The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol. 306, No. 3
September 2003
Contents
PERSPECTIVES IN PHARMACOLOGY
The Cholinergic Hypothesis of Age and Alzheimer's DiseaseRelated Cognitive Deficits: Recent Challenges and Their
Implications for Novel Drug Development
A. V. Terry Jr. and J. J. Buccafusco
Naoko Nonaka, Seiji Shioda,
Michael L. Niehoff, and William A. Banks
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Contribution of Lymphatically Transported Testosterone
David M. Shackleford,
Undecanoate to the Systemic Exposure of Testosterone after
W. A. (Fried) Faassen, Natalie Houwing,
Oral Administration of Two Andriol Formulations in
Holger Lass, Glenn A. Edwards,
Conscious Lymph Duct-Cannulated Dogs
Christopher J. H. Porter, and
William N. Charman
Linda Stilgenbauer, Darryl Gilbert, Summer
Characterization of Blood-Brain Barrier Permeability to
Jolley, Ralph H. Stern, and Edward L.
,* in the Mouse
LeCluyse
Avasimibe Induces CYP3A4 and Multiple Drug Resistance
Gregory J. R. Charrois and Theresa M. Allen
Protein 1 Gene Expression through Activation of the
Pregnane X Receptor
Sujal V. Deshmukh, Tatiana N. Nanovskaya,
and Mahmoud S. Ahmed
Ronald N. Hines, Zhaohui Luo, Kathleen A.
Multiple Injections of Pegylated Liposomal Doxorubicin:
Hopp, Erwin T. Cabacungan, Sevasti B.
Pharmacokinetics and Therapeutic Activity
Koukouritaki, and D. Gail McCarver
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)
BEHAVIORAL PHARMACOLOGY
Topical Capsaicin-Induced Allodynia in Unanesthetized
Primates: Pharmacological Modulation
821
Jasminder Sahi, Mark A. Milad, Xianxian
Zheng, Kelly A. Rose, Hongbing Wang,
925
948
1027
1058
1099
1210
Eduardo R. Butelman, Jonathan W. Ball,
Todd J. Harris, and Mary Jeanne Kreek
1106
Temporal Effects of Stress by Immobilization and Sensitivity
of the Isolated Rat Pacemaker to Isoproterenol: Roles of
Corticosterone, Neuronal Uptake, and /3-Adrenergic
Homogeneity
Marco Aurelio de Paula Brotto
1152
GABAergic Systems Modulate Nicotinic Receptor-Mediated
Seizures in Mice
Peter Dobelis, Scott Hutton, Ying Lu, and
Allan C. Collins
1159
Relative Efficacy of Buprenorphine, Nalbuphine and
Morphine in Opioid-Treated Rhesus Monkeys Discriminating
Naltrexone
Stacy L. Sell, Lance R. McMahon, and
Charles P. France
1167
CARDIOVASCULAR
Role of Peripheral Benzodiazepine Receptors in
Mitochondrial, Cellular, and Cardiac Damage Induced by
Oxidative Stress and Ischemia-Reperfusion
Nathalie Leducq, Francoise Bono,
Thierry Sulpice, Valerie Vin, Philip Janiak,
Gerard Le Fur, Steve E. O'Connor, and JeanMarc Herbert
828
Nicotine Induces a Long QT Phenotype in Kcnql-Deficient
Mouse Hearts
Toshimasa Tosaka, Mathew C. Casimiro,
Qi Rong, Srihari Telia, Michelle Oh,
Alexander N. Katchman, John C. Pezzullo,
Karl Pfeifer, and Steven N. Ebert
980
Effects of Reboxetine on Sympathetic Neuroeffector
Transmission in Rabbit Carotid Artery
Lasse E. Rasmusscn and Ove A. Nedergaard
995
Pilot Intervention: Aerosolized AdrenomeduIIin Reduces
Pulmonary Hypertension
Michael A. Kandler, Katharina von der Hardt,
Suleiman Mahfoud, Martin Chada, Ellen
Sclioof, Thomas Papadopouios, Wolfgang
Rascher, and Jorg Dotsch
1021
Inhibition of Canine (NCX1.1) and Drosophita (CALX1.1)
Na+-Ca2+ Exchangers by 7-Chloro-3,5-dihydro-5-phenyl-lff4,1 -benzothiazepine-2-one (CGP-37157)
Alexander Omelchenko, Ron Bouchard, Hoa
Dinh Le, Platon Choptiany, Neeraj Visen,
Mark Hnatowich, and Larry V. Hryshko
1050
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
1115
Pharmacological Characterization of the New Stable
Antiarrhythmic Peptide Analog Ac-D-Tyr-D-Pro-D-Hyp-Gly-DAla-Gly-NH2 (ZP123): In Vivo and in Vitro Studies
Anne Louise Kj0lbye,
Carsten Boye Knudsen, Trine Jepsen,
Bjarne Due Larsen, and
J0rgen S0berg Petersen
1191
Functional and Binding Characterizations of Urotensin IIRelated Peptides in Human and Rat Urotensin II-Receptor
Assay
Alexandre Brkovic, Almut Hattenberger, Evi
Kostenis, Thomas Klabunde, Stefanie Flohr,
Michael Kurz, Steve Bourgault, and Alain
Fournier
1200
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
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
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
838
870
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
