The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
June 2005
Vol. 313, No. 3
Contents
PERSPECTIVES IN PHARMACOLOGY
The Evolution of in Vitro Fertilization: Integration of
Pharmacology, Technology, and Clinical Care
Eve C. Feinberg, Jason G. Bromer, and
William H. Catherino
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Hydrolysis of Capecitabine to 5'-Deoxy-5-fluorocytidine by
S. K. Quinney, S. P. Sanghani, W. I. Davis,
Human Carboxylesterases and Inhibition by Loperamide
T. D. Hurley, Z. Sun, D. J. Murry, and
W. F. Bosron
935
1011
Modulation of Metoprolol Pharmacokinetics and
Hemodynamics by Diphenhydramine Coadministration during
Exercise Testing in Healthy Premenopausal Women
Ashish Sharma, Philippe Pibarot, Sylvie
Pilote, Jean G. Dumesnil, Marie Arsenault,
Pierre Maxime Belanger, Bernd Meibohm,
and Bettina A. Hamelin
1172
Renal Clearance of y-Hydroxybutyric Acid in Rats:
Increasing Renal Elimination as a Detoxification Strategy
Marilyn E. Morris, Ke Hu, and Qi Wang
1194
Relative Bioavailability of Calcium from Calcium Formate,
Calcium Citrate, and Calcium Carbonate
Robert P. Hanzlik, Stephen C. Fowler, and
Daniel H. Fisher
1217
Use of a Physiologically Based Pharmacokinetic Model to
Study the Time to Reach Brain Equilibrium: An
Experimental Analysis of the Role of Blood-Brain Barrier
Permeability, Plasma Protein Binding, and Brain Tissue
Binding
Xingrong Liu, Bill J. Smith, Cuiping Chen,
Ernesto Callegari, Stacey L. Becker,
Xi Chen, Julie Cianfrogna, Angela C. Doran,
Shawn D. Doran, John P. Gibbs,
Natilie Hosea, Jianhua Liu,
Frederick R. Nelson, Mark A. Szewc, and
Jeffery Van Deusen
1254
UDP Glucuronosyltransferase (UGT) 1A6 Pharmacogenetics:
I. Identification of Polymorphisms in the 5'-Regulatory and
Extm 1 Regions, and Association with Human Liver UGT1A6
Gene Expression and Glucuronidation
Soundararajan Krishnaswaray, Qin Hao,
Abdul Al-Rohaimi, Leah M. Hesse, Lisa L.
von Moltke, David J. Greenblatt, and
Michael H. Court
1331
UDP Glucuronosyltransferase (UGT) 1A6 Pharmacogenetics:
II. Functional Impact of the Three Most Common
Nonsynonymous UGT1A6 Polymorphisms (S7A, T181A, and
R184S)
Soundararajan Krishnaswamy, Qin Hao,
Abdul Al-Rohaimi, Leah M. Hesse, Lisa L.
von Moltke, David J. Greenblatt, and
Michael H. Court
1340
BEHAVIORAL PHARMACOLOGY
Contribution of GABAA Receptor Subtypes to the AnxiolyticLike, Motor, and Discriminative Stimulus Effects of
Benzodiazepines: Studies with the Functionally Selective
Ligand SL651498 [6-Fluoro-9-methyl-2-phenyl-4-(pyrrolidin-lyl-carbonyl)-2,9-dihydro-li/-pyridol[3,4-&]indol-l-one]
Stephanie C. Licata, Donna M. Platt, James
M. Cook, P. V. V. Srirama Sarma, Guy
Griebel, and James K. Rowlett
1118
In Vivo Characterization of 6/3-Naltrexol, an Opioid Ligand
with Less Inverse Agonist Activity Compared with Naltrexone
and Naloxone in Opioid-Dependent Mice
Kirsten M. Raehal, John J. Lowery,
Castigliano M. Bhamidipati, Ryan M.
Paolino, Jennifer R. Blair, Danxin
Wang, Wolfgang Sade"e, and Edward J.
Bilsky
Su-Min Li, Amy Hauck Newman, and
Jonathan L. Katz
1150
Lawrence P. Carter, Huifang Wu, Weibin
Chen, Marilyn M. Matthews, Ashok K.
Mehta, R. Jason Hernandez, Jennifer A.
Thomson, Maharaj K. Ticku, Andrew
Coop. Wouter Koek, and Charles P.
