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VOLUME271 PHARMACOLOGY NUMBER 3 AND EXPERIMENTAL THERAPEUTICS

Contents

ANTI-INFLAMMATORIES Lecithinized Superoxide Dismutase Enhances Its R. Igarashi, J. Hoshino, A. Ochiai, 1672 Pharmacologic Potency by Increasing Its Cell Membrane Y. Morizawa and Y. Mizushima Affinity

ANALGESICS Role of Endogenous Cholecystokinin in the Facilitation of Mu- Florence Noble, Claire Smadja and 1127

Mediated Antinociception by Delta. Bernard P. Roques Downloaded from GBR12909 Attenuates -Induced Activation of Michael H. Baumann, George U. Char, 1216 Mesolimbic Dopamine Neurons in the Rat Brian R. Dc Costa, Kenner C. Rice and Richard B. Rothman Substance P N-Terminal Metabolites and Nitric Oxide Mediate Julie S. Kreeger, Kelley F. Kitto and 1281 Capsaicin-Induced Antinociception in the Adult Mouse Alice A. Larson

Antinociceptive Actions of Dexmedetomidine and the Kappa- Juhana J. Idanpaan-Heikkila, Eija A. Kalso 1306 jpet.aspetjournals.org Opioid U.5O,488H against Noxious Thermal, and Timo Seppala Mechanical and Inflammatory Stimuli Involvement of NMDA Receptors in -Induced Rustam Yu. Yukhananov and 1365 Contractions of the Isolated Guinea Pig ileum after Alice A. Larson Preincubation with

Development of Cross-Tolerance between - Fang Fan, David R. Compton, Susan Ward, 1383 , CP 55,940 and WIN 55,212 Lawrence Melvin and Billy R. Martin at ASPET Journals on October 2, 2021 Antinociceptive and Response Rate-Altering Effects of Kappa Raymond C. Pitts and Linda A. Dykstra 1501 Opioid Agonists, , and U69,593, Alone and in Combination with Opioid Antagonists in Squirrel Monkeys The Influence of Pharmacogenetics on Opioid Analgesia: Jim Cleary, Gerd Mikus, Andrew Somogyi 1528 Studies with and in the Sprague-Dawley/ and Felix Bochner Dark Agouti Rat Model Selective Antagonism of Opioid Analgesia by a Sigma System Chih-Cheng Chien and 1583 Gavril W. Pasternak Binding Affinity and Selectivity of at Mu, Delta and Paul J. Emmerson, Man-ru Liu, 1630 Kappa Receptors in Monkey Brain Membranes James H. Woods and Fedor Medzihradsky Increased Plasma Atrial Natriuretic Peptide after Acute Pascal Guillaume, Jolanta Gutkowska and 1656 Injection of Alcohol in Rats Christina Gianoulakis High Affinity Cocaine Recognition Sites on the Dopamine Julie K. Staley, W. Lee Hearn, 1678 Transporter are Elevated in Fatal Cocaine Overdose Victims A. James Ruttenber, C. V. Wetli and Deborah C. Mash Analysis of Delta- Activities Stably Expressed P. Y. Law, T. M. McGinn, M. J. Wick, 1686 in CHO Cell Lines: Function of Receptor Density? L. J. Erikson, C. Evans and H. H. Loh

AUTONOMIC PHARMACOLOGY Characterization of Alpha-i Adrenoceptor Subtypes in Human Aaron S. Goetz, Michael W. Lutz, 1228 and Canine Prostate Membranes Thomas J. Rimele and David L. Saussy, Jr. MEN 10,627, a Novel Polycydic Peptide Antagonist of Carlo Alberto Maggi, Mara Astolfi, 1489 Tachykinin NK2 Receptors Sandro Giuliani, Cristina Goso, Stefano Manzini, Stefania Meini, Riccardo Patacchini, Vincenzo Pavone, Carlo Pedone, Laura Quartara, Anna Rita Renzetti and Antonio Giachetti

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IDIIIIIUIIUIIIIN1 IIUUDINon:enu continued on ii J28R-SHB-6UQ9 Contents continuedfro.n i

Stimulatory Pathways and Sites of Action of Intrathecally Imran M. Khan, Palmer Taylor and 1550 Administered Nicotinic Agents Tony L Yaksh Muscarinlc Receptors Involved in Modulation of Miguel A. Casado, M. Angeles Sevifia, 1638 Norepinephrine Release and Vasodilatation in Guinea Pig M. Jesus Alonso, Jesus Mann and Carotid Arteries Mercedes Salaices

