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Ralph Stearns

Research Profile

Living Beings

Anatomy

Microsomes, Liver

Physiology

Biotransformation

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Chemicals & Drugs

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TOP 3
Qingmei Hong; Raman K Bakshi; Brenda L Palucki; Min K Park; Zhixiong Ye; Shuwen He; Patrick G Pollard; Iyassu K Sebhat; Jian Liu; Liangqin Guo; Doreen E Cashen; William J Martin; David Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R Miller; Ralph A Stearns; Howard Y Chen; Airu S Chen; Alison M Strack; Tung M Fong; D Euan MacIntyre; Matthew J Wyvratt; Ravi P Nargund
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Shuwen He; Zhixiong Ye; Peter H Dobbelaar; Raman K Bakshi; Qingmei Hong; James P Dellureficio; Iyassu K Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L Franklin; Mikhail Reibarkh; Mark A Holmes; David Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R Miller; Ralph A Stearns; Howard Y Chen; Airu S Chen; Alison M Strack; Tung M Fong; Matthew J Wyvratt; Ravi P Nargund
Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.
V B G Reddy; George A Doss; Bindhu V Karanam; Koppara Samuel; Thomas J Lanza; Linus S Lin; Nathan X Yu; A S Zhang; C E Raab; Ralph A Stearns; Sanjeev Kumar
In vitro and in vivo metabolism of a novel cannabinoid-1 receptor inverse agonist, taranabant, in rats and monkeys.

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All Publications

2011: Qingmei Hong; Raman K Bakshi; Brenda L Palucki; Min K Park; Zhixiong Ye; Shuwen He; Patrick G Pollard; Iyassu K Sebhat; Jian Liu; Liangqin Guo; Doreen E Cashen; William J Martin; David Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R Miller; Ralph A Stearns; Howard Y Chen; Airu S Chen; Alison M Strack; Tung M Fong; D Euan MacIntyre; Matthew J Wyvratt; Ravi P Nargund
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Bioorganic & medicinal chemistry letters 2011;21(8):2330-4.
2010: Shuwen He; Zhixiong Ye; Peter H Dobbelaar; Raman K Bakshi; Qingmei Hong; James P Dellureficio; Iyassu K Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L Franklin; Mikhail Reibarkh; Mark A Holmes; David Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R Miller; Ralph A Stearns; Howard Y Chen; Airu S Chen; Alison M Strack; Tung M Fong; Matthew J Wyvratt; Ravi P Nargund
Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.
Bioorganic & medicinal chemistry letters 2010;20(22):6524-32.
2010: V B G Reddy; George A Doss; Bindhu V Karanam; Koppara Samuel; Thomas J Lanza; Linus S Lin; Nathan X Yu; A S Zhang; C E Raab; Ralph A Stearns; Sanjeev Kumar
In vitro and in vivo metabolism of a novel cannabinoid-1 receptor inverse agonist, taranabant, in rats and monkeys.
Xenobiotica; the fate of foreign compounds in biological systems 2010;40(9):650-62.
2010: Shuwen He; Zhixiong Ye; Peter H Dobbelaar; Iyassu K Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L Franklin; Raman K Bakshi; James P Dellureficio; Qingmei Hong; David Weinberg; Tanya MacNeil; Rui Tang; Alison M Strack; Constantin Tamvakopoulos; Qianping Peng; Randy R Miller; Ralph A Stearns; Howard Y Chen; Airu S Chen; Tung M Fong; Matthew J Wyvratt; Ravi P Nargund
Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.
Bioorganic & medicinal chemistry letters 2010;20(15):4399-405.
2010: Shuwen He; Zhixiong Ye; Peter H Dobbelaar; Iyassu K Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L Franklin; Raman K Bakshi; James P Dellureficio; Qingmei Hong; Nancy N Tsou; Richard G Ball; Doreen E Cashen; William J Martin; David Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R Miller; Ralph A Stearns; Howard Y Chen; Airu S Chen; Alison M Strack; Tung M Fong; D Euan MacIntyre; Matthew J Wyvratt; Ravi P Nargund
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
Bioorganic & medicinal chemistry letters 2010;20(7):2106-10.
