The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
September 2003
Vol. 306, No. 3
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Contribution of Lymphatically Transported TestosteroneDavid M. Shackleford,
Undecanoate to the Systemic Exposure of Testosterone afterW. A. (Fried) Faassen, Natalie Houwing,
Oral Administration of Two Andriol Formulations inHolger Lass, Glenn A. Edwards,
Conscious Lymph Duct-Cannulated DogsChristopher J. H. Porter, and
William N. Charman
Contents
PERSPECTIVES IN PHARMACOLOGY
The Cholinergic Hypothesis of Age and Alzheimer's Disease-Related Cognitive Deficits: Recent Challenges and Their Implications for Novel Drug Development
Characterization of Blood-Brain Barrier Permeability to ,* in the Mouse
Avasimibe Induces CYP3A4 and Multiple Drug Resistance Protein 1 Gene Expression through Activation of the Pregnane X Receptor
Multiple Injections of Pegylated Liposomal Doxorubicin: Pharmacokinetics and Therapeutic Activity
Aromatase Is the Major Enzyme Metabolizing Buprenorphine in Human Placenta
Genetic Variability at the Human FMO1 Locus: Significance of a Basal Promoter Yin Yang 1 Element Polymorphism
(FMO 1*6)
A. V. Terry Jr. and J. J. Buccafusco
Naoko Nonaka, Seiji Shioda,
Michael L. Niehoff, and William A. Banks
Jasminder Sahi, Mark A. Milad, Xianxian Zheng, Kelly A. Rose, Hongbing Wang, Linda Stilgenbauer, Darryl Gilbert, Summer Jolley, Ralph H. Stern, and Edward L. LeCluyse
Gregory J. R. Charrois and Theresa M. Allen
Sujal V. Deshmukh, Tatiana N. Nanovskaya, and Mahmoud S. Ahmed
Ronald N. Hines, Zhaohui Luo, Kathleen A. Hopp, Erwin T. Cabacungan, Sevasti B. Koukouritaki, and D. Gail McCarver
821
925
948 1027
1058 1099
1210
BEHAVIORAL PHARMACOLOGY
Topical Capsaicin-Induced Allodynia in Unanesthetized Primates: Pharmacological Modulation
Temporal Effects of Stress by Immobilization and Sensitivity of the Isolated Rat Pacemaker to Isoproterenol: Roles of Corticosterone, Neuronal Uptake, and /3-Adrenergic Homogeneity
GABAergic Systems Modulate Nicotinic Receptor-Mediated Seizures in Mice
Relative Efficacy of Buprenorphine, Nalbuphine and Morphine in Opioid-Treated Rhesus Monkeys Discriminating
Naltrexone
CARDIOVASCULAR
Role of Peripheral Benzodiazepine Receptors in Mitochondrial, Cellular, and Cardiac Damage Induced by Oxidative Stress and Ischemia-Reperfusion
Nicotine Induces a Long QT Phenotype in Kcnql-Deficient
Mouse Hearts
Effects of Reboxetine on Sympathetic Neuroeffector Transmission in Rabbit Carotid Artery
Eduardo R. Butelman, Jonathan W. Ball,1106
Todd J. Harris, and Mary Jeanne Kreek
Marco Aurelio de Paula Brotto1152
Peter Dobelis, Scott Hutton, Ying Lu, and1159
Allan C. Collins
Stacy L. Sell, Lance R. McMahon, and1167
Charles P. France
Nathalie Leducq, Francoise Bono,828
Thierry Sulpice, Valerie Vin, Philip Janiak, Gerard Le Fur, Steve E. O'Connor, and Jean-Marc Herbert
Toshimasa Tosaka, Mathew C. Casimiro,980
Qi Rong, Srihari Telia, Michelle Oh, Alexander N. Katchman, John C. Pezzullo, Karl Pfeifer, and Steven N. Ebert
