Pharmacology March1992 and Experimental Therapeutics

The Journalof

VOLUME26O PHARMACOLOGY MARCH1992 AND EXPERIMENTAL THERAPEUTICS

Contents

ANTI-INFLAMMATORIES Correlation of Anti-Inflammatory Activity with Peak Tissue Alison M. Bendele, 1194 Rather Than Peak Plasma Levels of BF389 Kenneth J. Ruterbories, Stephen M. Spaethe, Don N. Benslay, Terry D. Lindstrom, Sung J. Lee and Robert W. Naismith

ANALGESICS Downloaded from Increased Urinary Morphine, Codeine and K. Matsubara, S. Fukushima, A. Akane, 974 Tetrahydropapaveroline in Parkinsonian Patient Undergoing S. Kobayashi and H. Shiono L-3,4-Dihydroxyphenylalafline Therapy: A Possible Biosynthetic Pathway of Morphine from L-3,4- Dihydroxyphenylalanine in Humans Cholecystokinin Administered Intrathecally Selectively Leon F. Tseng and Keith A. Collins 1086 jpet.aspetjournals.org Antagonizes Intracerebroventricular t9-Endorphin-Induced Tail-Flick Inhibition in the Mouse Extremely Long-Lasting Antagonistic Actions of Nor- Peter Horan, Jill Taylor, 1237 Binaltorphimine (nor-BNI) in the Mouse Tail-Flick Test Henry I. Yamamura and Frank Porreca

AUTONOMIC PHARMACOLOGY

Central 5-Hydroxytryptamine2 Receptors Are Involved in the Francis Chaouloff, Sue H. Gunn and 1008 at ASPET Journals on September 26, 2021 Adrenal Catecholamine-Releasing and Hyperglycemic Effects James B. Young of the 5-Hydroxytryptamine Indirect Agonist d-Fenfluramine in the Conscious Rat Pharmacological Properties of Potassium Currents in Swine Hsiu-Ming H. Saunders and 1038 Tracheal Smooth Muscle Jerry M. Farley Pharmacological Evaluation of JO 1870: Relation to the C. Soulard, X. Pascaud, F. J. Roman, 1152 Potential Treatment of Urinary Bladder Incontinence A. Grouhel and J. L. Junien Evidence for Postjunctional Release of ATP Evoked by Takeshi Katsuragi, Osamu Soejima, 1309 Stimulation of Muscarinic Receptors in Ileal Longitudinal Takeo Tokunaga and Tatsuo Furukawa Muscles of Guinea Pig

BEHAVIORAL PHARMACOLOGY Discriminative Stimulus Properties of the Serotonergic Caroline E. Ybema, Jef L. Slangen, 1045 Compound Eltoprazine Berend Olivier and Jan Mos The Effects of Chronic Buprenorphine Treatment on Cocaine Nancy K. Mello, Scott E. Lukas, 1185 and Food Self-Administration by Rhesus Monkeys Jonathan B. Kamien, Jack H. Mendelson, John Drieze and Edward J. Cone Zolpidem Behavioral Pharmacology in Baboons: Self- Roland R. Griffiths, 1199 Injection, Discrimination, Tolerance and Withdrawal Christine A. Sannerud, Nancy A. Ator and Joseph V. Brady

CARDIOVASCULAR PHARMACOLOGY Nitrovasodilators as a New Class of Ocular Hypotensive James A. Nathanson 956 Agents Evaluation of LY203647 on Cardiovascular Leukotriene 1)4 Richard A. Hahn, Brian R. MacDonald, 979 Receptors and Myocardial Reperfusion Injury Emily Morgan, Brian D. Potts, C. John Parli, Lynn E. Rinkema, Celia A. Whitesitt and Winston S. Marshall

