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Drug Metabolismand DispositIon:the biological fate of chemicals
January/February 1989 Vol. 17, No. 1
CONTENTS
Effect of Tick-Borne Fever (Ehrilichia phagocytophila)and Trypanosomiasis ( Trypanosoma brucei 1066)on the Pharmacokinetics of Suiphadimidine andits Metabolites in Goats. H. VAN GOGH, A. D. J.WATSON, J. F. M. Nouws, J. NIEUWENHUIJS,
AND A. S. J. P. A. M. VAN MIERT
Selective Mechanism-Based Inactivation of the MajorPhenobarbital-Inducible P.450 Cytochrome fromRabbit Liver by Phenyclidine and its OxidationProduct, the Iminium Compound. YOICHI OsAWA
AND MINOR J. COON
Metabolism of Atrial Natriuretic Peptide: Extractionby Organs in the Rat. PHILIP A. KRIETER AND AN-
GELO J. TRAPANI
Activities of Cytosolic and Microsomal Drug Oxidasesof Rat Hepatocytes in Primary Culture. A. J.SHERRATT AND L. A. DAMANI
Selective Inactivation of Rat Liver Cytochromes P-450by 2 1-Chlorinated Steroids. JAMES HALPERT,
JOHN-YAN JAW, LINDA J. CORNFIELD, CELIA
BALFOUR, AND EUGENE A. MASH 26
Effect of Organ Perfusion on Renal Drug Transport:Application to Furosemide in the Isolated Per-fused Rat Kidney. LING-JAR LEE AND DAVID E.SMITH 32
Inhibition of 3-Methylindole Bioactivation by the Cy-tochrome P-450 Suicide Substrates 1-Am-inobenzotriazole and a-Methylbenzylaminoben-zotriazole. JEANNETT C. HUIJZER, JAMES D.ADAMS, JR., JOHN-YAN JAW, AND GAROLD S.YOST
Isolation and Identification of 6-Desmethylnaproxen
Sulfate as a New Metabolite of Naproxen in Hu-man Plasma. CHIN-HEN KIANG, CAROL LEE, AND
STANLEY KUSHINSKY 43
Fluconazole Is a Potent Inhibitor of Antipyrine Metab-olism in Vivo in Mice. IGNAzI0 LA DELFA, QUAN
MING ZHU, ZHENGJI Mo, AND TERRENCE F.BLASCHKE 49
Cilastatin-Insulin Interaction in the Rat. GREGORY C.TOMPKINS, LANE J. BRUNNER, AND DAVID R.LUKE
Characterization of a Carbamic Acid Ester Glu-curonide of the Secondary Amine, Sertraline.LARRY M. TREMAINE, JUSTIN G. STROH, AND
ROBERT A. RONFELD 58
Stereoselective Oxidation of Nilvadipine, a New Dihy-dropyridine Calcium Antagonist, in Rat and DogLiver. TosHiRo NIWA, YoJI TOKUMA, KIKUKO
NAKAGAWA, AND HIDEYO NOGUCHI 64
Identification of Two Main Urinary Metabolites of[‘4CjOmeprazole in Humans. LARS RENBERG,
ROGER SIMONSSON, AND KURT-JURGEN
HOFFMANN 698(S)-(Glutathione-S-YL)Dihydromorphinone, a Novel
14 Metabolite of Morphine from Guinea Pig Bile.
TAKASHI ISHIDA, Y0sHITO KUMAGAI, YURIKA
IKEDA, KENICHI ITO, MASASHI YANO, SATOSHI
20 TOKI, KUNIHIDE MIHASHI, TOSHIHIRO FUJIYOKA,
YUKIKO IWASE, AND SHIzUK0 HACHIYAMA . ...
