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Items: 50

1.

Metabolism of rofecoxib in vitro using human liver subcellular fractions.

Slaughter D, Takenaga N, Lu P, Assang C, Walsh DJ, Arison BH, Cui D, Halpin RA, Geer LA, Vyas KP, Baillie TA.

Drug Metab Dispos. 2003 Nov;31(11):1398-408.

PMID:
14570773
2.

Acyl glucuronidation and glucosidation of a new and selective endothelin ET(A) receptor antagonist in human liver microsomes.

Tang C, Hochman JH, Ma B, Subramanian R, Vyas KP.

Drug Metab Dispos. 2003 Jan;31(1):37-45.

PMID:
12485951
3.

The disposition and metabolism of rofecoxib, a potent and selective cyclooxygenase-2 inhibitor, in human subjects.

Halpin RA, Porras AG, Geer LA, Davis MR, Cui D, Doss GA, Woolf E, Musson D, Matthews C, Mazenko R, Schwartz JI, Lasseter KC, Vyas KP, Baillie TA.

Drug Metab Dispos. 2002 Jun;30(6):684-93.

PMID:
12019196
4.

Mechanistic studies on the reversible metabolism of rofecoxib to 5-hydroxyrofecoxib in the rat: evidence for transient ring opening of a substituted 2-furanone derivative using stable isotope-labeling techniques.

Baillie TA, Halpin RA, Matuszewski BK, Geer LA, Chavez-Eng CM, Dean D, Braun M, Doss G, Jones A, Marks T, Melillo D, Vyas KP.

Drug Metab Dispos. 2001 Dec;29(12):1614-28.

PMID:
11717181
5.

Influence of beta-adrenoceptor antagonists on the pharmacokinetics of rizatriptan, a 5-HT1B/1D agonist: differential effects of propranolol, nadolol and metoprolol.

Goldberg MR, Sciberras D, De Smet M, Lowry R, Tomasko L, Lee Y, Olah TV, Zhao J, Vyas KP, Halpin R, Kari PH, James I.

Br J Clin Pharmacol. 2001 Jul;52(1):69-76.

6.

The absorption, distribution, metabolism and excretion of rofecoxib, a potent and selective cyclooxygenase-2 inhibitor, in rats and dogs.

Halpin RA, Geer LA, Zhang KE, Marks TM, Dean DC, Jones AN, Melillo D, Doss G, Vyas KP.

Drug Metab Dispos. 2000 Oct;28(10):1244-54.

PMID:
10997947
7.

Metabolism of A dopamine D(4)-selective antagonist in rat, monkey, and humans: formation of A novel mercapturic acid adduct.

Zhang KE, Kari PH, Davis MR, Doss G, Baillie TA, Vyas KP.

Drug Metab Dispos. 2000 Jun;28(6):633-42.

PMID:
10820134
8.

Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.

Lagu B, Tian D, Chiu G, Nagarathnam D, Fang J, Shen Q, Forray C, Ransom RW, Chang RS, Vyas KP, Zhang K, Gluchowski C.

Bioorg Med Chem Lett. 2000 Jan 17;10(2):175-8.

PMID:
10673105
9.
10.

Rizatriptan, a novel 5-HT1B/1D agonist for migraine: single- and multiple-dose tolerability and pharmacokinetics in healthy subjects.

Goldberg MR, Lee Y, Vyas KP, Slaughter DE, Panebianco D, Ermlich SJ, Shadle CR, Brucker MJ, McLoughlin DA, Olah TV.

J Clin Pharmacol. 2000 Jan;40(1):74-83.

PMID:
10631625
11.

Disposition and pharmacokinetics of the antimigraine drug, rizatriptan, in humans.

Vyas KP, Halpin RA, Geer LA, Ellis JD, Liu L, Cheng H, Chavez-Eng C, Matuszewski BK, Varga SL, Guiblin AR, Rogers JD.

Drug Metab Dispos. 2000 Jan;28(1):89-95.

PMID:
10611145
12.

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.

Wong WC, Sun W, Lagu B, Tian D, Marzabadi MR, Zhang F, Nagarathnam D, Miao SW, Wetzel JM, Peng J, Forray C, Chang RS, Chen TB, Ransom R, O'Malley S, Broten TP, Kling P, Vyas KP, Zhang K, Gluchowski C.

J Med Chem. 1999 Nov 18;42(23):4804-13.

PMID:
10579843
13.

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.

Lagu B, Tian D, Nagarathnam D, Marzabadi MR, Wong WC, Miao SW, Zhang F, Sun W, Chiu G, Fang J, Forray C, Chang RS, Ransom RW, Chen TB, O'Malley S, Zhang K, Vyas KP, Gluchowski C.

J Med Chem. 1999 Nov 18;42(23):4794-803.

PMID:
10579842
14.

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.

Murali Dhar TG, Nagarathnam D, Marzabadi MR, Lagu B, Wong WC, Chiu G, Tyagarajan S, Miao SW, Zhang F, Sun W, Tian D, Shen Q, Zhang J, Wetzel JM, Forray C, Chang RS, Broten TP, Schorn TW, Chen TB, O'Malley S, Ransom R, Schneck K, Bendesky R, Harrell CM, Vyas KP, et al.

