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Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
A good correlation was found between the logarithms of the equilibrium brain/blood concentration ratios in the rat and the partition parameter, delta log P, defined as log P (1-octanol/water)-log P (cyclohexane/water), which suggests that brain penetration might be improved by reducing overall hydrogen-bonding ability.
A role for histamine and H2-receptors in opioid antinociception.
It is suggested that stimulation of opioid receptors leads to antinociception by mechanisms that include activation of brain H2-receptors, and Cimetidine, unlike other H2 antagonists, potentiated MOR antinOCiception, potentiate opioid FSIA and increased brain MOR levels, actions that are not likely to be due to blockade of H1-receptor activity.
Zolantidine (SK&F 95282) is a potent selective brain‐penetrating histamine H2‐receptor antagonist
Zolantidine is characterized as a potent selective brain‐penetrating H2‐receptor antagonist, and will be a valuable pharmacological tool for investigating possible physiological and pathological roles for histamine in the central nervous system.
Kinetic relaxation measurement of rapid electron transfer reactions by flash photolysis. Conversion of light energy into chemical energy using the…
Dipole moment in relation to hydrogen receptor histamine antagonist activity for cimetidine analogs
H2-Rezeptor-Histaminantagonisten wie (III)-(VI) werden in uberwiegend literaturbekannter Weise synthetisiert und hinsichtlich ihrer Aktivitat mit Cimetidin (VII) verglichen.
Thrombocytopenia due to digitoxin. Demonstration of antibody and mechanisms of action.
Photochemical Generation of Ru(bpy)3+ and 02 -
Purine derivatives as competitive inhibitors of human erythrocyte membrane phosphatidylinositol 4-kinase.
- R. C. Young, M. Jones, K. Milliner, K. Rana, J. Ward
- Biology, ChemistryJournal of medicinal chemistry
- 1 August 1990
The possibility of deriving a potent, cell-penetrating inhibitor of human erythrocyte PI 4-kinase, competitive with respect to ATP, has been investigated in a series of purine derivatives and analogues, finding the optimum substitution pattern in purine to be an electron-releasing substituent in the 6-position.
An approach to the design of brain-penetrating histaminergic agonists
Total synthesis of the four stereoisomers of dihexadecanoyl phosphatidylinositol and the substrate stereospecificity of human erythrocyte membrane phosphatidylinositol 4-kinase.
Comparison of phosphorylation rates of the naturally occurring mammalian phospholipid, I, and its synthetic stereochemical counterpart, compound 10a, suggests that the enzyme is relatively tolerant to changes in fatty acid composition.