2008: Wei Tang; Ralph A Stearns; Regina W Wang; Randall R Miller; Qing Chen; Jason S Ngui; Raman K Bakshi; Ravi P Nargund; Dennis C Dean; Thomas A Baillie
Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: a case study with melanocortin-4 receptor agonists.
Xenobiotica; the fate of foreign compounds in biological systems 2008;38(11):1437-51.
2008: Wei Tang; Ralph A Stearns; Qing Chen; K Bleasby; Yohannes Teffera; Adria Colletti; M Hafey; Raymond Evers; Dennis C Dean; Plato A Magriotis; Thomas J Lanza; Linus S Lin; William K Hagmann; Thomas A Baillie
Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats.
Xenobiotica; the fate of foreign compounds in biological systems 2008;38(2):223-37.
2008: Ying Li; J Greg Slatter; Zhoupeng Zhang; Yan Li; George A Doss; Matthew P Braun; Ralph A Stearns; Dennis C Dean; Thomas A Baillie; Wei Tang
In vitro metabolic activation of lumiracoxib in rat and human liver preparations.
Drug metabolism and disposition: the biological fate of chemicals 2008;36(2):469-73.
2007: Maria G Beconi; James R Reed; Yohannes Teffera; Yuan-Qing Xia; Christopher J Kochansky; David Q Liu; Shiyao Xu; Charles S Elmore; Suzanne L Ciccotto; Donald F Hora; Ralph A Stearns; Stella H Vincent
Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs.
Drug metabolism and disposition: the biological fate of chemicals 2007;35(4):525-32.
2007: David Q Liu; Byron H Arison; Ralph A Stearns; Dooseop Kim; Stella H Vincent
Characterization of two cyclic metabolites of sitagliptin.
Drug metabolism and disposition: the biological fate of chemicals 2007;35(4):521-4.
2006: Qing Chen; George A Doss; Elaine C Tung; Wensheng Liu; Yui S Tang; Matthew P Braun; Varsha Didolkar; John R Strauss; Regina W Wang; Ralph A Stearns; David C Evans; Thomas A Baillie; Wei Tang
Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats.
Drug metabolism and disposition: the biological fate of chemicals 2006;34(1):145-51.
2005: Zhixiong Ye; Liangqin Guo; Khaled Barakat; Patrick G Pollard; Brenda L Palucki; Iyassu K Sebhat; Raman K Bakshi; Rui Tang; Rubana N Kalyani; Aurawan Vongs; Airu S Chen; Howard Y Chen; Charles I Rosenblum; Tanya MacNeil; David Weinberg; Qianping Peng; Constantin Tamvakopoulos; Randall R Miller; Ralph A Stearns; Doreen E Cashen; William J Martin; Joseph M Metzger; Alison M Strack; D Euan MacIntyre; Lex H T Van Der Ploeg; Arthur A Patchett; Matthew J Wyvratt; Ravi P Nargund
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Bioorganic & medicinal chemistry letters 2005;15(15):3501-5.
2005: Raman K Bakshi; Qingmei Hong; J T Olson; Zhixiong Ye; Iyassu K Sebhat; David Weinberg; Tanya MacNeil; Rubana N Kalyani; Rui Tang; William J Martin; Alison M Strack; Erin McGowan; Constantin Tamvakopoulos; Randall R Miller; Ralph A Stearns; Wei Tang; D Euan Maclntyre; Lex H T Van Der Ploeg; Arthur A Patchett; Ravi P Nargund
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bioorganic & medicinal chemistry letters 2005;15(14):3430-3.
2005: J Shang; Shiyao Xu; Yohannes Teffera; George A Doss; Ralph A Stearns; S Edmonson; Maria G Beconi
Metabolic activation of a pentafluorophenylethylamine derivative: formation of glutathione conjugates in vitro in the rat.
Xenobiotica; the fate of foreign compounds in biological systems 2005;35(7):697-713.