Central Nervous System Kinetics of Atenolol
Metoprolol in the Dog during Long-Term Treat-ment. T. ABRAHAMSSON, E. LIGNELL, A. MIK-
ULSKI, S.-G. OLovSoN, AND C.-G. REGARDH 82
The Pharmacokinetics of Salicylate in the Pregnant
Wistar Rat. MARGARET DEAN, STAN PENGLIS,
AND BERESFORD STOCK 87
Temporal Variations in the Pharmacokinetics of Iso-niazid and N-Acetylisoniazid in Rats. PIERRE M.BELANGER, MARCEL LALANDE, FRANCOIS M.DORE, AND GASTON LABRECQUE 91
In Vivo and in Vitro Pharmacokinetic Differences be-tween Four Structurally Closely Related An-thracyclines in Hematopoietic Cell Subtypes inHumans. PAUL A. J. SPETH, PETER C. M. LIN-
SSEN, EMIEL F. S. TERMOND, JAN B. M. BOEZE-
MAN, HANS M. C. WESSELS, AND CLEMENS
HAANEN
Pulmonary Toxicity of Trichloroethylene in Mice: Co-valent Binding and Morphological Manifestations.P. G. FORKERT AND D. W. BIRCH 106
SHORT COMMUNICATION
Hepatic Drug Metabolism in Female Fischer Rats as aFunction of Age. LORA E. RIKANS 114
DRUG METABOLISM AND DISPOSITION (ISSN 0090-9556) is an official publication of the American Society for Pharmacology and Experimental Therapeutics and
is published bimonthly by Williams & Wilkins, 428 E. Preston St., Baltimore. MD 21202-3993. Second class postage paid at Baltimore, MD and at additional mailingoffices. POSTMASTER: Send address changes to DRUG METABOLISM AND DISPOSITION. 428 E. Preston St., Baltimore. MD 21202-3993. Price per volume: USA
inidividual rate $60; Japan $85 (includes air freight): all other countries $70 surface mail. USA institutional rate $95: Japan $120 (includes air freight): all other countries$105 surface mail and $95 to $105 air mail depending upon location. single copy $15 ($17 foreign). Prices subject to change. Copyright (C) 1989 by the American Societyfor Pharmacology and Experimental Therapeutics.
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Drug MetabolIsmand Disposition:the biological fate of chemicals
March/April 1989 Vol. 17, No. 2
CONTENTS
Methoxyflurane Enhances Allyl Alcohol Hepatotoxic-ity in Rats: Possible Involvement of Increased Ac-rolein Formation. WILLIAM C. KERSHAW, DEBO-
RAH A. BARSOTrI, THOMAS B. LEONARD, JOHN G.DENT, AND GARY L. LAGE 117
The Covalent Binding to Protein of Valproic Acid andIts Hepatotoxic Metabolite, 2-n-Propyl-4-penten-oic Acid, in Rats and in Isolated Rat Hepatocytes.DAVID J. PORUBEK, MARK P. GRILLO, AND
THOMAS A. BAILLIE
A Characterization of Chlordecone Pretreatment-alter-ed Pharmacokinetics in Mice. HILLARY M. CAR-
PENTER AND LAWRENCE R. CURTIS 131
Role of Pharmacokinetics and Metabolism in the En-hanced Susceptibility of Middle-aged Male Spra-gue-Dawley Rats to Acetaminophen Nephrotoxic-ity. JOAN B. TARLOFF, ROBIN S. GOLDSTEIN, BRUCE
A. MIco, AND JERRY B. HOOK
Effect of Experimental Diabetes on Elimination Kinet-ics of Diflunisal in Rats. JIUNN H. � FLORENCIA
A. DELUNA, DOMINICK J. Toxo, AND EDGAR H.ULM 147
Cocaine Disposition in Humans after Intravenous In-jection, Nasal Insufflation (Snorting), or Smoking.A. ROBERT JEFFcOAT, MARIO PEREZ-REYES, Ju-DITH M. HILL, BRIAN M. SADLER, AND C. EDGAR
CooK
On the Antipyrine Test in Laboratory Animals: Studiesin the Dog and Monkey. F. F. VICKERS, T. A.BOWMAN, B. H. DVORCHIK, 0. T. PASSANANTI, D.M. HUGHES, AND E. S. VESELL 160
The Physiological Disposition of Lovastatin. D. E.DUGGAN, I.-W. CHEN W. F. BAYNE, R. A. HALPIN,C. A. DUNCAN, M. S. SCHWARTZ, R. J. STUBBS,
AND S. VICKERS 166
Pharmacokinetics and Metabolism of SK&F 86002 inMale and Female Sprague-Dawley Rats. J. F. NEW-TON, L. P. Y0DI5, D. KEOHANE, R. ECKARDT, R.DEWEY, J. DENT, AND B. MIGG 174
N-Methylation as a Toxication Route for Xenobiotics.II. In Vivo Formation of N,N’-Dimethyl-4,4’-bi-
pyridyl Ion (Paraquat) from 4,4’-Bipyridyl in theGuinea Pig. C. STEVEN GODIN AND PETER A.