BEHAVIORAL PHARMACOLOGY Relative Sensitivity to Naloxone of Multiple Indices of Gery Schulteis, Athina Markou, 1391 Withdrawal: A Quantitative Dose-Response Analysis Lisa H. Gold, Luis Stinus and George F. Koob Oligodeoxynudeotide Antisense to the D1 Dopamine Receptor Sui-Po Thang, Long-Wu Thou and 1462 mRNA Inhibits D1 Dopamine Receptor-Mediated Behaviors in Benjamin Weiss Normal Mice and in Mice Lesioned with 6-Hydroxydopamine

CARDIOVASCULAR PHARMACOLOGY Chronic Nicotine Administration Does Not Affect Peripheral Then Li, Victor Barrios, John N. Buchholz, 1135 Vascular Reactivity in the Rat Thomas C. Glenn and Sue Piper Duckles Downloaded from Cyclic GMP Potentiation by WIN 58237, a Novel Cyclic Paul J. Silver, Ronald L. Dundore, 1143 Nucleotide Phosphodlesterase Inhibitor Donald C. Bode, Lawrence de Garavilla, R. Allan Buchholz, Glenn Van Ailer, Linda T. Hamel, Edward Bacon, Baldev Singli, George Y. Lasher, Dennis Hiasta and Edward D. Pagani

Acute Effects of Ethanol on Cardiac Output and Its Abdel A. Abdel-Rabman 1150 jpet.aspetjournals.org Derivatives in Spontaneously Hypertensive and Normotensive Rats Unmasking of Activated Histamine H3-Receptors in Michiaki Imamura, Enzo Poli, 1259 Myocardlal Ischemia: Their Role as Regulators of Exocytotic Abimbola T. Omoniyi and Roberto Levi Noreplnephrine Release The Cardiac Effects of a Novel A1-Adenosine Receptor Agonist Luiz Belardinelli, Jiyuan Lu, Dunn Dennis, 1371 In Guinea Pig Isolated Heart Jeffrey Martens and John C. Shryock at ASPET Journals on October 2, 2021 Effects of Felodipine on Left Ventricular Systolic and Diastolic Che-Ping Cheng, Knut Pettersson and 1409 Performance in Congestive Heart Failure William C. Utile Characterization of PD 121981- and CGP 42112-Induced Ki Whan Hong, Byung Yong Rhixn, 1591 Unmasking of Low Concentration Effects of Anglotensin II in Yung Woo Shin and Sung-Eun Yoo Rabbit Abdominal Aorta

-.. Furosemide Enhances the Release of Endothelial Kinins, Nitric Gabriele Wiemer, Edwin Fink, 1611 Oxide and Prostacydlin Wolfgang Linz, Max Hropot, Bernward A. Sch#{246}lkensand Paulus Wohlfart A Possible Mechanism of Action of a New Potassium Channel Sumio Matzno, Maid Gohda, 1666 Opener, AL0671, on Lipid Metabolism In Obese Zucker Rats Masahiro Eda, Hajime Ebisu, Shusei Uno, Naomichi Ishida, Norifumi Nakamura and Kouichi Yamanouchi

CELLULAR AND MOLECULAR PHARMACOLOGY Isoflurane Reduces Ca4 Channel Current and Accelerates Dixon W. Wilde 1159 Current Decay in Guinea Pig Portal Vein Smooth Muscle Cells Electrophyslological and Radloligand Binding Studies of Nathalie Lepretre, Serge Arnaudeau, 1209 Elgodipine and Derivatives In Portal Vein Myocytes Jean Mironneau, Lala Rakotoarisoa, Chantal Mironneau and Alvaro Galiano Inhibition by Nickel of Endothelin-1-Induced Tension and Suraj S. Shetty and Dominick DelGrande 1223 Associated Ca Movements In Rabbit Aorta Influence of Cell Type upon the Desensitization of the Archana Chaudhry and 1253 fi3-Adrenerglc Receptor James G. Granneman Alaproclate Acts as a Potent, Reversible and Noncompetitive Anneli Wilkinson, Michael Courtney, 1314 Antagonist of the NMDA Receptor Coupled Ion Flow Anita Westhnd-Danielsson, Gerd Hailnemo and Karl E. 0. Akerman

