Irving Wainer - Academia.edu (original) (raw)
Papers by Irving Wainer
Verapamil (VER) first pass clearance: S-NOR verapmil (S-NOR) formation contributes less with age while R-NOR verapmil (R-NOR) formation does not change in aging
Clinical Pharmacology & Therapeutics, 1996
ABSTRACT
Drug Metabolism and Disposition, Jul 1, 2000
Chapter 7 Immobilized enzyme reactors in liquid chromatography: On-line bioreactors for use in synthesis and drug discovery
![Research paper thumbnail of Relationship between Dose Rate of [6RS]Leucovorin Administration, Plasma Concentrations of Reduced Folates, and Pools of 5,10-Methylenetetrahydrofolates and Tetrahydrofolates in Human Colon Adenocarcinoma Xenografts](https://attachments.academia-assets.com/54360467/thumbnails/1.jpg)
](Cancer Research, Jun 15, 1990
(5-formyltetrahydrofolate; 5-CHO-H4PteGlu) ad ministered in different regimens in combination wit... more (5-formyltetrahydrofolate; 5-CHO-H4PteGlu) ad ministered in different regimens in combination with 5-fluorouracil (FUra) has increased the response rates to FUra in patients with colon adenocarcinoma. Using preclinical models of human colon adenocarcinomas as xenografts in immune-deprived mice, the effect of the rate of administration of racemic |6AS]leucovorin on the concentration-time profile of reduced folates in plasma, size of ¡ritrai umor pools of 5,10methylenetetrahydrofolates (CH2-H4PteGlu„) and tetrahydrofolates (1 U'U'Ã-.luJ. and the distribution of their polyglutamate species have been examined.
Quantitative structure-enantioselective retention relationships for the chromatography of 1,4-benzodiazepines on a human serum albumin based HPLC stationary phase : an approach to the computational prediction of retention and enantioselectivity
Chromatographia, 1992
ABSTRACT
Immobilization of membrane receptor on HPLC
Genotype/phenotype comparisons: a probe for the effect of disease progression on drug metabolism
Current Opinion in Drug Discovery Development, Feb 1, 2002
The effect of disease state on drug metabolism has been investigated using the relationship betwe... more The effect of disease state on drug metabolism has been investigated using the relationship between genotype and metabolic phenotype. The two polymorphic probes, N-acetyltransferases-2 (NAT2) and cytochrome P450 2C19 (CYP2C19), were respectively used in HIV+/AIDS patients and patients with advanced cancer. The results of the studies suggest that advanced disease produces discordances between genotype and phenotype, indicating a reduction in the metabolic capabilities of these individuals. Thus, polymorphic enzymes such as CYP2C19 and NAT2 can be used to probe changes in drug-metabolizing enzyme capacities. The development of genotype/phenotype discordances should reflect general changes in metabolic capabilities and, thus, alterations in the activities of other important enzymes such as CYP3A. The data also suggest that the genotype/phenotype probes can be used to optimize the clinical treatment of patients with advanced disease states.
Fenoterol derivatives show multitarget interactions with beta2 adrenergic and 5-HT receptors
The Faseb Journal, Mar 1, 2008
A unique reversal of elution order during direct enantiomeric resolution of amide derivatives of 1-phenyl-2-aminopropane by high performance liquide chromatography on chiral stationary phases
Hrc Cc Journal of High Resolution Chromatography Chromatography Communications, 1984
High-performance liquid chromatographic separation of the diastereoisomers of propoxyphene Determination of microquantities of β-dl-propoxyphene in comercial preparations of α-d-propoxyphene
Journal of Chromatography a, May 21, 1982
Methods of regulating cannabinoid receptor activity-related disorders and diseases
High Performance Liquid Chromatography: Fundamental Principles and Practice (Paperback) - Taylor & Francis
Abstract 240: Phosphorylation of {beta}2-Adrenoceptor by cAMP-Dependent Protein Kinase Is Neither Necessary nor Sufficient to Mediate the Receptor Coupling to Gi Proteins
Circulation, Oct 28, 2008
Journal of Chromatography a, Oct 1, 1986
The steric and electronic effects in the resolution of enantiomeric amides on a commercially avai... more The steric and electronic effects in the resolution of enantiomeric amides on a commercially available (R)-N-(3,5-dinitrobenzoyl)phenylglycine chiral stationary phase (CSP) have been investigated. Several homologous series of enantiomeric amides were synthesized from alkyl and aromatic amines and from alkyl and aromatic acids. The results of the study indicate that chiral recognition is based on the formation of diastereomeric solute-CSP complexes that are due to attractive interactions located on a single bond in both the solute and CSP and on steric interactions within the complexes. The magnitude of the chiral resolution appears to depend on the steric bulk at the chiral center. In addition, when the amides synthesized from chiral amines were chromatographed, the (R)-enantiomers eluted first, whereas the opposite elution order was found for the amides synthesized from enantiomeric carboxylic acids. Thus, the amide moiety not only provides the sites of attractive interaction between the solute and CSP, but also influences the spatial orientation of the two molecules, thereby affecting the relative stabilities of the two diastereomeric complexes and determinging the enantiomeric elution order. 0021-9673/86/%03.50 0 1986 Elsevier Science Publishers B.V.