CROOKS
Spironolactone Metabolism in Target Tissues: Charac-teristics ofDeacetylation in Kidney, Liver, AdrenalCortex, and Testes. N. LYNN FLOWERS, JOHN P.O’DONNELL, AND HOWARD D. COLBY 186
Renal Tubular Secretion of Amioride and Its Inhibi-tion by Cimetidine in Humans and in an AnimalModel. ANDREW A. SOMOGYI, CHRISTOPHER M.HOVENS, MURRAY R. MUIRHEAD, AND FELIX
BOCHNER
Metabolism of Cyclosporin A. IV. Purification andIdentification of the Rifampicin-Inducible HumanLiver Cytochrome P-450 (Cyclosporin A Oxidase)as a Product of P4501 1 1A Gene Subfamily. JEAN
COMBALBERT, ISABELLE FABRE, GERARD FABRE,
ISABELLE DALET, J�N DERANcOURT, JEAN PAUL
CANO, AND PATRICK MAUREL
The Pharmacokinetics of Albumin Conjugates of �-
Penicillamine in Rats. DAVID A. JOYCE, DENIS N.WADE, AND BARBARA R. SWANSON 208
Stereoselective Metabolism and Pharmacokinetics ofRacemic Methylphenobarbital in Humans. WENGHUA LIM AND WAYNE D. HOOPER 212
Metabolic Interaction between Morphine and Nalox-one in Human Liver A Common Pathway ofGlucuronidation? AGNETA WAHLSTROM, KERSTIN
PERSSON, AND ANDERS RANE 218
SHORT COMMUNICATIONS
Species Differences in Protein Binding of Diflunisal.JIUNN H. LIN 221
Tissue Distribution of Intravenously Administered Di-
methyl Sulfoxide in the Normal Rat. MERRY C.NISHIMURA, PEYTON JACOB III, MARY E. CASSEL,
AND LAWRENCE H. Pirrs 224
Erratum 227
DRUG METABOLISM AND DISPOSITION (ISSN 0090-9556) is an official publication of the American Society for Pharmacology and Experimental Therapeuticsand is published bimonthly by Williams & Wilkins, 428 E. Preston St., Baltimore, MD 2 1202-3993. Second class postage paid at Baltimore, MD and at additionalmailing offices. POSTMASTER: Send address changes to DRUG METABOLISM AND DISPOSITION, 428 E. Preston St., Baltimore, MD 2 1202-3993. Price pervolume: USA individual rate $60; Japan $85 (includes air freight); all other countries $70 surface mail. USA institutional rate $95; Japan $120 (includes air freight); allother countries $105 surface mail and $95 to $105 air mail depending upon location, single copy $15 ($17 foreign). Prices subject to change. Copyright © 1989 by theAmerican 5ociety for Pharmacology and Experimental Therapeutics.
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Drug Metabolismand Disposition:the biological fate of chemicals
May/June 1989 Vol. 17, No. 3
CONTENTS
In Memoriam 229
Identification and Kinetic Characterization of Acetyla-tor Genotype-dependent and -independent Ary-
lamine Carcinogen N-Acetyltransferases in Ham-ster Bladder Cytosol. TOKUNBO YEROKUN, WARD
G. KIRLIN, ALMA TRINIDAD, RONALD J. FERGU-SON, FREDRICK OGOLLA, ALLEN F. ANDREWS,
PAMELA K. BRADY, AND DAVID W. HEIN
Kinetic Characterization of Acetylator Genotype-de-
pendent and -independent N-Acetyltransferase Iso-zymes in Homozygous Rapid and Slow AcetylatorInbred Hamster Liver Cytosol. ALMA TRINIDAD,WARD G. KIRLIN, FREDRICK OGOLLA, ALLEN F.ANDREWS, TOKUNBO YEROKUN, RONALD J. FER-GUSON, PAMELA K. BRADY, AND DAVID W. HEIN
Nasal Absorption and Metabolism of Progesterone and
l7f3-Estradiol in the Rat. RIMA N. BAWARSHI-NASSAR, ANWAR A. HUSSAIN, AND PETER A.
CROOKS 248
Human Intestinal Phenol Sulfotransferase: Assay Con-
ditions, Activity Levels and Partial Purification ofthe Thermolabile Form. RAJAH S. SUNDARAM,
CAROL SZUMLANSKI, DIANE OTFERNESS, JON A.VAN LOON, AND RICHARD M. WEINSHILBOUM ...