Lasse E. Rasmusscn and Ove A. Nedergaard995
Pilot Intervention: Aerosolized AdrenomeduIIin Reduces Pulmonary Hypertension
Inhibition of Canine (NCX1.1) and Drosophita (CALX1.1) Na+-Ca2+ Exchangers by 7-Chloro-3,5-dihydro-5-phenyl-lff-4,1 -benzothiazepine-2-one (CGP-37157)
Pharmacological Interruption of Acute Thrombus Formation with Minimal Hemorrhagic Complications by a Small Molecule Tissue Factor/Factor Vila Inhibitor: Comparison to Factor Xa and Thrombin Inhibition in a Nonhuman Primate Thrombosis Model
Pharmacological Characterization of the New Stable Antiarrhythmic Peptide Analog Ac-D-Tyr-D-Pro-D-Hyp-Gly-D-Ala-Gly-NH2 (ZP123): In Vivo and in Vitro Studies
Functional and Binding Characterizations of Urotensin II-Related Peptides in Human and Rat Urotensin II-Receptor Assay
Michael A. Kandler, Katharina von der Hardt, Suleiman Mahfoud, Martin Chada, Ellen Sclioof, Thomas Papadopouios, Wolfgang Rascher, and Jorg Dotsch
Alexander Omelchenko, Ron Bouchard, Hoa Dinh Le, Platon Choptiany, Neeraj Visen, Mark Hnatowich, and Larry V. Hryshko
Osman D. Suleymanov, James A. Szalony, Anita K. Salyers, Rhonda M. LaChance, John J. Parlow, Michael S. South, Rhonda S. Wood, and Nancy S. Nicholson
Anne Louise Kj0lbye,
Carsten Boye Knudsen, Trine Jepsen,
Bjarne Due Larsen, and
J0rgen S0berg Petersen
Alexandre Brkovic, Almut Hattenberger, Evi Kostenis, Thomas Klabunde, Stefanie Flohr, Michael Kurz, Steve Bourgault, and Alain Fournier
1021
1050
1115
1191
1200
CELLULAR AND MOLECULAR
A Selective and Oral Small Molecule Inhibitor of Vascular Epithelial Growth Factor Receptor (VEGFR)-2 and VEGFR-1 Inhibits Neovascularization and Vascular Permeability
Dopamine Modulation of Membrane Excitability in Striatal Spiny Neurons is Altered in DARPP-32 Knockout Mice
The Cytoplasmic Domain of Alzheimer's Amyloid-j3 Protein Precursor Causes Sustained Apoptosis Signal-Regulating Kinase 1/c-Jun NH2-Terminal Kinase-Mediated Neurotoxic
Signal via Dimerization
cDNA Microarray Analysis Reveals a Nuclear Factor-KB-Independent Regulation of Macrophage Function by Adenosine
Cilostazol Prevents Tumor Necrosis Factor-a-Induced Cell Death by Suppression of Phosphatase and Tensin Homolog Deleted from Chromosome 10 Phosphorylation and Activation of Akt/Cyclic AMP Response Element-Binding Protein
Phosphorylation
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL Prevention of Ethanol-Induced Liver Injury in Rats by an Agonist of Peroxisome Proliferator-Activated Receptor-y, Pioglitazone
Reversal of Multiple Drug Resistance in Cholangiocarcinoma by the Glutathione S-Transferase-Tr-Specific Inhibitor Ol-Hexadecyl-y-glutamyl-S-benzylcysteinyl-D-phenylglycine Ethylester
Neela Patel, Li Sun, Deborah Moshinsky, Hui Chen, Kathleen M. Leahy, Phuong Le, Katherine G. Moss, Xueyan Wang, Audie Rice, Danny Tarn, A. Douglas Laird, Xiaoming Yu, Qingling Zhang, Cho Tang, Gerald McMahon, and Anthony Howlett
Shao-Pii Onn, Allen A. Fienberg, and Anthony A. Grace