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Effects of a New Class of Calcium Antagonists, 5R33557 Georges Romey and Michel Lazdunski 1348 (Fantofarone) and SR33805, on Neuronal Voltage-Activated Ca’ Channels Ca Mobifization Mediated by Endothelin ETA Receptor In Ken-Ichi Amano, Masatoshi Hori, 1359 Endothelium of Rabbit Aortic Valve Hiroshi Ozaki, Yuzuru Matsuda and Hideaki Karaki The Ca-Channel Blocker Ro 40-5967 Blocks Differently G. Mehrke, X. G. Zong, V. Flockerzi and 1483 T-Type and L-Type Ca Channels F. Hofinann The Novel A4,ha-2 Adrenergic Radloligand [3H]-MK912 is Staffan Uhl#{233}n,Amy C. Porter and 1558 Alpha- Selective among Human Alpha.2A, Alpha-2B and Richard R. Neubig Alpha.2C Adrenoceptors

Mechanisms of Up-Regulation of Dopamine D2 Receptors by Theresa M. Filtz, Wei Guan, 1574 Agornsts and Antagonists in Transfected HEK-293 Cells Roman P. Artymyshyn, Mary Pacheco, Christine Ford and Perry B. Molinoff Disruption of GABA-Dependent Chloride Flux by Cyclodlenes Anna Pom#{233}s,Eduard RodrIguez-Faire and 1616 and Hexachiorocyclohexanes In Primary Cultures of Cortical Cristina Suflol

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ChEMOTHERAPY Decreased Intracellular Compartmentalization of Doxorubicin Margaret S. Dordal, Marisa Jackson-Stone, 1286 In Cell Lines Expressing P.Glycoproteln Amy C. Ho, Jane N. Winter and Arthur J. Atkinson, Jr.

Enhancement by O6-Benzyl-N-Acetylguanosine Derivatives of Catherine Cussac, Maryse Rapp, 1353 jpet.aspetjournals.org Chioroethylnitrosourea Antitumor Action in Emmanuelle Mounetou, Chioroethylnitrosourea-Resistant Human Malignant Jean Claude Madelinont, Melanocytes Jean Claude Maurizis, Denise Godeneche, Jean Michel Dupuy, Jacques Sauzieres, Jean Paul Baudry and Annie Veyre

DEVELOPMENTAL PHARMACOLOGY

Antitumor Activity of a Medium-Chain Triglyceride Solution Shigeo Yanai, Hiroaki Okada, 1267 at ASPET Journals on October 2, 2021 of the Angiogenesis Inhibitor TNP-470 (AGM-1470) When Masafumi Misaki, Kazuhiro Saito, Administered Via the Hepatic Artery to Rats Bearing Walker Yuji Kuge, Yasuaki Ogawa and 256 Carcinosarcoma In the Liver Hajime Toguchi Neonatal HypoxIa: Early Neurotransmltter Responses and the Dimitri Krajnc, Trina A. Wemlinger, 1299 Consequences of Treatment with GM1 Ganglioside Norton H. Neff and Maria Hadjiconstantinou

Potentlation of 51A Receptor-Mediated Neuroendocrine George Battaglia and Theresa M. Cabrera 1453 Responses In Male but not Female Rat Progeny after Prenatal Cocaine: Evidence for Gender Differences

DRUG METABOLISM AND DISPOSITION Maternal and Fetal Brain and Plasma Levels of Cocaine and Susan E. Robinson, E. Karl Enters, 1234 Benzoylecgonlne After Acute or Chronic Maternal Intravenous George F. Jackson, Vernon M. Chinchilli, Administration of Cocaine Jennifer R. Maher, Kelly P. McDowell, Holly M. Allen and Hongzhi Guo Enhanced Permeabifity of Tetragastrln across the Rat Etsuo Yodoya, Kazuyo Uemura, 1509 Intestinal Membrane and Its Reduced Degradation by Takehiro Tenma, Takuya Fujita, Acylatlon with Various Fatty Acids Masahiro Murakami, Akira Yamamoto and Shozo Muranishi Nonlinear Pharmacokinetics of a Recombinant Human Takashi Kuwabara, Yuzuru Kato, 1535 Granulocyte Colony-Stimulating Factor Derivative Satoshi Kobayashi, Hiroshi Suzuki and (Nartograstim): Species Differences Among Rats, Monkeys and Yuichi Sugiyama Humans