Characteristics of Warfarin Hydroxylation Catalyzed
by Human Liver Microsomes. ALLAN E. RETTIE,
A. CRAIG EDDY, LARRY D. HEIMARK, MIL0 GI-BALDI, AND WILLIAM F. TRAGER 265
Some Factors Affecting Phencyclidine Biotransforma-tion by Human Liver and Placenta. ROMANPOHORECKI, WILLIAM RAYBURN, WILLIAM W.COON, AND EDWARD F. DOMINO 271
dentification of Etretinate Metabolites in Human Bile.FLOIE M. VANE, CHRISTOPHER J. L. BUGGE, AND
LOLITA C. RODRIGUEZ 275
Identification of Etretinate Metabolites in HumanBlood. FLOIE M. VANE, CHRISTOPHER J. L. BuGGE,AND LOLITA C. RODRIGUEZ 280
Stereochemical Inversion of Haloxyfop in the Fischer344 Rat. M. J. BARTELS AND F. A. SMITH 286
Isolation of 10 Cyclosporine Metabolites from Human
Bile. C. PAUL WANG, NEIL R. HARTMAN, RAMANVENKATARAMANAN, IAN JARDINE, FU-TYAN LIN,
JOSEPH E. KNAPP, THOMAS E. STARZI, AND GIL-
BERT J. BURCKART
Quantitation of Multiple Pathways for the Metabolismof Nephrotoxic Cysteine Conjugates Using Selec-
tive Inhibitors of L-a-Hydroxy Acid Oxidase (i-
Amino Acid Oxidase) and Cysteine Conjugate
13-Lyase. JAMES L. STEVENS. PAUL B. HATZINGER,
AND PATRICK J. HAYDEN
Disposition ofthe Radioprotector Ethiofos in the Rhe-
sus Monkey: Influence ofRoute of Administration.DONALD J. MANGOLD, MICHAEL A. MILLER, Bi�-
LINDA K. HUELLE, DAWN 0. T. SANCHEZ-BARONA,
NOLLIE F. SWYNNERTON, LAWRENCE FLECKEN-
STEIN, AND THOMAS 0. LUDDEN
Metabolism of Bambuterol in Rat Liver Microsomes:Identification of Hydroxylated and DemethylatedProducts by Liquid Chromatography Mass Spec-
trometry. CLAES LINDBERG, CLAES Roos, ANDERSTUNEK, AND LEIF A. SVENSSON
Metabolism of the Antimycotic Agent, Croconazole,
in Rabbits. MASAYUKI NAKANO, YoslilKAzuNAKAJIMA, K0UJI IWATANI, YUJI lKENlSIll,
Yuzo NAKAGAWA, AND K0ICHI SUGENO 323
Haloperidol Reductase in Human and Guinea PigLivers. T. INABA AND J. KOVACS 330
Evidence in Humans for Variant Allozymes of the
Non-deficient Sparteine/Debrisoquine Mono-
oxygenase (P45OIID1) In Vitro. R. F. TYNDAI.E.
T. INABA, AND W. KALOW 334
Transport of Acetaminophen Conjugates in IsolatedRat Hepatocytes. SATOFUMI IIDA, TAKASHI Ml-
ZUMA, N0RIK0 SAKUMA, MASAHIRO HAYASHI, AND
SHOJI AWAZU 341
SHORT COMMUNICATIONS
Synthesis and Hydrolytic Behavior of the Sulfate Con-jugate of 2 ‘-Hydroxy-3,4,4’-trichlorocarbanilide.JOHN CRAIG, LARRY GRUENKE, HELEN N0RTII-
ROOT, AND NEAL CORBIN 345
Stimulation of in Vitro Bioactivation of Hydroquinone
by Phenol in Bone Marrow Cells. VANGALA V.SUBRAHMANYAM, ALBERT SADLER, ERIC SUBA,AND DAVID Ross 348
Carbonyl Sulfide: A Copper Chelating Metabolite ofDisulfiram. BENNY JOHANSSON 351
DRUG METABOLISM AND DISPOSITION (ISSN 0090-9556) is an official publication of the American Society for Pharmacology and Experimental Therapeutics
and is published bimonthly by Williams & Wilkins. 428 E. Preston St.. Baltimore. MD 21202-3993. Second class postage paid at Baltimore, MD and at additionalmailing offices. POSTMASTER: Send address changes to DRUG METABOLISM AND DISPOSITION. 428 E. Preston St.. Baltimore. MD 2 1202-3993. Price pervolume: USA individual rate $60: Japan $85 (includes air freight): all other countries $70 surface mail. USA institutional rate $95: Japan $120 (includes air freight): all
other countries $105 surface mail and $95 to $105 air mail depending upon location, single copy $15 ($17 foreign). Prices subject to change. Copyright c 989 h�’ the
American Society for Pharmacology and Experimental Therapeutics.