France
1314
1017
Af^V,Arrr?V'-Tetrakis(2-pyridylmethyl)-ethylenediamine
Improves Myocardial Protection against Ischemia by
Modulation of Intracellular Ca 2+ Homeostasis
Soghra Fatima, Fariborz A. Yaghini,
Zoran Pavicevic, Shailaja Kalyankrishna,
Nauzanene Jafari, Elizabeth Luong, Anne
Estes, and Kafait U. Malik
Yelena A. Shmist, Roman Kamburg, Gal
Ophir, Alex Kozak, Vladimir Shneyvays,
Yori J. Appelbaum, and Asher Shainberg
The Acute Estrogenic Dilation of Rat Aorta Is Mediated
Solely by Selective Estrogen Receptor-t* Agonists and Is
Abolished by Estrogen Deprivation
Chiara Bolego, Andrea Cignarella,
Paola Sanvito, Valeria Pelosi, Fabio
Pellegatta, Lina Puglisi, and
Christian Pinna
Place Conditioning and Locomotor Effects of N-Substituted,
4',4"-Difluorobenztropine Analogs in Rats
Novel y-Hydroxybutyric Acid (GHB) Analogs Share Some,
but Not All, of the Behavioral Effects of GHB and GABAB
Receptor Agonists
ARDIOVASCULAR
d] Intact Actin Filaments Are Required for Cytosolic
Phospholipase A2 Translocation but Not for Its Activation by
Norepinephrine in Vascular Smooth Muscle Cells
Opposing Roles of Endothelial and Smooth Muscle
Phosphatidylinositol 3-Kinase in Vasoconstriction: Effects of
Rho-Kinase and Hypertension
Klaudia Budzyn, Philip D. Marley, and
Christopher G. Sobey
Differential Agonist-Mediated Internalization of the Human 5Hydroxytryptamine 7 Receptor Isoforms
Kl Insulin Receptor-Protein Kinase C-y Signaling Mediates
Inhibition of Hypoxia-Induced Necrosis of Cortical Neurons
Angiotensin II Attenuates Synaptic GABA Release and Excites
Paraventricular-Rostral Ventrolateral Medulla Output
Neurons
Site of Action of /3-Ligands at the Human 01-Adrenoceptor
Functional Selectivity of Melanocortin 4 Receptor Peptide and
Nonpeptide Agonists: Evidence for Ligand-Specific
Conformational States
Neurokinin-1 Receptor Resensitization Precedes Receptor
Recycling
Desensitization of the Human Motilin Receptor by Motilides
Inhibition of Gene Markers of Fibrosis with a Novel Inhibitor
of Transforming Growth Factor-/^ Type I Receptor Kinase in
Puromycin-Induced Nephritis
1203
1248
1289
A. Banan, L. J. Zhang, M. Shaikh,
J. Z. Fields, S. Choudhary, C. B. Forsyth,
A. Farhadi, and A. Keshavarzian
Chris R. Guthrie, Aaron T. Murray, Allyn
A. Franklin, and Mark W. Hamblin
Wakako Hamabe, Ryousuke Fujita, and
Hiroshi Ueda
962
1003
1027
De-Pei Li and Hui-Lin Pan
1035
Jillian G. Baker
Sarah A. Nickolls, Beth Fleck, Sam
R. J. Hoare, and Rich A. Maki
V. J. Bennett, S. A. Perrine, and
M. A. Simmons
Leen Thielemans, Inge Depoortere, Jason
Perret, Patrick Robberecht, Yaoquan Liu,
Theo Thijs, Chris Carreras, Emmanuel
Burgeon, and Theo L. Peeters
T. Z. Su, M. R. Feng, and M. L. Weber
Mediation of Highly Concentrative Uptake of Pregabalin by LType Amino Acid Transport in Chinese Hamster Ovary
and Caco-2 Cells
;ASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
1046
Adebayo O. Oyekan
Differential Effects of 20-Hydroxyeicosatetraenoic Acid on
Intrarenal Blood Flow in the Rat
ELLULAR AND MOLECULAR
9 Isoform of Protein Kinase C Alters Barrier Function in
Intestinal Epithelium through Modulation of Distinct Claudin
Isotypes: A Novel Mechanism for Regulation of Permeability
1223
1163
1281
1347
1397
1406
Eugene T. Grygielko, William M. Martin,
Christopher Tweed, Peter Thornton, John
Harling, David P. Brooks, and Nicholas
J. Laping
943