2005: Brenda L Palucki; Min K Park; Ravi P Nargund; Rui Tang; Tanya MacNeil; David Weinberg; Aurawan Vongs; Charles I Rosenblum; George A Doss; Randall R Miller; Ralph A Stearns; Qianping Peng; Constantin Tamvakopoulos; Lex H T Van Der Ploeg; Arthur A Patchett
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Bioorganic & medicinal chemistry letters 2005;15(8):1993-6.
2005: Zhoupeng Zhang; Qing Chen; Ying Li; George A Doss; Brian J Dean; Jason S Ngui; Maria V Silva Elipe; Seongkon Kim; Jane Y Wu; Frank DiNinno; Milton L Hammond; Ralph A Stearns; David C Evans; Thomas A Baillie; Wei Tang
In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: formation of reactive iminium and quinone type metabolites.
Chemical research in toxicology 2005;18(4):675-85.
2005: George A Doss; Randall R Miller; Zhoupeng Zhang; Yohannes Teffera; Ravi P Nargund; Brenda L Palucki; Min K Park; Yui S Tang; David C Evans; Thomas A Baillie; Ralph A Stearns
Metabolic activation of a 1,3-disubstituted piperazine derivative: evidence for a novel ring contraction to an imidazoline.
Chemical research in toxicology 2005;18(2):271-6.
2005: Brenda L Palucki; Min K Park; Ravi P Nargund; Zhixiong Ye; Iyassu K Sebhat; Patrick G Pollard; Rubana N Kalyani; Rui Tang; Tanya MacNeil; David Weinberg; Aurawan Vongs; Charles I Rosenblum; George A Doss; Randall R Miller; Ralph A Stearns; Qianping Peng; Constantin Tamvakopoulos; Erin McGowan; William J Martin; Joseph M Metzger; Cherrie A Shepherd; Alison M Strack; D Euan MacIntyre; Lex H T Van Der Ploeg; Arthur A Patchett
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Bioorganic & medicinal chemistry letters 2005;15(1):171-5.
2005: Shiyao Xu; Bing Zhu; Yohannes Teffera; Deborah E Pan; Charles G Caldwell; George A Doss; Ralph A Stearns; David C Evans; Maria G Beconi
Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes.
Drug metabolism and disposition: the biological fate of chemicals 2005;33(1):121-30.
2004: Qing Chen; Eugene Tan; John R Strauss; Zhoupeng Zhang; Judy Fenyk-Melody; Catherine Booth-Genthe; Thomas H Rushmore; Ralph A Stearns; David C Evans; Thomas A Baillie; Wei Tang
Effect of quinidine on the 10-hydroxylation of R-warfarin: species differences and clearance projection.
The Journal of pharmacology and experimental therapeutics 2004;311(1):307-14.
2004: Wenji Yin; Kaushik Mitra; Ralph A Stearns; Thomas A Baillie; Sanjeev Kumar
Conversion of the 2,2,6,6-tetramethylpiperidine moiety to a 2,2-dimethylpyrrolidine by cytochrome P450: evidence for a mechanism involving nitroxide radicals and heme iron.
Biochemistry 2004;43(18):5455-66.
2004: Theodore M Kamenecka; You-Jung Park; Linus S Lin; Stephen E de Laszlo; Ermengilda McCauley; Gail Van Riper; Linda A Egger; Usha Kidambi; Richard A Mumford; Sharon Tong; Wei Tang; Adria Colletti; Yohannes Teffera; Ralph A Stearns; Malcolm MacCoss; John A Schmidt; William K Hagmann
Amidines as amide bond replacements in VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2004;14(9):2323-6.
2004: Zhoupeng Zhang; Ying Li; Magang Shou; Y Zhang; Jason S Ngui; Ralph A Stearns; David C Evans; Thomas A Baillie; Wei Tang
Influence of different recombinant systems on the cooperativity exhibited by cytochrome P4503A4.
Xenobiotica; the fate of foreign compounds in biological systems 2004;34(5):473-86.
2004: Randall R Miller; George A Doss; Ralph A Stearns
Identification of a hydroxylamine glucuronide metabolite of an oral hypoglycemic agent.