Journal of Chromatography a, 1983
In the past few years a number of advances have been made in the area of direct resolution of ena... more In the past few years a number of advances have been made in the area of direct resolution of enantiomers, using chiral stationary phases (CSPs) in gas-liquid and high-performance liquid chromatography (HPLC). Pirkle et al. ' have recently reported the development of a CSP, (R)-N-(3,5-dinitrobenzoyl)phenylglycine, which is ionically bonded to y-aminopropyl silanized silica gel. The resulting support has broad applicability toward HPLC resolution of enantiomers'J. We now report the application of this CSP to the separation of enantiomers via thin-layer chromatography (TLC).
Application of high-performance liquid chromatographic chiral stationary phases to pharmaceutical analysis Resolution of enantiomeric barbiturates, succinimides and related molecules on four commercially available chiral stationary phases
Journal of Chromatography a, Jun 1, 1985
Application of high-performance liquid chromatographic chiral stationary phases to pharmaceutical analysis: resolution of ephedrine
Journal of Chromatography a, 1983
The Application of HPLC Chiral Stationary Phases to Stereochemical Problems of Pharmaceutical Interest: A General Method for the Resolution of Enantiomeric Amines as β-Naphthylcarbamate Derivatives
Journal of Liquid Chromatography, 1986
Page 1. JOURNAL OF LIQUID CHROMATOGRAPHY, 9(2&3), 455-471 (1986) THE APPLICAT... more Page 1. JOURNAL OF LIQUID CHROMATOGRAPHY, 9(2&3), 455-471 (1986) THE APPLICATION OF HPLC CHIRAL STATIONARY PHASES TO STEREOCHEMICAL PROBLEMS OF PHARMACEUTICAL INTEREST: A GENERAL METHOD FOR THE RESOLUTION ...
On-line determination of lipase activity and enantioselectivity using an immobilized enzyme reactor coupled to a chiral stationary phase
Tetrahedron Lett, 1993
Immobilised G-protein coupled receptors on an artificial lipid membrane of a liquid chromatography stationary phase and use thereof for screening
Verapamil (VER) first pass clearance: S-NOR verapmil (S-NOR) formation contributes less with age while R-NOR verapmil (R-NOR) formation does not change in aging
Clinical Pharmacology & Therapeutics, 1996
ABSTRACT
Drug Metabolism and Disposition, Jul 1, 2000
Chapter 7 Immobilized enzyme reactors in liquid chromatography: On-line bioreactors for use in synthesis and drug discovery
Cancer Research, Jun 15, 1990
(5-formyltetrahydrofolate; 5-CHO-H4PteGlu) ad ministered in different regimens in combination wit... more (5-formyltetrahydrofolate; 5-CHO-H4PteGlu) ad ministered in different regimens in combination with 5-fluorouracil (FUra) has increased the response rates to FUra in patients with colon adenocarcinoma. Using preclinical models of human colon adenocarcinomas as xenografts in immune-deprived mice, the effect of the rate of administration of racemic |6AS]leucovorin on the concentration-time profile of reduced folates in plasma, size of ¡ritrai umor pools of 5,10methylenetetrahydrofolates (CH2-H4PteGlu„) and tetrahydrofolates (1 U'U'Ã-.luJ. and the distribution of their polyglutamate species have been examined.
Quantitative structure-enantioselective retention relationships for the chromatography of 1,4-benzodiazepines on a human serum albumin based HPLC stationary phase : an approach to the computational prediction of retention and enantioselectivity
Chromatographia, 1992
ABSTRACT
Immobilization of membrane receptor on HPLC
Genotype/phenotype comparisons: a probe for the effect of disease progression on drug metabolism
Current Opinion in Drug Discovery Development, Feb 1, 2002
The effect of disease state on drug metabolism has been investigated using the relationship betwe... more The effect of disease state on drug metabolism has been investigated using the relationship between genotype and metabolic phenotype. The two polymorphic probes, N-acetyltransferases-2 (NAT2) and cytochrome P450 2C19 (CYP2C19), were respectively used in HIV+/AIDS patients and patients with advanced cancer. The results of the studies suggest that advanced disease produces discordances between genotype and phenotype, indicating a reduction in the metabolic capabilities of these individuals. Thus, polymorphic enzymes such as CYP2C19 and NAT2 can be used to probe changes in drug-metabolizing enzyme capacities. The development of genotype/phenotype discordances should reflect general changes in metabolic capabilities and, thus, alterations in the activities of other important enzymes such as CYP3A. The data also suggest that the genotype/phenotype probes can be used to optimize the clinical treatment of patients with advanced disease states.