Contents continued on iv Contents continued from iii

The Relationship Between the Vitamin K Cycle Inhibition and J. J. Mosterd and H. H. W. Thijssen 1081 the Plasma Anticoagulant Response at Steady-State S- Warfarin Conditions in the Rat Vasopressin Modulates Cerebrovascular Responses to W. M. Armstead, R. Mirro, 1107 Opioids in Newborn Pigs S. L. Zuckerman and C. W. Leffler Amplification of Alpha Adrenergic Vasoconstriction in Canine H. Shimamoto, J.-P. Bourreau, 1119 Isolated Mesenteric Artery and Vein C. Y. Kwan and E. E. Daniel Effects of Diltiazem on Glycolysis and Oxidative Metabolism Gary D. Lopaschuk, Rick Barr and 1220 in the Ischemic and Isehemic/Reperfused Heart Richard Wambolt Mechanisms of the Cardioprotective Actions of WEB-2170, Xin-Liang Ma, Andrew S. Weyrich, 1229 bepafant, a Platelet Activating Factor Antagonist, in Stanley Krantz and Allan M. Lefer Myocardial Ischemia and Reperfusion Coronary Vascular Injury Due to Ischemia-Reperfusion Is Ira M. Dauber, Edward J. Lesnefsky, 1250 Roger C. Ashmore, Douglas M. Martel, Reduced by Pentoxifylline Frank M. Sheridan, John V. Weil and Lawrence D. Horwitz

Dipeptidyl(amino)peptidase IV and Aminopeptidase M Downloaded from Saleem Ahmad, Linhong Wang and 1257 Metabolize Circulating Substance P in Vivo Patrick E. Ward Cardiorespiratory Effects of the Novel Opioid Analgesic HP John W. Hubbard, Kenneth W. Locke, 1268 Hubert V. Forster, Alan G. Brice, 736 in the Anesthetized Dog and Conscious Goat Larry G. Pan, Tim F. Lowry, Anne- Mette L. Forster, Matthew A. Forster,

Michael Cornfeldt, Chen L. Vanselous, jpet.aspetjournals.org R. Richard L. Hamer, Edward J. Glamkowski and Stuart Fielding Evaluation of N-0861, (±)-N’-Endonorbornan-2-yl-9- John C. Shryock, 1292 methyladenine, as an A1 Subtype-Selective Adenosine Holly Coleman Travagii and Receptor Antagonist in the Guinea Pig Isolated Heart Luiz Belardinelli

Cardiac Responses and Binding Sites for Endothelin in Gordon T. Bolger, Robert Berry, 1314 at ASPET Journals on September 26, 2021 Francine Liard, Michel Garneau and Normal and Cardiomyopathic Hamsters Jorge Jaramillo Stimulant Effects of Muscarinic Agonists in Embryonic Chick Kanigula Mubagwa, Ana-Maria Vites 1323 Ventricular Muscle. Are the Effects Mediated by Protein and Achilles J. Pappano Kinase C? Inhibition by Amiloride and Quinacrine of Specific 13H1 Mimi Stokke, Else Marie Hagein, 1366 Nitrendipine Binding to Rat Cardiac Membranes Claire Poulsson, Renuka Patel, Yemane Haile and Odd Br#{248}rs Binding of f’25IJAtrial Natriuretic Factor to Mouse Lung A. Souque, C. Gros and J. C. Schwartz 1373 Membranes in Vivo: Characterization and Effects of Peptidase Inhibitors The Antiproteinuric Action of Enalapril in Stroke-Prone Charles T. Stier, Jr., Keyvan Mahboubi, 1410 Spontaneously Hypertensive Rats is Unrelated to Alterations Vincent A. DiPippo, Seymour Levine in Urinary Prostaglandins and Praveen N. Chander

CELLULAR AND MOLECULAR PHARMACOLOGY Bay K-8644 in Different Solvents Acts as a T Channel Lingyun Wu, Rui Wang, 966 Antagonist and an L Channel Agonist Edward Karpinski and Peter K. T. Pang Mechanism of Inhibitory Effects of Azelastine on Smooth Masatoshi Masuo, Tadahito Shimada 1300 Muscle Contraction and Toshio Kitazawa