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Drug Metabolismand Disposition:the biological fate of chemicals
July/August 1989 Vol. 17, No. 4
CONTENTS
Investigations of the N-Hydroxylation of 3’-Hydroxy-
acetanilide, a Non-hepatotoxic Positional Isomerof Acetaminophen. MOHAMED S. RASHED, AN-
THONY J. STREETER, AND SIDNEY D. NELSON . . . . 355
Isozyme-specific Monoclonal Antibody-directed As-
sessment of Induction of Hepatic Cytochrome P-450 by Clotrimazole. WASIUDDIN A. KHAN, CHRIS-
TINE KUHN, HANS F. MERK, SANG S. PARK, HARRYV. GELBOIN, DAVID R. BICKERS, AND HASAN
MUKHTAR
Influence of Nutritional Status on the Pharmacoki-
netics and Pharmacodynamics of Pentobarbital.DONALD JUNG AND PRATAPA P. PRASAD 365
Pharmacokinetics ofRecombinant Human Tumor Ne-
crosis Factor-alpha in Rats: Effects of Size andNumber of Doses and Nephrectomy. B. L. FER-RAIOLO, J. MCCABE, S. HOLLENBACH, B. HULT-GREN, R. Prrrl, AND H. WILKING
Pharmacokinetics and Excretion of the 2 1-Aminoster-oid Antioxidant U-74006F in Rat and PerfusedRat Liver. JEFFREY W. Cox, PHILIP G. LARSON,MICHAEL A. WYNALDA, VIRENDRA K. SOOD, MI-
CHAEL T. VERBURG, AND ROBERT H. PULLEN ...
The Role of Flavin-containing Monooxygenase in theN-Oxidation of the Pyrrolizidine Alkaloid Sene-cionine. DAVID E. WILLIAMS, RALPH L. REED,
BOGDAN KEDZIERSKI, DANIEL M. ZIEGLER, AND
DONALD R. BUHLER
Bioactivation and Detoxication of the Pyrrolizidine
Alkaloid Senecionine by Cytochrome P-450 En-
zymes in Rat Liver. DAVID E. WILLIAMS, RALPH
L. REED, BOGDAN KEDZIERSKI, GHAZI A. DAN-
NAN, F. PETER GUENGERICH, AND DONALD R.BUHLER
In Vitro Metabolic Degradation of a Bovine GrowthHormone-Releasing Factor Analog LEU27-bGRF(l-29)NH2 in Bovine and Porcine Plasma:
Correlation with Plasma Dipeptidylpeptidase Ac-tivity. TERESA KUBIAK, COLLEEN KELLY, AND
LAVERN KRABIL
An Active, Aldehydic Metabolite of the Cell-differen-tiating Agent Hexamethylene Bisacetamide. BABUSABRAMANYAM, PATRICK S. CALLERY, MERRILL J.EGORIN, STUART SNYDER, AND BARBARA A.CONLEY
Plasma Pharmacokinetics and Urinary Excretion ofThalidomide After Oral Dosing in Healthy MaleVolunteers. TIAN-LING CHEN, GEORGIA B. VOGEL-
SANG, BRENT G. PErrY, ROBERT B. BRUNDRETr,
DENNIS A. N0E, GEORGE W. SANTOS, AND 0.MICHAEL COLVIN
Hydroxylation of 4.4’-Methylenebis(2-chloroaniline)
by Canine, Guinea Pig, and Rat Liver Microsomes.T. H. CHEN, B. I. KU5LIKI5, AND W. E. BRASELTON,JR . 406
Direct Determination of Diastereomeric Carprofen
Glucuronides in Human Plasma and Urine andPreliminary Measurements of Stereoselective Met-abolic and Renal Elimination After Oral Admin-istration of Carprofen in Man. SEIGO IWAKAWA,
TOSHIYUKI SUGANUMA, SHII-FUENG LEE. HILDE-
GARD SPAHN, LESLIE Z. BENET, AND EMIL T. LIN
Disposition ofFlavodilol in Laboratory Animals. MARY
COAN AND Ro� SIMMONS 420
Dose-dependent Kinetics of Cilastatin in LaboratoryAnimals. JIUNN H. LIN, 1-Wu CHEN, AND EDGAR
H. ULM 426
Glucuronidation of E-10-Hydroxynortriptyline in Hu-man Liver, Kidney, and Intestine: Organ-specificDifferences in Enantioselectivity. MARJA-LIISA
DAHL-PUUSTINEN, ETIENNE DUMONT, AND LEIF
BERTILSSON
Doxofylline in Rat Brain in Relation to LocomotorActivity. CARLO CRAVANZOLA, MARIA CAMILLAREBOANI, GI0RGI0 GROSA, AND JosE SEBASTIAN
FRANZONE 437
3,3’,4,4’-Tetrachlorobiphenyl: Excretion and TissueRetention of Hydroxylated Metabolites in the
Mouse. E. KLASSON WEHLER. A. BERGMAN, I.BRANDT, P. 0. DARNERUD. AND C. A. WACHT-
MEISTER