ENDOCRINE PHARMACOLOGY Alkyiglycosides Enhance Systemic Absorption of Insulin Dennis J. Pillion, Joycelyn A. Atchison, 1274 Applied Topically to the Rat Eye Rong-Xiang Wang and Elias Meezan Antihypertensive Effects of Metformin In Fructose-Fed Subodh Verma, Sanjay Bhanot and 1334 Hyperlnsullnemlc, Hypertensive Rats John H. McNeill

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GASTROINTESTINAL PHARMACOLOGY Inhibition of Motilin-Induced Phase ifi Contractions by Osamu Yamamoto, Yugo Matsunaga, 1471 Pentagastrin in Heidenhain Pouch Dogs Yoshihiro Shiba, Norihiro Haga, Isamu Sano and Zen Itoh

,,- NItric Oxide Synthase Activity, Viabifity and Cyclic GMP B. L Tepperman, J. F. Brown, 1477 Levels in Rat Colonic Epithelial Cells: Effect of Endotoxin R. Korolkiewicz and B. J. R. Whittle Challenge

IMMUNOPHARMACOLOGY Suppression of Human Eoslnophil Respiratory Burst and Gordon Dent, Mark A. Giembycz, 1167 Cyclic AMP Hydrolysis by Inhibitors of Type IV Pat M. Evans, Klaus F. Rabe and Phosphodlesterase: Interaction with the Beta Adrenoceptor Peter J. Barnes Agonist Albuterol

NEUROPHARMACOLOGY Ethanol-Induced Depressions of Cerebellar Purkinje Neurons Anya M-Y. Un, Ronald K. Freund, 1175 Barry J. Hoffer and Michael R. Palmer Are Potentiated by 13.Adrenergic Mechanisms in Rat Brain Downloaded from Evidence That Systemically Administered Dopamine Michele L. Pucak and Anthony A. Grace 1181 Antagonists Activate Dopamine Neuron Firing Primarily by Blockade of Somatodendritic Autoreceptors Haloperldol-Induced Behavioral Supersensitivity Is Increased U. Schr#{246}der,H. Schr#{246}der,W. Augustin and 1193 by Monosialoganglioside Treatment In Rats Without Affecting B. A. Sabel

SpiroperidolBinding jpet.aspetjournals.org Blood-Brain Barrier Permeability and in Vivo Activity of Jiunn H. Un, 1.-Wu Chen and Tsu-Han Un 1197 Partial Agonists of Benzodiazepine Receptor: A Study of L- 663,581 and Its Metabolites In Rats Differential Receptor Reserve for 5-HT1A Receptor-Mediated Emanuel Meller and Karen Bohmaker 1246 Regulation of Plasma Neuroendocrine Hormones Young-Hee Lee, Karen Spuhler-Phillips, 1291 Effects of Prenatal Ethanol Exposure on N-Methyl-u- Aspartate-Medlated Calcium Entry into Dissociated Neurons Patrick K. Randall and Steven W. Leslie at ASPET Journals on October 2, 2021 Protection against -Induced Neurotoxicity to Karen T. Delle Donne and 1320 NeOstriatal Dopaminerglc Neurons by Adenosine Receptor Patricia K. Sonsalla Activation

In the Search for a Novel Class of Antipsychotic Drugs: Anders BjOrk, Erik Christensson, 1338 Predlinical Pharmacology of FG5803, a Agneta Albinsson, Bo Gustafsson, 1-Piperazinecarboxamide DerIvative Eva Pettersson, G#{246}ranPettersson, Jan Svartengren and Gunnar Andersson Electrophyslological Effects of SKF 38393 in Rats with Kai-Xing Huang and Judith R. Walters 1434 Reserpine Treatment and 6-Hydroxydopamine-Induced NIgrOStrIatal Lesions Reveal Two Types of Plasticity in Dl Dopamine Receptor Modulation of Basal Ganglia Output Structure-Activity Relationships for Cocaine Congeners in Maarten E. A. Reith and Lon L. Coffey 1444 Inhibiting Dopamine Uptake into Rat Brain Synaptic Vesicles and Bovine Chromaffin Granule Ghosts Precoupling of A4,ha-2B Adrenergic Receptors and G-Protelns An-Guo Shi and Richard C. Deth 1520 in Transfected PC-12 Cell Membranes: Influence of Pertussis Toxin and a Lysine-Directed Cross-linker Ethanol Inhibits Glutamatergic Neurotransmlssion in Nucleus Zhiguo Nie, Samuel G. Madamba and 1566 Accumbens Neurons by Multiple Mechanisms George Robert Siggins Autoregulatlon and Monoamine Interactions in the Ventral Nian-Hang Chen and Maarten E. A. Reith 1597 Tegmental Area In the Absence and Presence of Cocaine: A Microdialysis Study in Freely Moving Rats Effects of an Antlstroke Agent MCI-186 on Cerebral Toshiaki Watanabe and Mitsuo Egawa 1624 Arachidonate Cascade Evidence that ACTH Secretion Is Regulated by Serotonln2 Peter A. Rittenhouse, Erica A. Bakkum, 1647 (5-HT) Receptors Andrew D. Levy, Qian U, Molly Carnes and Louis D. Van de Kar