J Med Chem. 1999 Nov 18;42(23):4778-93.

PMID:
10579841
15.

In vitro and in vivo studies on the metabolism of tirofiban.

Vickers S, Theoharides AD, Arison B, Balani SK, Cui D, Duncan CA, Ellis JD, Gorham LM, Polsky SL, Prueksaritanont T, Ramjit HG, Slaughter DE, Vyas KP.

Drug Metab Dispos. 1999 Nov;27(11):1360-6.

PMID:
10534322
16.

Pharmacokinetics of intravenous alendronate.

Cocquyt V, Kline WF, Gertz BJ, Van Belle SJ, Holland SD, DeSmet M, Quan H, Vyas KP, Zhang KE, De Grève J, Porras AG.

J Clin Pharmacol. 1999 Apr;39(4):385-93.

PMID:
10197297
17.

Metabolism of MK-499, a class III antiarrhythmic agent, in rats and dogs.

Vickers S, Duncan CA, Slaughter DE, Arison BH, Greber T, Olah TV, Vyas KP.

Drug Metab Dispos. 1998 May;26(5):388-95.

PMID:
9571219
18.

In vitro metabolism of simvastatin in humans [SBT]identification of metabolizing enzymes and effect of the drug on hepatic P450s.

Prueksaritanont T, Gorham LM, Ma B, Liu L, Yu X, Zhao JJ, Slaughter DE, Arison BH, Vyas KP.

Drug Metab Dispos. 1997 Oct;25(10):1191-9.

PMID:
9321523
19.
20.

Disposition of L-738,167, a potent and long-acting fibrinogen receptor antagonist, in dogs. Dose-dependent pharmacokinetics.

Prueksaritanont T, Gorham LM, Naue JA, Hamill TG, Askew BC, Vyas KP.

Drug Metab Dispos. 1997 Mar;25(3):355-61.

PMID:
9172954
21.

Species and organ differences in first-pass metabolism of the ester prodrug L-751,164 in dogs and monkeys. In vivo and in vitro studies.

Prueksaritanont T, Gorham LM, Ellis JD, Fernandez-Metzler C, Deluna P, Gehret JR, Strong KL, Hochman JH, Askew BC, Duggan ME, Gilbert JD, Lin JH, Vyas KP.

Drug Metab Dispos. 1996 Nov;24(11):1263-71.

PMID:
8937862
22.

Comparative studies of drug-metabolizing enzymes in dog, monkey, and human small intestines, and in Caco-2 cells.

Prueksaritanont T, Gorham LM, Hochman JH, Tran LO, Vyas KP.

Drug Metab Dispos. 1996 Jun;24(6):634-42.

PMID:
8781778
23.

Microsomal metabolism of the 5-lipoxygenase inhibitor L-739,010: evidence for furan bioactivation.

Zhang KE, Naue JA, Arison B, Vyas KP.

Chem Res Toxicol. 1996 Mar;9(2):547-54.

PMID:
8839061
24.
25.

Disposition of MK-852, a fibrinogen receptor antagonist, in rats and dogs.

Vickers S, Duncan CA, Yuan AS, Vyas KP.

Drug Metab Dispos. 1994 Jul-Aug;22(4):631-6.

PMID:
7956740
26.

Biotransformation of lovastatin. V. Species differences in in vivo metabolite profiles of mouse, rat, dog, and human.

Halpin RA, Ulm EH, Till AE, Kari PH, Vyas KP, Hunninghake DB, Duggan DE.

Drug Metab Dispos. 1993 Nov-Dec;21(6):1003-11.

PMID:
7905377
27.

In vivo and in vitro metabolism studies on a class III antiarrhythmic agent.

Vickers S, Duncan CA, Kari PH, Homnick CF, Elliott JM, Pitzenberger SM, Hichens M, Vyas KP.

Drug Metab Dispos. 1993 May-Jun;21(3):467-73.

PMID:
8100503
28.
29.

HMG-CoA reductase inhibitor-induced myopathy in the rat: cyclosporine A interaction and mechanism studies.

Smith PF, Eydelloth RS, Grossman SJ, Stubbs RJ, Schwartz MS, Germershausen JI, Vyas KP, Kari PH, MacDonald JS.

J Pharmacol Exp Ther. 1991 Jun;257(3):1225-35.

PMID:
1904494
30.

Metabolism of antiparkinson agent dopazinol by rat liver microsomes.

Vyas KP, Kari PH, Ramjit HG, Pitzenberger SM, Hichens M.

Drug Metab Dispos. 1990 Nov-Dec;18(6):1025-30.

PMID:
1981508
31.

In vitro and in vivo biotransformation of simvastatin, an inhibitor of HMG CoA reductase.

Vickers S, Duncan CA, Vyas KP, Kari PH, Arison B, Prakash SR, Ramjit HG, Pitzenberger SM, Stokker G, Duggan DE.

Drug Metab Dispos. 1990 Jul-Aug;18(4):476-83.

PMID:
1976071
32.
33.

