrophic mice
Published September 21, 2009; doi:10.1124/jpet.109.157099 [Abstract] [PDF]  

18 September 2009

Rachel Thomas, Christopher James Langmead, Martyn Wood, and R.A. John Challiss

Contrasting Effects of Allosteric and Orthosteric Agonists on M₁ Muscarinic Acetylcholine Receptor Internalization and Down-regulation
Published September 18, 2009; doi:10.1124/jpet.109.160242 [Abstract] [PDF]  

Masaaki Miyata, Yuki Takamatsu, Hideaki Kuribayashi, and Yasushi Yamazoe

Administration of ampicillin elevates hepatic primary bile acid synthesis through suppression of ileal FGF15 expression
Published September 18, 2009; doi:10.1124/jpet.109.160093 [Abstract] [PDF]  

17 September 2009

Xiaoming Deng, Ganna Tolstanova, Tetyana Khomenko, Longchuan Chen, Andrzej S. Tarnawski, Sandor Szabo, and Zsuzsanna Sandor

Mesalamine restores angiogenic balance in experimental ulcerative colitis by reducing expression of endostatin and angiostatin: Novel molecular mechanism for mesalamine's therapeutic action
Published September 17, 2009; doi:10.1124/jpet.109.158022 [Abstract] [PDF]  

Yuenmu Chen, John R. Falck, Venugopal R. Tuniki, and William B. Campbell

20-¹²⁵Iodo-14,15-Epoxyeicosa-5Z-enoic Acid: a High Affinity Radioligand Used to Characterize the Epoxyeicosatrienoic Acid Antagonist Binding Site
Published September 17, 2009; doi:10.1124/jpet.109.157818 [Abstract] [PDF] [Data Supplement]  

16 September 2009

Jenny Ying Lin Lu, Yuhua Yang, Gilles Gnacadja, Arthur Christopoulos, and Jeff D. Reagan

Effect of the Calcimimetic R-568 on Correcting Inactivating Mutations in the Human Calcium-Sensing Receptor
Published September 16, 2009; doi:10.1124/jpet.109.159228 [Abstract] [PDF]  

Michael Erb, Sarina Meinen, Patrizia Barzaghi, Lazar T. Sumanovski, Isabelle Courdier-Fruh, Markus A. Ruegg, and Thomas Meier

Omigapil ameliorates the pathology of muscle dystrophy caused by laminin-2 deficiency
Published September 16, 2009; doi:10.1124/jpet.109.160754 [Abstract] [PDF] [Data Supplement]  

15 September 2009

Matthew J Fell, Kenneth W Perry, Julie F Falcone, Bryan G Johnson, Vanessa N Barth, Karen S Rash, Virginia L Lucaites, Penny G Threlkeld, James A Monn, David McKinize, Gerard J Marek, Kjell A Svensson, and David L. Nelson

In vitro and in vivo evidence for a lack of interaction with Dopamine D₂ receptors by the mGlu_2/3 receptor agonists LY354740 and LY379268
Published September 15, 2009; doi:10.1124/jpet.109.160598 [Abstract] [PDF] [Data Supplement]  

Concetta Crisafulli, Stefano Bruscoli, Emanuela Esposito, Emanuela Mazzon, Rosanna Di Paola, Tiziana Genovese, Placido Bramanti, Graziella Migliorati, and Salvatore Cuzzocrea

PPAR- contributes to the anti-inflammatory activity of 17-estradiol
Published September 15, 2009; doi:10.1124/jpet.109.156646 [Abstract] [PDF]  

14 September 2009

Qing Liu, Manjunatha Bhat, Wayne D Bowen, and Jianguo Cheng

Signaling pathways from CB1 receptor activation to inhibition of NMDA-mediated calcium influx and neurotoxicity in dorsal root ganglion neurons
Published September 14, 2009; doi:10.1124/jpet.109.156216 [Abstract] [PDF]  

11 September 2009

Daniel S Lorrain, Gretchen Bain, Lucia D Correa, Charles Chapman, Alex Broadhead, Angelina Santini, Pat Prodanovich, Janice Darlington, John H Hutchinson, Christopher King, Catherine Lee, Christopher Baccei, Yiwei Li, Jeannie Arruda, and Jilly F Evans

Pharmacological Characterization of AM103, a Novel Selective Five-lipoxygenase -Activating Protein (FLAP) Inhibitor Reduces Acute and Chronic Inflammation
Published September 11, 2009; doi:10.1124/jpet.109.158089 [Abstract] [PDF]  

Laura M Kreckler, Elizabeth Gizewski, Tina C Wan, and John A. Auchampach

Adenosine suppresses LPS-induced TNF- production by murine macrophages through a protein kinase A- and Epac-independent signaling pathway
Published September 11, 2009; doi:10.1124/jpet.109.157651 [Abstract] [PDF]  