Drug metabolism and disposition: the biological fate of chemicals 2004;32(2):178-85.
2004: Wenji Yin; George A Doss; Ralph A Stearns; Sanjeev Kumar
N-acetylation of the glutamate residue of intact glutathione conjugates in rats: a novel pathway for the metabolic processing of thiol adducts of xenobiotics.
Drug metabolism and disposition: the biological fate of chemicals 2004;32(1):43-8.
2003: Koppara Samuel; Wenji Yin; Ralph A Stearns; Yui S Tang; Ashok G Chaudhary; James P Jewell; Thomas J Lanza; Linus S Lin; William K Hagmann; David C Evans; Sanjeev Kumar
Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques.
Journal of mass spectrometry : JMS 2003;38(2):211-21.
2003: Wenji Yin; George A Doss; Ralph A Stearns; Ashok G Chaudhary; Cornelis E C A Hop; Ronald B Franklin; Sanjeev Kumar
A novel P450-catalyzed transformation of the 2,2,6,6-tetramethyl piperidine moiety to a 2,2-dimethyl pyrrolidine in human liver microsomes: characterization by high resolution quadrupole-time-of-flight mass spectrometry and 1H-NMR.
Drug metabolism and disposition: the biological fate of chemicals 2003;31(2):215-23.
2002: Sanjeev Kumar; Koppara Samuel; Raju Subramanian; Matthew P Braun; Ralph A Stearns; Shuet-Hing Lee Chiu; David C Evans; Thomas A Baillie
Extrapolation of diclofenac clearance from in vitro microsomal metabolism data: role of acyl glucuronidation and sequential oxidative metabolism of the acyl glucuronide.
The Journal of pharmacology and experimental therapeutics 2002;303(3):969-78.
2002: Iyassu K Sebhat; William J Martin; Zhixiong Ye; Khaled Barakat; Ralph T Mosley; David B R Johnston; Raman Bakshi; Brenda L Palucki; David Weinberg; Tanya MacNeil; Rubana N Kalyani; Rui Tang; Ralph A Stearns; Randall R Miller; Constantin Tamvakopoulos; Alison M Strack; Erin McGowan; Doreen E Cashen; Jennifer E Drisko; Gary J Hom; Andrew D Howard; D Euan MacIntyre; Lex H T Van Der Ploeg; Arthur A Patchett; Ravi P Nargund
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Journal of medicinal chemistry 2002;45(21):4589-93.
2002: Ihor E Kopka; Linus S Lin; Richard A Mumford; Thomas J Lanza; Plato A Magriotis; David Young; Stephen E DeLaszlo; Malcolm MacCoss; Sander G Mills; Gail Van Riper; Ermengilda McCauley; Kathryn Lyons; Stella Vincent; Linda A Egger; Usha Kidambi; Ralph A Stearns; Adria Colletti; Yohannes Teffera; Sharon Tong; Karen Owens; Dorothy A Levorse; John A Schmidt; William K Hagmann
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(17):2415-8.
2002: Qing Chen; Jason S Ngui; George A Doss; Regina W Wang; Xiaoxin Cai; Frank DiNinno; Timothy A Blizzard; Milton L Hammond; Ralph A Stearns; David C Evans; Thomas A Baillie; Wei Tang
Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation.
Chemical research in toxicology 2002;15(7):907-14.
2002: Wei Tang; Ralph A Stearns; Randall R Miller; Jason S Ngui; Robert J Mathvink; Ann E Weber; Gloria Y Kwei; John R Strauss; Carol Ann Keohane; George A Doss; Shuet-Hing Lee Chiu; Thomas A Baillie
Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate.
Drug metabolism and disposition: the biological fate of chemicals 2002;30(7):778-87.
2002: Ralph A Stearns; Randall R Miller; Wei Tang; Gloria Y Kwei; Frank S Tang; Robert J Mathvink; Elizabeth M Naylor; Dawn Chitty; Vincent J Colandrea; Ann E Weber; Adria Colletti; John R Strauss; Carol Ann Keohane; William P Feeney; Susan A Iliff; Shuet-Hing Lee Chiu
The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and monkeys: improving oral bioavailability.