Biotransformation of lovastatin. I. Structure elucidation of in vitro and in vivo metabolites in the rat and mouse.

Vyas KP, Kari PH, Pitzenberger SM, Halpin RA, Ramjit HG, Arison B, Murphy JS, Hoffman WF, Schwartz MS, Ulm EH, et al.

Drug Metab Dispos. 1990 Mar-Apr;18(2):203-11.

PMID:
1971574
34.

Regioselectivity and stereoselectivity in the metabolism of HMG-CoA reductase inhibitors.

Vyas KP, Kari PH, Pitzenberger SM.

Biochem Biophys Res Commun. 1990 Feb 14;166(3):1155-62.

PMID:
2306236
35.
36.

A radioimmunoassay for the anticonvulsant and neuroprotective agent, MK-801.

Hichens M, Greber TF, Vyas KP.

J Immunoassay. 1990;11(4):477-502.

PMID:
2283390
37.

Radioimmunoassays for the enantiomeric components of indacrinone and their phenolic metabolites.

Vyas KP, Hichens M, Mulcahy WS, Hand EL.

J Immunoassay. 1987;8(2-3):179-201.

PMID:
3624493
38.
39.

Stereoselectivity of cytochrome P-450c in the formation of naphthalene and anthracene 1,2-oxides.

van Bladeren PJ, Vyas KP, Sayer JM, Ryan DE, Thomas PE, Levin W, Jerina DM.

J Biol Chem. 1984 Jul 25;259(14):8966-73.

41.

Metabolism and hepatotoxicity of the naturally occurring benzo[b]pyran precocene I.

Halpin RA, Vyas KP, El-Naggar SF, Jerina DM.

Chem Biol Interact. 1984 Mar;48(3):297-315.

PMID:
6713597
42.

Regioselectivity and stereoselectivity in the metabolism of trans-1,2-dihydroxy-1,2-dihydrobenz[a]anthracene by rat liver microsomes.

Vyas KP, van Bladeren PJ, Thakker DR, Yagi H, Sayer JM, Levin W, Jerina DM.

Mol Pharmacol. 1983 Jul;24(1):115-23.

PMID:
6865920
43.

Metabolism of alpha-naphthoflavone and beta-naphthoflavone by rat liver microsomes and highly purified reconstituted cytochrome P-450 systems.

Vyas KP, Shibata T, Highet RJ, Yeh HJ, Thomas PE, Ryan DE, Levin W, Jerina DM.

J Biol Chem. 1983 May 10;258(9):5649-59. No abstract available.

44.

Tumorigenicity of enantiomers of chrysene 1,2-dihydrodiol and of the diastereomeric bay-region chrysene 1,2-diol-3,4-epoxides on mouse skin and in newborn mice.

Chang RL, Levin W, Wood AW, Yagi H, Tada M, Vyas KP, Jerina DM, Conney AH.

Cancer Res. 1983 Jan;43(1):192-6. No abstract available.

45.

Mutagenicity of the optical isomers of the diastereomeric bay-region chrysene 1,3-diol-3,4-epoxides in bacterial and mammalian cells.

Wood AW, Chang RL, Levin W, Yagi H, Tada M, Vyas KP, Jerina DM, Conney AH.

Cancer Res. 1982 Aug;42(8):2972-6.

46.

Stereoselective metabolism of the (+)- and (-)-enantiomers of trans-1,2-dihydroxy-1,2-dihydrochrysene to bay-region 1,2-diol-3,4-epoxide diastereomers by rat liver enzymes.

Vyas KP, Levin W, Yagi H, Thakker DR, Ryan DE, Thomas PE, Conney AH, Jerina DM.

Mol Pharmacol. 1982 Jul;22(1):182-9. No abstract available.

PMID:
7121449
47.

Stereoselective metabolism of the optical isomers of trans-1,2-dihydroxy-1,2-dihydrophenanthrene to bay-region diol epoxides by rat liver microsomes.

Vyas KP, Thakker DR, Levin W, Yagi H, Conney AH, Jerina DM.

Chem Biol Interact. 1982 Jan;38(2):203-13. No abstract available.

PMID:
7055851
48.

Metabolism of (-)-trans-(3R, 4R)-dihydroxy-3,4-dihydrochrysene to diol epoxides by liver microsomes.

Vyas KP, Yagi H, Levin W, Conney AH, Jerina DM.

Biochem Biophys Res Commun. 1981 Feb 27;98(4):961-9. No abstract available.

PMID:
7225135
49.

Metabolism of chrysene and phenanthrene to bay-region diol epoxides by rat liver enzymes.

Nordqvist M, Thakker DR, Vyas KP, Yagi H, Levin W, Ryan DE, Thomas PE, Conney AH, Jerina DM.

Mol Pharmacol. 1981 Jan;19(1):168-78. No abstract available.

PMID:
7207460
50.

Substituent effects on the hepatotoxicity of thiobenzamide derivatives in the rat.

Hanzlik RP, Vyas KP, Traiger GJ.

Toxicol Appl Pharmacol. 1978 Dec;46(3):685-94. No abstract available.

PMID:
746555

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