Abstract
Various salts of 3-allyl-1,1-dibenzyl-2-ethyl-isothiourea, 1 (hydrochloride), 2 (hydrobromide), and 3 (hydroiodide), were synthesized. Ca-blocking properties of these salts were studied. Comparative analysis of the potentiating effects of 3 and cyclothiazide (CT) on transmembrane currents caused by kainic acid (KA) and glutamate in Purkinje neurons was performed. Analysis of the effects of 1 on N-methyl-D-aspartate (NMDA) receptors was performed on primary culture of heterogeneous neurons of rat cerebral cortex. Single crystals were grown and X-ray diffraction experiments solving the crystal structures of 1-3 were carried out. Analysis of conformations of the molecules in the crystal lattices was performed. The temperature dependencies of the solubility of 1-3 in water and n-octanol were obtained, and the thermodynamic parameters of solubility process were calculated. The effect of halogen atoms on the solubility was analyzed. The partitioning processes in the water-octanol system were studied at 25 degrees C. Chemical stability of tested salts in pH 7.4 phosphate buffer was determined at 25 degrees C.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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1-Octanol
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Allyl Compounds / chemical synthesis*
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Allyl Compounds / chemistry
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Allyl Compounds / pharmacology
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Animals
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Brain / cytology
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Calcium / metabolism
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Crystallography, X-Ray
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Drug Stability
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Drug Synergism
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In Vitro Techniques
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Ligands
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Neurons / drug effects
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Neurons / physiology
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Neuroprotective Agents / chemical synthesis*
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / pharmacology
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Nootropic Agents / chemical synthesis*
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Nootropic Agents / chemistry
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Nootropic Agents / pharmacology
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Patch-Clamp Techniques
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Purkinje Cells / drug effects
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Purkinje Cells / physiology
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Rats
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Receptors, AMPA / agonists
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Receptors, AMPA / physiology
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Receptors, N-Methyl-D-Aspartate / agonists
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Receptors, N-Methyl-D-Aspartate / physiology
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Solubility
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Structure-Activity Relationship
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Synaptosomes / drug effects
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Synaptosomes / metabolism
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Temperature
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Thermodynamics
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Thiourea / analogs & derivatives*
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Thiourea / chemical synthesis
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Thiourea / chemistry
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Thiourea / pharmacology
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Water
Substances
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3-allyl-1,1-dibenzyl-2-ethylisothiourea
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Allyl Compounds
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Ligands
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Neuroprotective Agents
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Nootropic Agents
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Receptors, AMPA
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Receptors, N-Methyl-D-Aspartate
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Water
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Thiourea
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1-Octanol
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Calcium