Yuichi Hashimoto, Takako Niikura, Tomohiro Chiba, Emi Tsukamoto, Hisae Kadowaki, Hideki Nishitoh, Yohichi Yamagishi, Miho Ishizaka, Marina Yamada, Mikiro Nawa, Kenzo Terashita, Sadakazu Aiso, Hidenori Ichijo, and Ikuo Nishimoto
Zoltan H. Nemeth, S. Joseph Leibovich, Edwin A. Deitch, E. Sylvester Vizi, Csaba Szabd, and Gyorgy Hasko
Ki Whan Hong, Ki Young Kim, Hwa Kyoung Shin, Jeong Hyun Lee, Jae Moon Choi, Yong-Geun Kwak, Chi Dae Kim, Won Suk Lee, and Byung Yong Rhim
Nobuyuki Enomoto, Yoshiyuki Takei, Miyoko Hirose, Akira Konno, Tomoyoshi Shibuya, Shujiro Matsuyama, Satoko Suzuki,
Kenichi Ikejima Tsuneo Kitamura, and Nobuhiro Sato
Takaharu Nakajima, Tetsuji Takayama, Koji Miyanishi, Atsushi Nobuoka, Tsuyoshi Hayashi, Tomoyuki Abe, Junji Kato, Kiyoyuki Sakon, Yoshimitsu Naniwa, Hirohumi Tanabe, and Yoshiro Niitsu
838
870 889
1042
1182
846
861
INFLAMMATION AND IMMUNOPHARMACOLOGY
A Small Molecule ct4fotlfx4$7Antagonist Differentiates between the Low-Affinity States of a^ and a4f57: Characterization of Divalent Cation Dependence
Evidence for Cannahinoid Receptor-Dependent and -Independent Mechanisms of Action in Leukocytes
Effect of Ibuprofen on Neutrophil Migration in Vivo in Cystic Fibrosis and Healthy Subjects
The Orally Available Spleen Tyrosine Kinase Inhibitor 2-[7-(3,4-Dimethoxy phenyl)-imidazo[l,2-c]pyrimidin-5-ylamino]-nicotinamide Dihydrochloride (BAY 61-3606) Blocks Antigen-Induced Airway Inflammation in Rodents
Linda A. Egger, Jin Cao, Christine McCallura, Usha Kidambi, Gail Van Riper, Ermengilda McCauley, Richard A. Mumford, Thomas J. Lanza, Linus S. Lin, Stephen E. de Laszlo, David N. Young, Ginger Yang, Dennis C. Dean, Conrad E. Raab, Mike A. Wallace, Allen N. Jones, William K. Hagmann, John A. Schmidt, R. Blake Pepinsky, Daniel M. Scott, Wen-Cherng Lee, Mark A. Cornebise, and Patricia A. Detmers
Barbara L. Faubert Kaplan, Cheryl E. Rockwell, and Norbert E. Kaminski
Michael W. Konstan, Jeanne E. Krenicky, Marcie R. Finney, H. Lester Kirchner, Kathleen A. Hilliard, Jay B. Hilliard, Pamela B. Davis, and Charles L. Hoppel
Noriyuki Yarnamoto, Keisuke Takeshita, Mkhitaka Shichijo, Toshio Kokubo, Masako Sato, Kosuke Nakashima, Mina Ishimori, Hiroichi Nagai, Ying-Fu Li, Takeshi Yura, and Kevin B. Bacon
903
1077
1086
1174
NEUROPHARMACOLOGY
Sympathetic Innervation in the 1 -Methyl -4-phenyl-l,2,3,6-tetrahydropyridine Primate Model of Parkinson's Disease
Differential Regulation of the Endocannabinoids Anandamidc and 2-Arachidonylglycerol within the Limbic Forebrain by Dopamine Receptor Activity
Differential Actions of Fipronil and Dieldrin Insecticides on GABA-Gated Chloride Channels in Cockroach Neurons
Steroids Modulate /V-Methyl-D-aspartate-stimulated [3H]Dopamine Release from Rat Striatum via or Receptors
The Novel Melatonin Agonist Agomelatine (S20098) Is an Antagonist at 5-Hydroxytryptamine2c Receptors, Blockade of Which Enhances the Activity of Frontocortical Dopaminergic and Adrenergic Pathways