In Vitro Formation of an Inhibitory Complex Between
an Isosafrole Metabolite and Rat Hepatic Cyto-chrome P-450 PB-B. MICHAEL MURRAY AND GOR-
DON F. REIDY 449
Studies of Metabolic Pathways of Trimebutine by Si-multaneous Administration of Trimebutine andIts Deuterium-labeled Metabolite. YUJI MIURA,
SUSUMU CHISIMA, AND SHIGEYUKI TAKEYAMA... 455
Oxidation of Tenoxicam by Leukocyte Peroxidases andH�O2 Produces Novel Products. S. ICHIHARA, H.TOMI5AWA, H. FUKAZAWA, M. TATEISHI, R. JOLY,
ANDR.HEINTZ 463
DRUG METABOLISM AND DISPOSITION (I5SN 0090-9556) is an official publication of the American Society for Pharmacology and Experimental Therapeutics
and is published bimonthly by Williams & Wilkins. 428 E. Preston St.. Baltimore. MD 21202-3993. Second class postage paid at Baltimore. MD and at additionalmailing offices. POSTMASTER: Send address changes to DRUG METABOLISM AND DISPOSITION. 428 E. Preston St.. Baltimore. MD 21202-3993. Price pervolume: USA individual rate $60: Japan $85 (includes air freight): all other countries $70 surface mail. USA institutional rate $95: Japan $ 120 (includes air freight): all
other countries $105 surface mail and $95 to $105 air mail depending upon location, single copy $15 ($17 foreign). Prices subject to change. Copyright c 1989 by theAmerican Society for Pharmacology and Experimental Therapeutics.
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Drug Metabolismand Disposition:the biological fate of chemicals
September/October 1989 Vol. 17, No. 5
CONTENTS
Inhibition of the Localization and Metabolism of Ure-thane in the Mouse by Dimethyl Sulfoxide(DMSO). WILLIAM J. WADDELL, CAROLYN MAR-LOWE, TOSHINORI YAMAMOTO, AND MARY Jo
CLARK
The Pharmacokinetics ofEtretinate and Its Metabolitesin the Dog. PHENSRI THONGNOPNUA, JOSEPH W.MASSARELLA, AND CHERYL L. ZIMMERMAN 473
Metabolism of Acrylonitrile to 2-Cyanoethylene Oxidein F-344 Rat Liver Microsomes, Lung Micro-somes, and Lung Cells. ALAN E. ROBERTS, STEVENA. LACY, DENI5 PILON, MAX J. TURNER, JR., AND
DOUGLAS E. RICKERT
Characteristics of Monooxygenase-mediated CovalentBinding of Methoxychior in Human and Rat LiverMicrosomes. WILLIAM H. BULGER AND DAVID
KUPFER 487
Pharmacokinetics and Metabolism of a 4’-MethylthioDerivative of Propranolol in the Dog. S. A. BAI,D. E. EA5TERLING, M. J. WILSON, U. K. WALLE,C. A. HANEY, N. P. Pm, J. K. PRUETT, AND T.WALLE
Age-related Changes in the Disposition of Benzyl Ace-tate: A Model Compound for Glycine Conjugation.TIMOTHY F. MCMAHON, JANET J. DILIBERTO, AND
LINDA S. BIRNBAUM 506
Metabolic Conversion of 2-Propylpentanal Acetals toVaiproic Acid In Vitro: Model of Prodrugs of Car-boxylic Acid Agents. DOMENICK VICCHIO AND PA-
TRICK S. CALLERY 513
Disposition, Metabolism, and Excretion of U-7l038, ANovel Renin Inhibitor Peptide, in the Rat. JOHN
C. GREENFIELD, KATHLEEN J. COOK, AND IRVING
A. O’LEARY 518
Human and Dog, But Not Rat, Isolated HepatocytesHave Decreased Foreign Compound-metabolizing
Ability Compared to Liver Slices. G. P0wIS, D. C.MELDER, AND T. J. WILKE 526
Biotransformation of Tipredane, A Novel Topical Ste-roid, in Mouse, Rat, and Human Liver Homoge-nates. S. J. LAN, L. M. SCANLAN, S. H. WEINSTEIN,
R. K. YARMA, B. M. WARRACK, S. E. UNGER, M.A. PORUBCAN, AND B. H. MIGDALOF
Metabolism and Disposition of the 4-HT UptakeBlocker Sertraline in the Rat and Dog. LARRY M.TREMAINE, WILLARD M. WELCH, AND ROBERT A.RONFELD 542