Drug metabolism and disposition: the biological fate of chemicals 2002;30(7):771-7.
2002: Zhoupeng Zhang; Ying Li; Ralph A Stearns; Paul R. Ortiz de Montellano; Thomas A Baillie; Wei Tang
Cytochrome P450 3A4-mediated oxidative conversion of a cyano to an amide group in the metabolism of pinacidil.
Biochemistry 2002;41(8):2712-8.
2002: Ihor E Kopka; David N Young; Linus S Lin; Richard A Mumford; Plato A Magriotis; Malcolm MacCoss; Sander G Mills; Gail Van Riper; Ermengilda McCauley; Linda E Egger; Usha Kidambi; John A Schmidt; Kathryn Lyons; Ralph A Stearns; Stella Vincent; Adria Colletti; Zhen Wang; Sharon Tong; Junying Wang; Song Zheng; Karen Owens; Dorothy A Levorse; William K Hagmann
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(4):637-40.
2002: Linus S Lin; Ihor E Kopka; Richard A Mumford; Plato A Magriotis; Thomas J Lanza; Philippe L Durette; Theodore M Kamenecka; David N Young; Stephen E de Laszlo; Ermengilda McCauley; Gail Van Riper; Usha Kidambi; Linda A Egger; Xinchun Tong; Kathryn Lyons; Stella Vincent; Ralph A Stearns; Adria Colletti; Yohannes Teffera; Judy Fenyk-Melody; John A Schmidt; Malcolm MacCoss; William K Hagmann
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(4):611-4.
2001: Grace K Poon; Qing Chen; Yohannes Teffera; Jason S Ngui; Patrick R Griffin; Matthew P Braun; George A Doss; C Freeden; Ralph A Stearns; David C Evans; Thomas A Baillie; Wei Tang
Bioactivation of diclofenac via benzoquinone imine intermediates-identification of urinary mercapturic acid derivatives in rats and humans.
Drug metabolism and disposition: the biological fate of chemicals 2001;29(12):1608-13.
2001: Jason S Ngui; Qing Chen; Magang Shou; Regina W Wang; Ralph A Stearns; Thomas A Baillie; Wei Tang
In vitro stimulation of warfarin metabolism by quinidine: increases in the formation of 4'- and 10-hydroxywarfarin.
Drug metabolism and disposition: the biological fate of chemicals 2001;29(6):877-86.
2000: Robert J Mathvink; J S Tolman; Dawn Chitty; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
Journal of medicinal chemistry 2000;43(21):3832-6.
2000: Jason S Ngui; Wei Tang; Ralph A Stearns; Magang Shou; Randall R Miller; Y Zhang; Jiunn H Lin; Thomas A Baillie
Cytochrome P450 3A4-mediated interaction of diclofenac and quinidine.
Drug metabolism and disposition: the biological fate of chemicals 2000;28(9):1043-50.
2000: Szalkowski Deborah; D D Feng; Gui-Bai Liang; H Kuo; Xiaoxia Qian; Elizabeth M Naylor; Vincent J Colandrea; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Ralph A Stearns; Catherine D Strader; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.
Bioorganic & medicinal chemistry letters 2000;10(13):1431-4.
2000: D D Feng; Szalkowski Deborah; Mari Rios Candelore; Margaret A Cascieri; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Catherine D Strader; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Bioorganic & medicinal chemistry letters 2000;10(13):1427-9.
1999: Wei Tang; Ralph A Stearns; Gloria Y Kwei; Susan A Iliff; Randall R Miller; Marjorie A Egan; Nathan X Yu; Dennis C Dean; Sanjeev Kumar; Magang Shou; Jiunn H Lin; Thomas A Baillie
Interaction of diclofenac and quinidine in monkeys: stimulation of diclofenac metabolism.
The Journal of pharmacology and experimental therapeutics 1999;291(3):1068-74.
1999: Thomas L Shih; Mari Rios Candelore; Margaret A Cascieri; Shuet-Hing Lee Chiu; Lawrence F Colwell; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Catherine D Strader; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Bioorganic & medicinal chemistry letters 1999;9(9):1251-4.