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
cDNA Microarray Analysis Reveals a Nuclear Factor-KBIndependent Regulation of Macrophage Function by
Adenosine
Zoltan H. Nemeth, S. Joseph Leibovich,
Edwin A. Deitch, E. Sylvester Vizi, Csaba
Szabd, and Gyorgy Hasko
1042
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
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
1182
Dopamine Modulation of Membrane Excitability in Striatal
Spiny Neurons is Altered in DARPP-32 Knockout Mice
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 OlHexadecyl-y-glutamyl-S-benzylcysteinyl-D-phenylglycine
Ethylester
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
889
846
861
INFLAMMATION AND IMMUNOPHARMACOLOGY
A Small Molecule ct4fotlfx4$7 Antagonist Differentiates
between the Low-Affinity States of a^ and a 4f5 7:
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 AntigenInduced 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, WenCherng Lee, Mark A. Cornebise, and
Patricia A. Detmers
903
1077
1086
1174
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
NEUROPHARMACOLOGY
Sympathetic Innervation in the 1 -Methyl -4-phenyl-l,2,3,6tetrahydropyridine Primate Model of Parkinson's Disease
David S. Goldstein, Sheng-Ting Li,
Courtney Holmes, and Krys Bankiewicz
855
Differential Regulation of the Endocannabinoids Anandamidc
and 2-Arachidonylglycerol within the Limbic Forebrain by
Dopamine Receptor Activity
Sachin Patel, David J. Rademacher, and
Cecilia J. Hillard
880
Differential Actions of Fipronil and Dieldrin Insecticides on
GABA-Gated Chloride Channels in Cockroach Neurons
Xilong Zhao, Vincent L. Salgado,
Jay Z. Yeh, and Toshio Narahashi
914
Steroids Modulate /V-Methyl-D-aspartate-stimulated
[3H]Dopamine Release from Rat Striatum via or Receptors
Samer J. Nuwayhid and Linda L. Werling
934
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
M. J. Millan, A. Gobert, F. Lejeune, A.
Dekeyne, A. Newman-Tancredi, V. Pasteau,
J.-M. Rivet, and D. Cussac
954
jx-Opioid-Induced Desensitization of Opioid Receptor-Like 1
and fi-Opioid Receptors: Differential Intracellular Signaling *
Determines Receptor Sensitivity
Chitra D. Mandyam, Deepak R. Thakker,
and Kelly M. Standifer
965
L-Setegiline Potentiates the Cellular Poly(ADP-Ribosyl)ation
Response to Ionizing Radiation
Christine Brabeck, Ragen Pfeiffer,
Alan Leake, Sascha Beneke, Ralph Meyer,
and Alexander Biirkle
973
The Endogenous Cannabinoid Anandamide Inhibits a?
Nicotinic Acetylcholine Receptor-Mediated Responses in
Xenopus Oocytes
Murat Oz, Arippa Ravindran,
Oscar Diaz-Ruiz, Li Zhang, and
Marisela Morales
1003
/V-H-Alkylpyridinium Analogs, a Novel Class of Nicotinic
Receptor Antagonists: Selective Inhibition of Nicotine-Evoked
[3H]Dopamine Overflow from Superfused Rat Striatal Slices
Vladimir P. Grinevich, Peter A. Crooks,
Sangeetha P. Sumilhran, Aaron J. Haubner,
Joshua T. Ayers, and Linda P. Dwoskin
1011
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-4isoxazole Propionate (AMPA)/Kainate Glutamate Receptors
Regulate the Deficit in Brain Reward Function Associated
with Nicotine Withdrawal in Rats
J. E. Gibbs, T. Rashid, and S. A. Thomas
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
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
ATP Augments Peptide Release from Rat Sensory Neurons in
Culture through Activation of P2Y Receptors
H. Huang, X. Wu, G. D. Nicol, S. Meller,
and M. R. Vasko
Long-Term Effects of Olanzapine, Risperidone, and
Quetiapine on Ionotropic Glutamate Receptor Types:
Implications for Antipsychotic Drug Treatment
Frank I. Tarazi, Ross J. Baldessarini,
Nora S. Kula, and Kehong Zhang
TOXICOLOGY
Rat Hepatic CYP2E1 Is Induced by Very Low Nicotine Doses:
An Investigation of Induction, Time Course, Dose Response,
and Mechanism
Alina L. Micu, Sharon Miksys,
Edward M. Sellers, Dennis R. Koop, and
Rachel F. Tyndale
1145
941
Role of Cysteine S-Conjugate 0-Lyase in the Metabolism of
Cisplatin
Lei Zhang and Marie H. Hanigan
988
Comparative Effects of Methylmercury and Hg 2+ on Human
Neuronal N- and R-Type High-Voltage Activated Calcium
Channels Transiently Expressed in Human Embryonic Kidney
293 Cells
Ravindra K. Hajela, Shuang-Qing Peng, and
William D. Atchison
1129