7

77

37

98

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.

at ASPE

T Journals on A

ugust 3, 2021dm

d.aspetjournals.orgD

ownloaded from

123

139

190

197

153

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.

at ASPE

T Journals on A

ugust 3, 2021dm

d.aspetjournals.orgD

ownloaded from

231

238

297

304

311

255

292

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.

at ASPE

T Journals on A

ugust 3, 2021dm

d.aspetjournals.orgD

ownloaded from

360

402

414

433

369

373

380

387

393

398

441

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.

at ASPE

T Journals on A

ugust 3, 2021dm

d.aspetjournals.orgD

ownloaded from

469

481

532

495

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.

at ASPE

T Journals on A

ugust 3, 2021dm

d.aspetjournals.orgD

ownloaded from

583

590

595

600

606

612

618

625

634

641

646

652

656

662

669

673

677

683

690

694

699

704

709

711

713

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.

at ASPE

T Journals on A

ugust 3, 2021dm

d.aspetjournals.orgD

ownloaded from