CHEMOTHERAPY Direct Measurement of Melphalan Conjugation with Thomas M. Guenthner, Robert Whalen 1331 Glutathione: Studies with Human Melanoma Cells and and Vesna Jevtovi#{234}-Todorovi#{233} Mammalian Liver

DRUG METABOLISM AND DISPOSITION Enzymatic Basis for the Transesterificatlon of Cocaine in the C. Scott Boyer and Dennis R. Petersen 939 Presence of Ethanol: Evidence for the Participation of Microsomal Carboxylesterases

Contents continued on v Contents continued from iv

Predictability of the in Vivo Metabolism of Verapamil from Heyo K. Kroemer, Hirotoshi Echizen, 1052 in Vitro Data: Contribution of Individual Metabolic Pathways Hugo Heidemann and and Stereoselective Aspects Michel Eichelbaum A New Approach to the Study of Ifosfamide Metabolism by Robert Martino, Fran#{231}oisCrasnier, 1133 the Analysis of Human Body Fluids with 31P Nuclear Nadia Chouini-Lalanne, Magnetic Resonance Spectroscopy V#{233}roniqueGilard, UlfNiemeyer, Marcel de Forni and Marie-C. Malet- Martino In Vitro N-Glucuronidation of a Novel Antiepileptic Drug, Jacques Magdalou, Regine Herber, 1166 Lamotrigine, by Human Liver Microsomes Roselyne Bidault and Gerard Siest Colchicine-Specific Fab Fragments Alter Colchicine Main E. Sabouraud, Michel Urtizberea, 1214 Disposition in Rabbits Nathalie J. Cano, Michel Grandgeorge, Jean-Marc Rouzioux and Jean- Michel G. Scherrmann Long-Term Diabetes Alters the Hepatobiliary Clearance of John B. Watkins III and 1337 Acetaminophen, Bilirubin and Digoxin Susan E. Sherman Chiral Inversion and Stereoselective Glutatbione Conjugation Martine Polhuijs, Alexander C. Tergau 1349 Downloaded from of the Four 2-Bromo-3-Methylvaleric Acid Stereoisomers in and Gerard J. Mulder the Rat in Vivo and in Vitro The Antipsychotic Clozapine is Metabolized by the V. Fischer, B. Vogels, G. Maurer and 1355 Polymorphic Human Microsomal and Recombinant R. E. Tynes Cytochrome P450 2D6 Selective Inhibition of Rat Hepatic Microsomal Cytochrome T. Chang, M. Levine, S. M. Bandiera 1441 jpet.aspetjournals.org P-450. I. Effect of the in Vivo Administration of Cimetidine and G. D. Bellward Selective Inhibition of Rat Hepatic Microsomal Cytochrome T. Chang, M. Levine and G. D. Bellward 1450 P-450. II. Effect of the in Vitro Administration of Cimetidine

ENDOCRINE PHARMACOLOGY The Role of the Fourth Cerebroventricle in Nicotine- Shannon G. Matta and Burt M. Sharp 1285 Stimulated Prolactin Release in the Rat: Involvement of Catecholamines at ASPET Journals on September 26, 2021 Effects of Repetitive Administration of Recombinant Human Norihiko Murakami, Junichi Fukata, 1344 Interleukin-lfl, an Analog or Corticotropin-Releasing Takeshi Usui, Yoshiyuki Naito, Hormone Combined with Lysine Vasopressin on Rats with Tomoko Tominaga, Yoshikatsu Nakai, Glucocorticoid-Induced Secondary Adrenocortical Yoshihiro Masui, Kemchiro Nakao and Insufficiency Hiroo Imura

GASTROINTESTINAL PHARMACOLOGY Effects of a Prostacydlin Analog, U-68,215, on Gastric Acid Terez Shea-Donohue, 1023 Secretion, Gastric Emptying and Systemic Blood Pressure in Ambukarasi Kandasamy and Primates Andre Dubois Gastrointestinal Motor Alterations Induced by Precipitated J. Martinez, M. J. Fargeas and L. Bueno 1067 Benzodiazepine Withdrawal in Rats Neurally Mediated Relaxation of Opossum Internal Anal Sushanta Chakder and Satish Rattan 1113 Sphincter: Influence of Superoxide Anion Generator and the Scavenger