1999: Emma R Parmee; Elizabeth M Naylor; L Perkins; Vincent J Colandrea; Hyun O Ok; Mari Rios Candelore; Margaret A Cascieri; L Deng; William P Feeney; Michael J Forrest; Gary J Hom; D Euan MacIntyre; Randall R Miller; Ralph A Stearns; Catherine D Strader; Laurie M Tota; Matthew J Wyvratt; Michael H Fisher; Ann E Weber
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
Bioorganic & medicinal chemistry letters 1999;9(5):749-54.
1999: Wei Tang; Ralph A Stearns; S M Bandiera; Y Zhang; Conrad E Raab; Matthew P Braun; Dennis C Dean; Jianmei Pang; Kwan H Leung; George A Doss; John R Strauss; Gloria Y Kwei; Thomas H Rushmore; Shuet-Hing Lee Chiu; Thomas A Baillie
Studies on cytochrome P-450-mediated bioactivation of diclofenac in rats and in human hepatocytes: identification of glutathione conjugated metabolites.
Drug metabolism and disposition: the biological fate of chemicals 1999;27(3):365-72.
1999: Wei Tang; Ralph A Stearns; Regina W Wang; Shuet-Hing Lee Chiu; Thomas A Baillie
Roles of human hepatic cytochrome P450s 2C9 and 3A4 in the metabolic activation of diclofenac.
Chemical research in toxicology 1999;12(2):192-9.
1998: Bindhu V Karanam; Randall R Miller; Adria Colletti; T Montgomery; K D Carey; T Hawkins; Yui S Tang; M Lavin; Ralph A Stearns; Shuet-Hing Lee Chiu; Stella H Vincent
Disposition of L-732,531, a potent immunosuppressant, in rats and baboons.
Drug metabolism and disposition: the biological fate of chemicals 1998;26(10):949-57.
1998: Ann E Weber; Hyun O Ok; Raul Alvaro; Mari Rios Candelore; Margaret A Cascieri; Shuet-Hing Lee Chiu; L Deng; Michael J Forrest; Gary J Hom; JE Hutchins; J Kao; D Euan MacIntyre; Robert J Mathvink; Debra McLoughlin; Randall R Miller; R C Newbold; Timothy V Olah; Emma R Parmee; L Perkins; Ralph A Stearns; Catherine D Strader; J Szumiloski; Yui S Tang; Laurie M Tota; Michael H Fisher
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Bioorganic & medicinal chemistry letters 1998;8(16):2111-6.
1998: Michael H Fisher; A M Amend; TJ Bach; J M Barker; Edward J Brady; Mari Rios Candelore; D Carroll; Margaret A Cascieri; Shuet-Hing Lee Chiu; L Deng; Michael J Forrest; B Hegarty-Friscino; Xiao-Ming Guan; Gary J Hom; JE Hutchins; Linda J Kelly; Robert J Mathvink; Joseph M Metzger; Randall R Miller; Hyun O Ok; Emma R Parmee; Richard Saperstein; Catherine D Strader; Ralph A Stearns; D Euan MacIntyre
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.
The Journal of clinical investigation 1998;101(11):2387-93.
1997: Ray Bakhtiar; Kwan H Leung; Ralph A Stearns; Cornelis E C A Hop
Evidence for a novel heme adduct generated by the in vitro reaction of 2,4,6-trinitrotoluene with human hemoglobin using electrospray ionization mass spectrometry.
Journal of inorganic biochemistry 1997;68(4):273-8.
1997: D Luffer-Atlas; Stella H Vincent; S K Painter; Byron H Arison; Ralph A Stearns; Shuet-Hing Lee Chiu
Orally active inhibitors of human leukocyte elastase. III. Identification and characterization of metabolites of L-694,458 by liquid chromatography-tandem mass spectrometry.
Drug metabolism and disposition: the biological fate of chemicals 1997;25(8):940-52.
