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Biomedical subjects

M Z Kagan

Publications and source records attributed to M Z Kagan.

8 recordsLinked to original sources
PubMed2001

Normal-phase high-performance liquid chromatographic separations using ethoxynonafluorobutane as hexane alternative. I. Analytical and chiral applications.

A novel, environmentally friendly, fluorinated solvent--ethoxynonafluorobutane--has been used to replace n-hexane in normal-phase HPLC applications. Fast gradients of methanol in ethoxynonafluorobutane on a cyano column have been successfully applied to the separation of steroids, benzodiazepines, NSAIDs, tricyclic antidepressants, beta-adrenergic blocking agents and mixtures of purines and pyrimidines. Small amounts of triethylamine and trifluoroacetic acid added to such gradients significantly improved peak shape and column performance for basic and acidic solutes. Ethoxynonafluorobutane and its mixtures with methanol have also been demonstrated to have a unique selectivity in chiral HPLC applications.

Adrenergic beta-Antagonists↗
PubMed1997

New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.

A series of 2-(aminomethyl)chromans (2-AMCs) was synthesized and evaluated for their affinity and selectivity for both the high- and low-affinity agonist states (D2High and D2Low, respectively) of the dopamine (DA) D2 receptor. The 7-hydroxy-2-(aminomethyl)chroman moiety was observed to be the primary D2 agonist pharmacophore. The 2-methylchroman moiety was discovered to be an entirely novel scaffold which could be used to access the D2 agonist pharmacophore. Attaching various simple alkyl and arylalkyl side chains to the 7-hydroxy 2-AMC nucleus had significant effects on selectivity for the D2High receptor vs the 5HT1A and alpha 1 receptors. A novel DA partial agonist, (R)-(-)-2-(benzylamino)methyl)chroman-7-ol [R-(-)-35c], was identified as having the highest affinity and best selectivity for the D2High receptor vs the alpha 1 and 5HT1A receptors. Several regions of the 2-AMC nucleus were modified and recognized as potential sites to modulate the level of intrinsic activity. The global minimum conformer of the 7-hydroxy-2-AMC moiety was identified as fulfilling the McDermed model D2 agonist pharmacophoric criteria and was proposed as the D2 receptor-bound conformation. Structure-activity relationships gained from these studies have aided in the synthesis of D2 partial agonists of varying intrinsic activity levels. These agents should be of therapeutic value in treating disorders resulting from hypo- and hyperdopaminergic activity, without the side effects associated with complete D2 agonism or antagonism.

Animals↗
PubMed1997

Polysulfated carbohydrates analyzed as ion-paired complexes with basic peptides and proteins using electrospray negative ionization mass spectrometry.

Electrospray ionization mass spectrometry was used in the negative ion mode to analyze complexes of sucrose octasulfate, sucrose heptasulfate and sulfated alpha-, beta- and gamma-cyclodextrins with synthetically prepared basic peptides, the basic protein ubiquitin and polyamines. The spectra presented demonstrate that complexes with these basic molecules facilitate the analysis of these polysulfated oligosaccharides. Stable (1:1) complexes result from the ion pairing between the protonated basic arginine and lysine residues of the peptide and the anionic sulfate groups of the polysulfated oligosaccharides. Fragmentation of the polysulfated oligosaccharides resulting in the loss of SO3 could be suppressed by controlling the experimental conditions, such as the nozzle-skimmer voltage, used to obtain the spectra. In the absence of fragmentation, it was possible to obtain data on the purity of sucrose octasulfate and sucrose heptasulfate as well as the distribution of the sulfated cyclodextrins. The confounding presence of sodium counter-ions is also eliminated using this method. Complete chemical sulfation of oligosaccharides is difficult to achieve. Thus, data on sample purity are essential for the characterization of sulfated oligosaccharides used as pharmaceutical agents.

Carbohydrates↗
PubMed1990

[A nontraditional approach to the study of gastric contents].

Acidification of the gastric contents is known to be the principal function of the stomach. The efficacy of acidification for digestion is limited by chymus formation, and that for absorption manifests as the enteral barrier permeability governing, mediated by the duodenal hormonal system, thus optimizing the absorption of nutrient substances in accordance with homeostasis requirements. The author suggests a simplified method of gastric intubation, improving the informative value of the results of examination.

Gastric Acidity Determination↗