Cytochromes P-450 in Murine Lung: An Immunohis-tochemical Study with Monoclonal Antibodies. P.G. FORKERT, M. L. VESSEY, S. S. PARK, H. V.GELBOIN, AND S. P. C. COLE 551
First-Pass Metabolism of Salicylamide: Studies in theOnce-Through Vascularly Perfused Rat Intestine-Liver Preparation. XIN XU, HIR0KI HIRAYAMA,
AND K. SANDY PANG 556
Deimidazolation of Antimycotic Croconazole ThroughEpoxide Formation in Rabbit Liver Microsomes.MASAYUKI NAKANO AND KENJI MIz0JIRI 564
In Vitro Studies of Human Liver Alcohol Dehydroge-nase Variants Using a Variety of Substrates. JEAN-
INE P. KAssAM, BING K. TANG, DEzso KADAR,
AND WERNER KALOW 567
Systemic Intestinal Metabolism of 1-Naphthol: A Studyin the Isolated Vascularly Perfused Rat Small In-testine. MICHIEL H. DE VRIES, GERARD A. H0F-
MAN, ANDRIES 5j. KO5TER, AND JAN NOORDHOEK 573
The Influence of Phenobarbital Administration on He-patic Monooxygenase Activity at Various Stages ofGestation in the Rat. MARGARET E. DEAN AND
BERESFORD H. STOCK 579
DRUG METABOLISM AND DISPOSITION (ISSN 0090-9556) is an official publication of the American Society for Pharmacology and Experimental Therapeuticsand is published bimonthly by Williams & Wilkins. 428 E. Preston St., Baltimore, MD 2 1202-3993. Second class postage paid at Baltimore, MD and at additionalmailing offices. POSTMASTER: Send address changes to DRUG METABOLISM AND DISPOSITION, 428 E. Preston St., Baltimore, MD 2 1202-3993. Price pervolume: USA individual rate $60; Japan $85 (includes air freight); all other countries $70 surface mail. USA institutional rate $95; Japan $120 (includes air freight); allother countries $105 surface mail and $95 to $105 air mail depending upon location, single copy $15 ($17 foreign). Prices subject to change. Copyright © 1989 by theAmerican Society for Pharmacology and Experimental Therapeutics.
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Drug Metabolismand Disposition:the biological fate of chemicals
November/December 1989 Vol. 17, No. 6
CONTENTS
Best Paper of 1988
Disposition and Pharmacokinetics of Naltrexone AfterIntravenous and Oral Administration in RhesusMonkeys. RICHARD H. REUNING, SUSAN B. AsH-CROFT, JAMES N. WILEY, AND BRENT E.MORRISON
Comparative Pharmacokinetics of 3’-Azido-3’-deoxy-
thymidine (AZT) and 3’-Azido-2’,3 ‘-dideoxyuri-dine (AZddU) in Mice. KOKILA J. DOSHI, JAMES
M. GALLO, F. DOUGLAS BOUDINOT, AND CHUNG
K. CHUPharmacokinetic Analysis ofCyclosporine in Adjuvant
Arthritic Rats. STANLEY H. POLLOCK, HEWITT W.MATTHEWS, AND MARTIN J. D’SOUZA
Enterohepatic Circulation of T-2 Toxin Metabolites inthe Rat. KATHLEEN A. CODDINGTON, STEVEN P.SWANSON, ASLAM S. HASSAN, AND WILLIAM B.BUCK
Metabolism of a Nitrogen-containing Steroid by RatHepatocytes and Hepatic Subcellular Fractions.
GREGORY L. KEDDERIS, LOIS S. ARGENBRIGHT,
JOHN S. WALSH, JACK L. SMITH, RALPH A.STEARNS, BYRON A. ARISON, AND GERALD T.MIWA
Metabolism, Disposition, and Mutagenicity of 2,6-Diaminotoluene, a Mutagenic Noncarcinogen.
MICHAEL L. CUNNINGHAM, LEO T. BURKA, AND
H. B. MATTHEWS
Biotransformation of Etretinate and DevelopmentalToxicity of Etretin and Other Aromatic Retinoids
in Teratogenesis Bioassays. D. M. KOCHHAR, J. D.PENNER, AND L. M. MINUTELLA
Metabolism of the Antianxiety Drug Buspirone in the
Rat. HEMANT K. JAJOO, ROBERT F. MAYOL, JOHN
A. LABUDDE, AND IAN A. BLAIR
Metabolism of the Antianxiety Drug Buspirone in Hu-
man Subjects. HEMANT K. JAJOO, ROBERT F.MAY01, JOHN A. LABUDDE, AND IAN A. BLAIR..