IMMUNOPHARMACOLOGY Modulation of Human Basophil Histamine Release by Protein H#{227}kanBergstrand, Britta Lundquist, 1028 Kinase C Inhibitors Differs with Secretagogue and with Kostas Karabelas and Peter Michelsen Inhibitor The Effects of FK-506, a Novel and Potent Yuji Hiraoka, Chiharu Kishimoto, 1386 Immunosuppressant, upon Murine Coxsackievirus B3 Masahiko Kurokawa, Hiroshi Ochiai Myocarditis and Shigetake Sasayama

NEUROPHARMACOLOGY High-Affinity Dextromethorphan and (+)-3-(-3- Martine Klein and Jos#{233}M.Musacchio 990 Hydroxyphenyl)-N-(1-Propyl)Piperidine Binding Sites in Rat Brain. Allosteric Effects of Ropizine Characterization of Brain Imidazoline Receptors in Gabriel Olmos, Antonio Miralles, 1000 Normotensive and Hypertensive Rats: Differential Regulation Fernando Barturen and Jesus A. Garcia-

Contents continued on vi Contents continuedfrom v

by Chronic Imidazoline Drug Treatment Sevilla Beneficial Effects of Naftidrofuryl Oxalate on Brain Regional Keiko Miyake, Taku Taguchi, 1058 Energy Metabolism after Microsphere-Induced Cerebral Kouichi Tanonaka, Tomoko Horiguchi, Embolism Norio Takagi and Satoshi Takeo In Vitro and in Vivo Inhibition of N-Acetyl-L-Aspartyl-L- V. Serval, T. Galli, A. Cheramy, 1093 Glutamate Catabolism by N-Acylated L-Glutamate Analogs J. Glowinski and S. Lavielle a-Ammo-,-Hydroxy--Methylisoxazole-’.-Propionate/Kainate David L. Wiffins, Lane J. Wallace, 1145 Receptor Antagonists in the Nucleus Accumbens and Ventral Duane D. Miller and Norman J. Uretsky Pallidum Decrease the Hypermotiuity Response to Psychostimulant Drugs DAT-582, a Novel Serotonin3 Receptor Antagonist, Is a Naoyuki Yoshida, Hiroko Omoya and 1159 Potent and Long-Lasting Antiemetic Agent in the Ferret and Tsugutaka Ito Dog Effects of Ketamine on Sensory Perception: Evidence for a Ivar #{248}ye,Ole Paulsen and Atle Maurset 1209 Role of N-Methyl-D-Aspartate Receptors Low-Level N-Methyl-D-Aspartate Receptor Activation Constance G. Craig and 1278 Provides a Purinergic Inhibitory Threshold Against Further Thomas D. White Downloaded from N-Methyl-r-Aspartate-Mediated Neurotransmission in the Cortex Binding of Typical and Atypical Antipsychotic Agents to Bryan L. Roth, Roland D. Ciaranello 1361 Transiently Expressed 5-HTc Receptors and Herbert Y. Meltzer Tetraalkylammonium Ion Block of Potassium Currents in F. N. Quandt and W. B. Im 1379 jpet.aspetjournals.org Mouse Neuroblastoma Cells Dopaminergic Neurotoxicity of 1-Methyl-4-Phenylpyridimum Michael S. Saporito, 1400 Analogs in Cultured Neurons: Relationship to the Dopamine Richard E. Heikkila, Uptake System and Inhibition of Mitochondrial Respiration Stephen K. Youngster, William J. Nicklas and Herbert M. Geller Somatostatin Causes Vasoconstriction, Reduces Blood Flow Joseph B. Long, Donald 1). Rigamonti, 1425 and Increases Vascular Permeability in the Rat Central Kumi Dosaka, Joyce M. Kraimer and at ASPET Journals on September 26, 2021 Nervous System Alberto Martinez-Arizala CholecystokiinA and CholecystokininB Receptors in Neurons P. Branchereau, G. A. B#{246}hme, 1433 of the Brainstem Solitary Complex of the Rat: J. Champagnat, M.-P. Morin-Surun, Pharmacological Identification C. Durieux, J. C. Blanchard, B. P. Roques and M. Denavit-Saubi#{233}