Yukio Hara, Asako Ike, Riyo Tanida, Muneyoshi Okada, and Hideyuki Yamawaki

Involvement of cyclooxygenase-2 in carbachol-induced positive inotropic response in mouse isolated left atrium
Published September 11, 2009; doi:10.1124/jpet.109.156992 [Abstract] [PDF]  

10 September 2009

Cecilia Cialdai, Sandro Giuliani, Claudio Valenti, Manuela Tramontana, and Carlo Alberto Maggi

Effect of intra-articular MEN16132, a kinin B₂ receptor antagonist, on nociceptive response in monosodium iodoacetate-induced experimental osteoarthritis in rats
Published September 10, 2009; doi:10.1124/jpet.109.159657 [Abstract] [PDF]  

Kathrin Hatlapatka, Antje Wienbergen, Claudia Kuehne, Anne Joerns, Michael Willenborg, and Ingo Rustenbeck

Selective enhancement of nutrient-induced insulin secretion by K_ATP channel-blocking imidazolines
Published September 10, 2009; doi:10.1124/jpet.109.152751 [Abstract] [PDF]  

9 September 2009

Yasco Aracava, Edna Pereira, Miriam Akkerman, Michael Adler, and Edson X Albuquerque

Effectiveness of donepezil, rivastigmine and (±)huperzine A in counteracting the acute toxicity of organophosphorus nerve agents: Comparison with galantamine
Published September 9, 2009; doi:10.1124/jpet.109.160028 [Abstract] [PDF]  

Michael J. Wacker, Lisa M. Kosloski, William J.R. Gilbert, Chad D. Touchberry, David S. Moore, John K. Kelly, Marco A. Brotto, and James A. Orr

Inhibition of thromboxane A₂-induced arrhythmias and intracellular calcium changes in cardiac myocytes by blockade of the IP₃ pathway
Published September 9, 2009; doi:10.1124/jpet.109.157677 [Abstract] [PDF]  

Shi Liang, Kevin Pong, Cathleen Gonzales, Yi Chen, Huai-Ping Ling, Robert J. Mark, Frank Boschelli, Diane H. Boschelli, Fei Ye, Ana C. Barrios Sosa, Tarek S. Mansour, Philip Frost, Andrew Wood, Menelas N. Pangalos, and Margaret M. Zaleska

Neuroprotective Profile of Novel Src Kinase Inhibitors in Rodent Models of Cerebral Ischemia
Published September 9, 2009; doi:10.1124/jpet.109.156562 [Abstract] [PDF]  

Andrew G. Jobson, George T. Lountos, Philip L. Lorenzi, Jenny Llamas, John Connelly, David Cerna, Joseph E. Tropea, Akikazu Onda, Gabriele Zoppoli, Sudhir Kondapaka, Guangtao Zhang, Natasha J. Caplen, John H. Cardellina, Stephen S. Yoo, Anne Monks, Christopher Self, David S. Waugh, Robert H. Shoemaker, and Yves Pommier

Cellular inhibition of Chk2 kinase and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019
Published September 9, 2009; doi:10.1124/jpet.109.154997 [Abstract] [PDF] [Data Supplement]  

Eun Joo Jung, Minkyu Hur, Young Lim Kim, Ge Hyeong Lee, Jeongmin Kim, Ikyon Kim, MinWoo Lee, Ho-Kyun Han, Mi-Soon Kim, Sejin Hwang, Sungjoo Kim, A Mi Woo, Yeup Yoon, Heon Jin Park, and Jonghwa Won

Oral administration of 1, 4-aryl-2-mercaptoimidazole (KRM-III) inhibits T cell proliferation and reduces clinical severity in murine experimental autoimmune encephalomyelitis model
Published September 9, 2009; doi:10.1124/jpet.109.154948 [Abstract] [PDF]  

8 September 2009

Kento Kitada, Nozomi Yui, Chika Matsumoto, Tatsuhiko Mori, Mamoru Ohkita, and Yasuo Matsumura

Inhibition of Endothelin ET_B Receptor System Aggravates Neointimal Hyperplasia after Balloon Injury of Rat Carotid Artery
Published September 8, 2009; doi:10.1124/jpet.109.157065 [Abstract] [PDF]  

4 September 2009

Xin Chen, Tharsika Tharmanathan, Baskar Mannargudi, Hong Gou, and Jack P Uetrecht

A Study of the Specificity of Lymphocytes in Nevirapine-induced Skin Rash
Published September 4, 2009; doi:10.1124/jpet.109.157362 [Abstract] [PDF]  