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Neuroanatomical Specificity and Dose Dependency in the lime Gary E. Duncan, Dana J. Knapp, 1699 Course of -Induced Beta Adrenergic Receptor Karley Y. Utile and George R. Breese Down-regulation In Rat Brain

PROSTAGLANDINS, LEUKOTRIENES AND OTHER EICOSANOIDS Tepoxalin: A Dual Cycbooxygenase/5-Llpoxygenase Inhibitor of Dennis C. Argentien, David M. Ritchie, 1399 Arachidonic Add Metabolism with Potent Anti-Inflammatory Michael P. Ferro, Thomas Kirchner, Activity and a Favorable Gastrointestinal Profile Michael P. Wachter, David W. Anderson, Marvin E. Rosenthale and Robert J. Capetola BIRM 270: A Novel Inhibitor of Arachidonate Release that P. R. Farina, A. G. Graham, A. F. Hoffman, 1418 Blocks Leukotriene B4 and Platelet-Activating Factor J. M. Watrous, P. Borgeat, M. Nadeau, Biosynthesis in Human Neutrophils G. Hansen, R. M. Dinallo, J. Adams, C. K. Miao, E. S. Lazer, T. P. Parks and C. A. Homon Reglo- and Stereoselective Epoxidatlon of Arachidonic Acid by Brian E. Daikh, Jerome M. Lasker, 1427 Human Cytocbromes P450 2C8 and 2C9 Judy L Raucy and Dennis R. Koop Downloaded from Stereochemical Analysis and Biological ACtIVIty of 3-Hydroxy- Pat Wheelan, Angelo Sam, 1514 Leukotriene B4: A Metabolite from Ethanol-Treated Rat Giancarlo Folco, Simonetta Nicosia, Hepatocytes J. R. Falck, Rama K. Bhatt and Robert C. Murphy Biochemical and Pharmacological Characterization of the Paola Patrignani, Maria R. Panara, 1705 Cydooxygenase ACtIVIty of Human Blood Prostaglandin Anita Greco, Ornella Fusco, Clara Natoli, Endoperoxide Synthases Stefano lacobelli, Francesco Cipollone, jpet.aspetjournals.org Antonina Ganci, Christophe Cr#{233}minon, Jacques Maclouf and Carlo Patrono

PULMONARY PHARMACOLOGY Alteration of G Protein Levels in Antigen-Challenged Guinea Joanna Y. Lee, Yoshiyuki Uchida, 1713 Pigs Tohru Sakarnoto, Aiko Hirata,

Shizuo Hasegawa and Fusao Hirata at ASPET Journals on October 2, 2021

RENAL PHARMACOLOGY Cyclic GMP But Not Cyclic AMP Prevents Renal Platelet Madhu S. Chintala, Vernon Bernardino and 1203 Accumulation After Ischemla-Reperfusion in Anesthetized Peter J. S. Chiu Rats Transport of Cefadroxil In Rat Kidney Brush-border Michaela Ries, Uwe Wenzel and 1327 Membranes Is MedIated by Two Electrogenic H’-Coupled Hannelore Daniel Systems

TOXICOLOGY Inhibition of Insulin Release by a Formamidine Pesticide Ter-Hsin Chen and Walter H. Hsu 1240 Amltraz and Its Metabolites in a Rat Beta-Cell Line: An Action MedIated by Aluha-2 Adrenoceptors, a GTP-Bindlng Protein and a Decrease in Cyclic AMP Effects of Fluoroquinolones on Cultured Articular Marie Thuong-Guyot, Olivier Domarle, 1544 Chondrocytes: Flow Cytometric Analysis of Free Radical Jean-Jacques Pocidalo and Gilles Hayem Production DNA as a CrItical Target in Toxic Cell Death: Enhancement Usa M. Kamendulis and 1695 of Dlmethylnltrosamlne Cytotoxidty by DNA Repair Inhibitors George B. Corcoran