Fenoterol derivatives show multitarget interactions with beta2 adrenergic and 5-HT receptors
The Faseb Journal, Mar 1, 2008
A unique reversal of elution order during direct enantiomeric resolution of amide derivatives of 1-phenyl-2-aminopropane by high performance liquide chromatography on chiral stationary phases
Hrc Cc Journal of High Resolution Chromatography Chromatography Communications, 1984
High-performance liquid chromatographic separation of the diastereoisomers of propoxyphene Determination of microquantities of β-dl-propoxyphene in comercial preparations of α-d-propoxyphene
Journal of Chromatography a, May 21, 1982
Methods of regulating cannabinoid receptor activity-related disorders and diseases
High Performance Liquid Chromatography: Fundamental Principles and Practice (Paperback) - Taylor & Francis
Abstract 240: Phosphorylation of {beta}2-Adrenoceptor by cAMP-Dependent Protein Kinase Is Neither Necessary nor Sufficient to Mediate the Receptor Coupling to Gi Proteins
Circulation, Oct 28, 2008
Journal of Chromatography a, Oct 1, 1986
The steric and electronic effects in the resolution of enantiomeric amides on a commercially avai... more The steric and electronic effects in the resolution of enantiomeric amides on a commercially available (R)-N-(3,5-dinitrobenzoyl)phenylglycine chiral stationary phase (CSP) have been investigated. Several homologous series of enantiomeric amides were synthesized from alkyl and aromatic amines and from alkyl and aromatic acids. The results of the study indicate that chiral recognition is based on the formation of diastereomeric solute-CSP complexes that are due to attractive interactions located on a single bond in both the solute and CSP and on steric interactions within the complexes. The magnitude of the chiral resolution appears to depend on the steric bulk at the chiral center. In addition, when the amides synthesized from chiral amines were chromatographed, the (R)-enantiomers eluted first, whereas the opposite elution order was found for the amides synthesized from enantiomeric carboxylic acids. Thus, the amide moiety not only provides the sites of attractive interaction between the solute and CSP, but also influences the spatial orientation of the two molecules, thereby affecting the relative stabilities of the two diastereomeric complexes and determinging the enantiomeric elution order. 0021-9673/86/%03.50 0 1986 Elsevier Science Publishers B.V.
Journal of Chromatography a, 1983
In the past few years a number of advances have been made in the area of direct resolution of ena... more In the past few years a number of advances have been made in the area of direct resolution of enantiomers, using chiral stationary phases (CSPs) in gas-liquid and high-performance liquid chromatography (HPLC). Pirkle et al. ' have recently reported the development of a CSP, (R)-N-(3,5-dinitrobenzoyl)phenylglycine, which is ionically bonded to y-aminopropyl silanized silica gel. The resulting support has broad applicability toward HPLC resolution of enantiomers'J. We now report the application of this CSP to the separation of enantiomers via thin-layer chromatography (TLC).
Application of high-performance liquid chromatographic chiral stationary phases to pharmaceutical analysis Resolution of enantiomeric barbiturates, succinimides and related molecules on four commercially available chiral stationary phases
Journal of Chromatography a, Jun 1, 1985
Application of high-performance liquid chromatographic chiral stationary phases to pharmaceutical analysis: resolution of ephedrine
Journal of Chromatography a, 1983
The Application of HPLC Chiral Stationary Phases to Stereochemical Problems of Pharmaceutical Interest: A General Method for the Resolution of Enantiomeric Amines as β-Naphthylcarbamate Derivatives
Journal of Liquid Chromatography, 1986
Page 1. JOURNAL OF LIQUID CHROMATOGRAPHY, 9(2&3), 455-471 (1986) THE APPLICAT... more Page 1. JOURNAL OF LIQUID CHROMATOGRAPHY, 9(2&3), 455-471 (1986) THE APPLICATION OF HPLC CHIRAL STATIONARY PHASES TO STEREOCHEMICAL PROBLEMS OF PHARMACEUTICAL INTEREST: A GENERAL METHOD FOR THE RESOLUTION ...
On-line determination of lipase activity and enantioselectivity using an immobilized enzyme reactor coupled to a chiral stationary phase
Tetrahedron Lett, 1993
Immobilised G-protein coupled receptors on an artificial lipid membrane of a liquid chromatography stationary phase and use thereof for screening