The Pharmacokinetics of (3H)l-(l-(2-Thienyl)cyclo-hexyl)piperidine (TCP) in Sprague-Dawley Rats.MARK ZORBAS, S. MICHAEL OWENS, LAURA M.PLUNKETT, AND HOANG BUI
Influence of Pregnancy on the Pharmacokinetic Dis-
position of Two Aromatic Retinoids (Etretinate
and Acitretin) in the Rat. I. Intravenous Studies.KENNETH R. BROUWER AND PATRICK J.MCNAMARA
Influence of Pregnancy on the Pharmacokinetic Dis-position of Two Aromatic Retinoids (Etretinateand Acitretin) in the Rat. II. Single and Multiple
Oral Dosing Studies. KENNETH R. BROUWER AND
PATRICK J. MCNAMARA
Metabolism, Disposition, and Pharmacokinetics of aPotent Anticonvulsant, 4-Amino-N-(2,6-Dime-thylphenyl)benzamide (LY2O1 1 16), in Rats.BRIAN D. Porrs, STEVE GABRIEL, AND C. JOHN
PARLI
In Vivo Metabolism of Isoxicam in Rats, Dogs, and
Monkeys. THOMAS F. WOOLF, ANN BLACK, JAMES
L. HICKS, HELEN LEE, CHE C. HUANG, AND TSUN
CHANG
Physiological Disposition of CGS 16617 in Rat, Dog,and Man. H. EGGER, G. KOCHAK, P. ROBERTSON,R. IANNUCCI, F. A. RUFINO, AND F. STANCATO ..
Oral Idazoxan Bioavailability in Rat: Relevance of In-testinal and Hepatic First-Pass Effect. J. VALLES, J.PRU?ZJONOSA, A. MENARGUES, M. NOMEN, AND R.OBACH
Dose-related Effects of Phenobarbital on Hepatic Glu-tathione S-transferase Activity and Ligandin Levelsin the Rat. HIROKAI OKUDA, BARRY J. POTTER,
BRIGETrE BLADES, TERESA A. MCHUGH, NATALIE
L. JACOBS, AND PAUL D. BERKBiotransformation of 5-(2-Chloroethyl)-2’-deoxyuri-
dine in Male NMRI Mice. I. SZINAI AND E. DE
CLERCQ
The Uptake of Clodronate (Dichloromethylene Bis-phosphonate) by Macrophages In Vivo and In Vi-
tro. JUKKA MONKKONEN, ARTO URTTI, PETFERI
PARNONEN, HEIKKI A. ELO, AND PAULI YLITALO.
Sensitivity of the Rat Liver Microsomal Oxidation ofPyrazole to Antibody Raised Against the Ethanol-inducible Rabbit Liver Cytochrome P-450 Iso-
zyme. LIvIU A. CLEJAN, DENNIS R. Koo�, AND
ARTHUR I. CEDERBAUM
Disposition of Sandostatin, a New Synthetic Somato-statin Analogue, in Rats. M. LEMAIRE, M. AZRIA,
R. DANNECKER, P. MARBACH, A. SCHWEITZER,
AND G. MAURER
Amiodarone-Digoxin Interaction in Rats: A Reductionin Hepatic Intake. CHANTAL LAMBERT, DANIEL
LAMONTAGNE, HELEN HOTTLET, AND PATRICK DU
SOUICH
SHORT COMMUNICATION
Regional Differences in Adrenal Activation of Spiron-
olactone: Relationship to Steroid 17a-HydroxylaseActivity. J. H. SHERRY, P. B. JOHNSON, M. LEVITT,
J. BERGSTROM, AND H. D. COLBY
Author Index
Subject Index
DRUG METABOLISM AND DISPOSITION (ISSN 0090-9556) is an official publication of the American Society for Pharmacology and Experimental Therapeutics
and is published bimonthly by Williams & Wilkins, 428 E. Preston St. Baltimore. MD 2 1 202-3993. Second class postage paid at Baltimore, MD and at additionalmailing offices. POSTMASTER: Send address changes to DRUG MEt ABOLISM AND DISPOSITION, 428 E. Preston St., Baltimore, MD 2 1 202-3993. Price pervolume: USA individual rate $70; Japan $107 (includes air freight); all other countries $85 surface mail. USA institutional rate $1 10; Japan $147 (includes air freight):
all other countries $125 surface mail. Single copy $15.00 ($18.00 foreign). Prices subject to change. Copyright © 1989 by the American Society for Pharmacology andExperimental Therapeutics.
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