jx-Opioid-Induced Desensitization of Opioid Receptor-Like 1 and fi-Opioid Receptors: Differential Intracellular Signaling * Determines Receptor Sensitivity
L-Setegiline Potentiates the Cellular Poly(ADP-Ribosyl)ation Response to Ionizing Radiation
The Endogenous Cannabinoid Anandamide Inhibits a? Nicotinic Acetylcholine Receptor-Mediated Responses in
Xenopus Oocytes
/V-H-Alkylpyridinium Analogs, a Novel Class of Nicotinic Receptor Antagonists: Selective Inhibition of Nicotine-Evoked [3H]Dopamine Overflow from Superfused Rat Striatal Slices
Effect of Transport Inhibitors and Additional Anti-HIV Drugs on the Movement of Lamivudine (3TC) across the Guinea Pig Brain Barriers
Group II Metabotropic and a-Amino-3-hydroxy-5-methyl-4-isoxazole Propionate (AMPA)/Kainate Glutamate Receptors Regulate the Deficit in Brain Reward Function Associated with Nicotine Withdrawal in Rats
Treatment of Adverse Effects of Excessive Phencyclidine Exposure in Rats with a Minimal Dose of Monoclonal Antibody
Role of Na+,K+-ATPase in Morphine-Induced Antinociception
David S. Goldstein, Sheng-Ting Li, Courtney Holmes, and Krys Bankiewicz
Sachin Patel, David J. Rademacher, and Cecilia J. Hillard
Xilong Zhao, Vincent L. Salgado, Jay Z. Yeh, and Toshio Narahashi
Samer J. Nuwayhid and Linda L. Werling
M. J. Millan, A. Gobert, F. Lejeune, A. Dekeyne, A. Newman-Tancredi, V. Pasteau, J.-M. Rivet, and D. Cussac
Chitra D. Mandyam, Deepak R. Thakker, and Kelly M. Standifer
Christine Brabeck, Ragen Pfeiffer,
Alan Leake, Sascha Beneke, Ralph Meyer,
and Alexander Biirkle
Murat Oz, Arippa Ravindran, Oscar Diaz-Ruiz, Li Zhang, and Marisela Morales
Vladimir P. Grinevich, Peter A. Crooks, Sangeetha P. Sumilhran, Aaron J. Haubner, Joshua T. Ayers, and Linda P. Dwoskin
J. E. Gibbs, T. Rashid, and S. A. Thomas
Paul J. Kenny, Fabrizio Gasparini, and Athina Markou
Elizabeth M. Laurenzana,
Melinda G. Gunnell, W. Brooks Gentry, and
S. Michael Owens
Willias Masocha, Gyongyi Horvath, Ahmad Agil, Maria Ocafia, Esperanza Del Pozo, Margit Szikszay, and Jose M. Baeyens
855 880
914 934 954
965
973
1003
1011
ATP Augments Peptide Release from Rat Sensory Neurons in Culture through Activation of P2Y Receptors
Long-Term Effects of Olanzapine, Risperidone, and Quetiapine on Ionotropic Glutamate Receptor Types: Implications for Antipsychotic Drug Treatment
TOXICOLOGY
Rat Hepatic CYP2E1 Is Induced by Very Low Nicotine Doses: An Investigation of Induction, Time Course, Dose Response, and Mechanism
Role of Cysteine S-Conjugate 0-Lyase in the Metabolism of Cisplatin
Comparative Effects of Methylmercury and Hg2+ on Human Neuronal N- and R-Type High-Voltage Activated Calcium Channels Transiently Expressed in Human Embryonic Kidney
293 Cells
H. Huang, X. Wu, G. D. Nicol, S. Meller, and M. R. Vasko
Frank I. Tarazi, Ross J. Baldessarini, Nora S. Kula, and Kehong Zhang
Alina L. Micu, Sharon Miksys,
Edward M. Sellers, Dennis R. Koop, and
Rachel F. Tyndale
Lei Zhang and Marie H. Hanigan
Ravindra K. Hajela, Shuang-Qing Peng, and William D. Atchison
1145
941
988 1129