Long-Term Treatment of Bile Duct-Ligated Rats with
Rapamycin (Sirolimus) Significantly Attenuates Liver
Fibrosis: Analysis of the Underlying Mechanisms
Erwin Biecker, Andrea De Gotlardi,
Markus Neef, Matthias Unternahrer,
Vreni Schneider, Monika Ledermann,
Hans Sagesser, Sidney Shaw, and Jurg
Reichen
952
Cholinergic Stimulation of Amylase Secretion from Pancreatic
Acinar Cells Studied with Muscarinic Acetylcholine Receptor
Mutant Mice
Dinesh Gautam, Sung-Jun Han,
Thomas S. Heard, Yinghong Cui,
Georgina Miller, Lanh Bloodworth, and
Jurgen Wess
995
Demonstration of a Specific Site of Covalent Labeling of the
Human Motilin Receptor Using a Biologically Active
Photolabile Motilin Analog
Bunzo Matsuura, Maoqing Dong,
Bernard Coulie, Delia I, Pinon, and
Laurence J. Miller
C. Jane Dixon, Pamela J. White,
John F. Hali, Shaun Kingston, and
Michael R. Boarder
1101
Stephen B. Phagoo, Krisanavane Reddi,
Bertrand J. Silvallana,
L. M. Fredrik Leeb-Lundberg, and
David Warburton
1231
Pharmacological Characterization of CXC Chcraokine
Receptor 3 Ligands and a Small Molecule Antagonist
Christopher E. Heise, Anil Pahuja,
Sarah C. Hudson, Monica S. Mistry,
Amy L. Putnam, Molly M. Gross,
Peter A. Gottlieb, Warren S. Wade,
Mehrak Kiankarimi, David Schwarz,
Paul Crowe, Albert Zlotnik, and
David G. Alleva
1263
Potentiation of des-Argy-Kallidin-Induced Vasoconstrictor
Responses by Metallopeptidase Inhibition in Isolated Human
Umbilical Artery
A Novel Effect for Annexin 1-Derived Peptide Ac2-26:
Reduction of Allergic Inflammation in the Rat
Facundo German Pelorosso,
Paula Tamara Brodsky, Camila Lidia Zold,
and Rodolfo Pedro Rothlin
Christianne Bandeira-Melo,
Andre Gustavo C. Bonavita, Bruno L. Diaz,
Patricia M. R. e Silva, Vinfcius F. Carvalho,
Peter J. Jose, Roderick J. Flower, Mauro
Perrelli, and Marco A. Martins
1355
Gregory M. Miller, Christopher D. Verrico,
Amy Jassen, Martha Konar, Hong Yang,
Helen Panas, Mary Bahn, Ryan Johnson, and
Bertha K. Madras
Leo Kinarsky, Bihua Feng,
Donald A. Skifter, Richard M. Morley,
Simon Sherman, David E. Jane, and
Daniel T. Monaghan
983
Regulation of Human Hepatocytes by P2Y Receptors: Control
of Glycogen Phosphorylase, Ca 2+, and Mitogen-Activated
Protein Kinases
INFLAMMATION AND IMMUNOPHARMACOLOGY
Infection-Induced Kinin Bj Receptors in Human Pulmonary
Fibroblasts: Role of Intact Pathogens and p38 MitogenActivated Protein Kinase-Dependent Signaling
NEUROPHARMACOLOGY
Primate Trace Amine Receptor 1 Modulation by the
Dopamine Transporter
Identification of Subunit- and Antagonist-Specific Amino Acid
Residues in the iV-Methyl-D-aspartate Receptor GlutamateBinding Pocket
1305
1416
1066
Delivery of /3-Galactosidase to Mouse Brain via the BloodBrain Barrier Transferrin Receptor
Yun Zhang and William M. Pardridge
1075
Subcellular Alterations of Protein Kinase C Isozymes in the
Rat Brain after Organophosphate Poisoning
Eugenia Bloch-Shildennan, Tamar Kadar,
Aharon Levy, Rita Sahar, Ishai Rabinovitz,
and Eran Gilat
1082
Stilbazulenyl Nitrone, a Second-Generation Azulenyl Nitrone
Antioxidant, Confers Enduring Neuroprotection in
Experimental Focal Cerebral Ischemia in the Rat:
Neurobehavior, Histopathology, and Pharmacokinetics
James J. Ley, Alexey Vigdorchik,
Ludmila Belayev, Weizhao Zhao,
Raul Busto, Larissa Khoutorova,
David A. Becker, and Myron D. Ginsberg
1090
Endothelin (ET)-l-Induced Inhibition of ATP Release from