1996: Kwan H Leung; D A Cohn; Randall R Miller; George A Doss; Ralph A Stearns; R E Simpson; William P Feeney; Shuet-Hing Lee Chiu
Pharmacokinetics and disposition of L-692,429. A novel nonpeptidyl growth hormone secretagogue in preclinical species.
Drug metabolism and disposition: the biological fate of chemicals 1996;24(7):753-60.
1995: Kwan H Leung; M Yao; Ralph A Stearns; Shuet-Hing Lee Chiu
Mechanism of bioactivation and covalent binding of 2,4,6-trinitrotoluene.
Chemico-biological interactions 1995;97(1):37-51.
1995: P A Krieter; Adria Colletti; Randall R Miller; Ralph A Stearns
Absorption and glucuronidation of the angiotensin II receptor antagonist losartan by the rat intestine.
The Journal of pharmacology and experimental therapeutics 1995;273(2):816-22.
1995: Shuet-Hing Lee Chiu; K A Thompson; Stella H Vincent; R F Alvaro; S W Huskey; Ralph A Stearns; Douglas J Pettibone
The role of drug metabolism in drug discovery: a case study in the selection of an oxytocin receptor antagonist for development.
Toxicologic pathology 1995;23(2):124-30.
1995: Suresh K Balani; Byron H Arison; L Mathai; L R Kauffman; Randall R Miller; Ralph A Stearns; I-Wu Chen; Jiunn H Lin
Metabolites of L-735,524, a potent HIV-1 protease inhibitor, in human urine.
Drug metabolism and disposition: the biological fate of chemicals 1995;23(2):266-70.
1995: Ralph A Stearns; P K Chakravarty; R Chen; Shuet-Hing Lee Chiu
Biotransformation of losartan to its active carboxylic acid metabolite in human liver microsomes. Role of cytochrome P4502C and 3A subfamily members.
Drug metabolism and disposition: the biological fate of chemicals 1995;23(2):207-15.
1995: Ray Bakhtiar; Ralph A Stearns
Studies on non-covalent associations of immunosuppressive drugs with serum albumin using pneumatically assisted electrospray ionization mass spectrometry.
Rapid communications in mass spectrometry : RCM 1995;9(3):240-4.
1994: E S Venkataramani; J R Carlin; U Dolling; P Christofalo; R J Magliette; Byron H Arison; Ralph A Stearns
Biotransformation of finasteride (MK-0906) by Selenastrum capricornutum (green algae).
Annals of the New York Academy of Sciences 1994;745():51-60.
1993: Ralph A Stearns; Randall R Miller; Byron H Arison; A Rosegay; J L Smith; N B Mantlo; Shuet-Hing Lee Chiu
Evidence for a 1,2-hydride shift in the microsomal metabolism of the heterocycle L-158,338, a nonpeptide angiotensin II receptor antagonist.
Drug metabolism and disposition: the biological fate of chemicals 1993;21(4):670-6.
1992: Ann E Weber; M G Steiner; P A Krieter; Adria Colletti; J R Tata; T A Halgren; R G Ball; J J Doyle; TW Schorn; Ralph A Stearns
Highly potent, orally active diester macrocyclic human renin inhibitors.
Journal of medicinal chemistry 1992;35(21):3755-73.
1992: Y Y Liu; Anthony Y H Lu; Ralph A Stearns; Shuet-Hing Lee Chiu
In vivo covalent binding of [14C]trinitrotoluene to proteins in the rat.
Chemico-biological interactions 1992;82(1):1-19.
1992: Ralph A Stearns; Randall R Miller; George A Doss; P K Chakravarty; A Rosegay; G J Gatto; Shuet-Hing Lee Chiu
The metabolism of DuP 753, a nonpeptide angiotensin II receptor antagonist, by rat, monkey, and human liver slices.
Drug metabolism and disposition: the biological fate of chemicals 1992;20(2):281-7.
1991: Ralph A Stearns; George A Doss; Randall R Miller; Shuet-Hing Lee Chiu
Synthesis and identification of a novel tetrazole metabolite of the angiotensin II receptor antagonist DuP 753.
Drug metabolism and disposition: the biological fate of chemicals 1991;19(6):1160-2.