3 September 2009

Anna M. Nelson, Gaynor A. Larson, and Nancy R. Zahniser

Low or high cocaine responding rats differ in striatal extracellular dopamine levels and dopamine transporter number
Published September 3, 2009; doi:10.1124/jpet.109.159897 [Abstract] [PDF]  

Frank S. Menniti, JingMei Ren, Timothy M. Coskran, Jing Liu, Daniel G. Morton, Dana K. Sietsma, Angel Som, Diane T. Stephenson, Barbara A. Tate, and Seth P. Finklestein

PDE5A inhibitors improve functional recovery after stroke in rats: optimized dosing regimen with implications for mechanism
Published September 3, 2009; doi:10.1124/jpet.109.156919 [Abstract] [PDF] [Data Supplement]  

2 September 2009

Hao Sun, De-Pei Li, Shao-Rui Chen, Walter Hittelman, and Hui-Lin Pan

Sensing of Blood Pressure Increase by Transient Receptor Potential Vanilloid 1 Receptors on Baroreceptors
Published September 2, 2009; doi:10.1124/jpet.109.160473 [Abstract] [PDF]  

Corigan Thetford Smothers and John J Woodward

Expression of Glycine-Activated Diheteromeric NR1/NR3 Receptors in HEK293 Cells is NR1 Splice Variant Dependent
Published September 2, 2009; doi:10.1124/jpet.109.158493 [Abstract] [PDF]  

Toshihisa Inada, Keita Arai, Michiko Kawamura, Ko Hatanaka, Yuichi Sato, Makoto Noshiro, and Yoshiteru Harada

Contribution of the prostaglandin E2/EP2 receptor-signaling pathway in abscess formation in rat zymosan-induced pleurisy
Published September 2, 2009; doi:10.1124/jpet.109.155358 [Abstract] [PDF]  

31 August 2009

Heidi R Hope, Gary D Anderson, Barry L Burnette, Robert P Compton, Rajesh V Devraj, Jeffrey L Hirsch, Robert H Keith, Xiong Li, Gabriel Mbalaviele, Dean M Messing, Matthew J Saabye, John F Schindler, Shaun R Selness, Loreen I Stillwell, Elizabeth G Webb, Jian Zhang, and Joseph B Monahan

Anti-inflammatory Properties of a Novel N-phenyl Pyridinone Inhibitor of p38 MAP Kinase: Preclinical to Clinical Translation
Published August 31, 2009; doi:10.1124/jpet.109.158329 [Abstract] [PDF]  

Wei Gu, Hai Yan, Katherine A. Winters, Renee Komorowski, Steven Vonderfecht, Larissa Atangan, Glenn Sivits, David Hill, Jie Yang, Vivian Bi, Yuqing Shen, Sylvia Hu, Tom Boone, Richard A. Lindberg, and Murielle M. Veniant

Long-term Inhibition of the Glucagon Receptor with a Monoclonal Antibody in Mice Causes Sustained Improvement in Glycemic Control, with Reversibility of Alpha-Cell Hyperplasia and Hyperglucagonemia
Published August 31, 2009; doi:10.1124/jpet.109.157685 [Abstract] [PDF]  

28 August 2009

Kyle E Montgomery, Markus Kessler, and Amy C. Arai

Modulation of agonist binding to AMPA receptors by CX546: Differential effects across brain regions and GluA1-4/TARP combinations
Published August 28, 2009; doi:10.1124/jpet.109.158014 [Abstract] [PDF] [Data Supplement]  

Komal Sodhi, Kazuyoshi Inoue, Katherine Gotlinger, Martina Canestraro, Luca Vanella, Dong Hyun Kim, Vijay L. Manthati, Sreenivasulu Reddy Koduru, John R. Falck, Michal L. Schwartzman, and Nader G. Abraham

EET Agonist Rescues the Metabolic Syndrome Phenotype of HO-2 Null Mice
Published August 28, 2009; doi:10.1124/jpet.109.157545 [Abstract] [PDF]  

Martin de Borst, Jai Prakash, Maria Sandovici, Pieter A. Klok, Inge Hamming, Robbert Jan Kok, Gerjan Navis, and Harry van Goor

c-Jun N-terminal kinase is crucially involved in renal tubulo-interstitial inflammation
Published August 28, 2009; doi:10.1124/jpet.109.154179 [Abstract] [PDF]  

27 August 2009

Taline V Khroyan, Willma E. Polgar, Faming Jiang, Nurulain T. Zaveri, and Lawrence Toll

NOP Receptor Activation Attenuates Antinociception Induced by Mixed NOP/Mu-Opioid Receptor Agonists
Published August 27, 2009; doi:10.1124/jpet.109.156711 [Abstract] [PDF]  

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