PC-12 Cells Is Mediated by the ETB Receptor: Differential
Response to ET-1 on ATP, Neuropeptide Y, and Dopamine
Levels
Effects of Chronic Infusion of a GABA A Receptor Agonist or
Antagonist into the Vestibular Nuclear Complex on Vestibular
Compensation in the Guinea Pig
Pharmacokinetic-Pharmacodynamic Modeling of the
Antinociceptive Effect of Buprenorphine and Fentanyl in
Rats: Role of Receptor Equilibration Kinetics
A. Gardner, T. C. Westfall, and
H. Macarthur
1109
Catherine M. Gliddon,
Cynthia L. Darlington, and Paul F. Smith
1126
Ashraf Yassen, Erik Olofsen, Albert Dahan,
and Meindert Danhof
1136
Cross-Sensitization to Morphine in Cocaine-Sensitized Rats:
Behavioral Assessments Correlate with Enhanced Responding
of Ventral Pallidal Neurons to Morphine and Glutamate, with
Diminished Effects of GABA
J. McDaid, J. E. Dallimore, A. R. Mackie,
A. L. Mickiewicz, and T. C. Napier
1182
Comparison of the Antinociceptive Profiles of Gabapentin and
3-Methylgabapentin in Rat Models of Acute and Persistent
Pain: Implications for Mechanism of Action
M. O. Urban, K. Ren, K. T. Park,
B. Campbell, N. Anker, B. Stearns, J. Aiyar,
M. Belley, C. Cohen, and L. Bristow
V. L. Tawfik, M. L. LaCroix-Fralish,
N. Nutile-McMenemy, and J. A. DeLeo
1209
Additive Effects of Endogenous Cannabinoid Anandamide and
Ethanol on «7-Nicotinic Acetylcholine Receptor-Mediated
Responses in Xenopus Oocytes
Group III Metabotropic Glutamate-Receptor-Mediated
Modulation of Excitatory Transmission in Rodent Substantia
Nigra Pars Compacta Dopamine Neurons
Murat Oz, Shelley N. Jackson,
Amina S. Woods, Marisela Morales, and Li
Zhang
Ornella Valenti, Guido Mannaioni,
Guy R. Seabrook, P. Jeffrey Conn, and
Michael J. Marino
1272
5-Hydroxytryptamine 1A Receptors in the Paraventricular
Nucleus of the Hypothalamus Mediate Oxytocin and
Adrenocorticotropin Hormone Release and Some Behavioral
Components of the Serotonin Syndrome
Patrick Osei-Owusu, Amy James,
James Crane, and Karie E. Scrogin
1324
Development of a Rationally Designed, Low Abuse Potential,
Biogenic Amine Releaser That Suppresses Cocaine SelfAdministration
Richard B. Rothman, Bruce E. Blough,
William L. Woolverton, Karen G. Anderson,
S. Stevens Negus, Nancy K. Mello, Bryan
L. Roth, and Michael H. Baumann
1361
Pharmacokinetic Analysis of the Blood-Brain Barrier
Transport of J25I-Amyloid {i Protein 40 in Wild-Type and
Alzheimer's Disease Transgenic Mice (APP,PS1) and Its
Implications for Amyloid Plaque Formation
Karunya K. Kandimalla, Geoffry L. Curran,
Silvina S. Holasek, Emily J. Grilles,
Thomas M. Wengenack, and
Joseph F. Poduslo
1370
Effects of the 7V-Methyl-D-aspartate Receptor Antagonist
Perzinfotel [EAA-090; [2-(8,9-Dioxo-2,6diazabicyclo[5.2.0]nonl(7)-en-2-yl)-ethyl]phosphonic Acid] on
Chemically Induced Thermal Hypersensitivity
Michael R. Brandt, Terri A. Cummons,
Lisa Potestio, Stacey J. Sukoff, and
Sharon Rosenzweig-Lipson
1379
o- Receptor Activation Blocks Potassium Channels and
Depresses Neuroexcitability in Rat Intracardiac Neurons
Hongling Zhang and Javier Cuevas
1387
Dean J. Naisbitt, John Farrell,
Peter J. Chamberlain, Josephine E. Hopkins,
Neil G. Berry, Munir Pirmohamed, and B.
Kevin Park
1058
Transcriptional and Translational Regulation of Glial
Activation by Morphine in a Rodent Model of Neuropathic
Pain
TOXICOLOGY
Characterization of the T-Cell Response in a Patient with
Phenindione Hypersensitivity
1239
1296