PHARMACOLOGY OF SUBSTANCE ABUSE Comparison of the Effects of the Uncompetitive N-Methyl-i>. Kathleen A. Grant, Lawrence D. Snell, 1017 Aspartate Antagonist (±)-5-Aminocarbonyl-1O,1I-Dihydro- Michael A. Rogawski, Andrew Thurkauf 5H-Dibenzoa,dJCyclohepten-5,1O-Imine (ADCI) with Its and Boris Tabakoff Structural Analogs Dizocilpine (MK-8OI) and Carbamazepine on Ethanol Withdrawal Seizures Behavioral Effects of Novel Cocaine Analogs: A Comparison Elizabeth J. Clime, Ursula Scheffel, 1174 with in Vivo Receptor Binding Potency John W. Boja, F. Ivy Carroll, Jonathan L. Katz and Michael J. Kuhar Inhibition of Protein Phosphorylation by Opioid-Inhibited Lynne M. Fleming, Gabriel Ponjee and 1416 Adenylyl Cyclase in Rat Brain Membranes Steven R. Childers

PROSTAGLANDINS, LEUKOTRIENES, AND OTHER EICOSANOIDS Mechanism of Inositol 1,4,5-Trisphosphate-Induced Irma Knezevic, Jeanette P. Dieter and 947 Aggregation in Saponin-Permeabilized Platelets Guy C. Le Breton Prostaglandin E1-Induced Vasorelaxation in Porcine Coronary Satoru Fukuda, Mutsumi Morioka, 1128 Arteries Tsuyoshi Tanaka and Koki Shimoji Indirect Actions of Thapsigargin on Human Platelets: Kenneth C. Malcolm and 1244 Activation of Eicosanoid Biosynthesis and Cellular Signaling Frank A. Fitzpatrick Pathways

PULMONARY PHARMACOLOGY The Effect of Sensory Nerve Depletion on Cholinergic David Stretton, Maria G. Belvisi and 1073 Neurotransmission in Guinea Pig Airways Peter J. Barnes

Contents continued on vii Contents continuedfrom vi

Characterization of the Contractile Serotonergic Receptor in Stephanie W. Watts and 1 101 Guinea Pig Trachea with Agonists and Antagonists Marlene L. Cohen Functional Innervation of Pig Tracheal Smooth Muscle: M. S. Kannan and D. E. Johnson 1180 Neural and Nonneural Mechanisms of Relaxation

RENAL PHARMACOLOGY Characterization of Renal Angiotensin II Receptors Using Richard M. Edwards, Elwood J. Stack, 933 Subtype Selective Antagonists Edwin F. Weidley, Nambi Aiyar, Richard M. Keenan, David T. Hill and Joseph Weinstock Role of Endothelium-Derived Relaxing Factor in the in Vivo Michiaki Okumura, Katsuyuki Miura, 1262 Renal Vascular Action of Adenosine in Dogs Yutaka Yamashita, Tokihito Yukimura and Kenjiro Yamamoto

TOXICOLOGY Reversal of Desipramine Toxicity in Rats Using Drug-Specific Gregory J. Brunn, Daniel E. Keyler, 1392 Antibody Fab’ Fragment: Effects on Hypotension and Susan M. Pond and Paul R. Pentel

Interaction with Sodium Bicarbonate Downloaded from

ERRATUM 1456

Index, Volume 260, January-March, 1992 1457 jpet.aspetjournals.org at ASPET Journals on September 26, 2021