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showing 10 items of 1921 documents
Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice.
2011
Abstract The kinetics of excretion of the novel tranquilizer cinazepam (3-hydroxy-7-bromo-5-( ortho -chlorophenyl)-1,2-dihydro-3H-1,4-benzdiazepin-2-one hemisuccinate (I)) in mice after a single administration and different schemes of multiple administration were determined. Mass balance was studied daily in excretions of mice (feces and urine) for 5-10 days. We observed that monoexponen-tial renal excretion of 14 C-cinazepam and its metabolites predominated with all dosage regimens. Cinazepam and its metabolites were almost fully (> 90%) eliminated in urine and feces over the period of study (5-10 days), which means that no significant accumulation of the drug in the body occurred. The kin…
Cytotoxicity of main anthraquinone aglycons towards drug sensitive and multi drug resistant T leukaemia cancer cells
2016
Influence of Rhein on Rat Colonic Na<sup>+</sup>, K<sup>+</sup>-ATPase and Permeability in vitro
1988
Rhein, an aglucone of a laxative-acting anthraquinone, which induces net secretion in the human jejunum and colon, does not induce net secretion under open circuit current in in vitro conditions but r
Optically active titanium complexes containing a tridentate linked amido-cyclopentadienyl ligand
2000
Optically active titanium complexes Ti{η5:η1-C5R4SiMe2NC6H10 (OCH2Ph)-2}Cl2 (R = H, Me), containing a cyclopentadienyl ligand linked to the chiral trans-2-benzyloxycyclohexylamido group, were synthesized and characterized in both enantiomerically pure forms. A single crystal X-ray structure analysis of (−)-(R,R)-Ti{η5:η1-C5H4SiMe2NC6H10(OCH2Ph)-2}Cl2 shows a structure in which the benzyloxy group in the amido sidechain is not interacting with the titanium center. Upon activation with n-butyllithium, these complexes hydrogenate acetophenone N-benzylimine with low enantioselectivity. Chirality 12:472–475, 2000. © 2000 Wiley-Liss, Inc.
Evaluation of alprazolam-induced behavioural effects: differences with chlordiazepoxide after interaction with desipramine and rolipram, a cAMP phosp…
1989
Head-twitch and forepaw-shake responses after single and repeated treatment with rolipram: interaction with noradrenergic and dopaminergic agonists a…
1988
Development of predictive retention-activity models of butyrophenones by biopartitioning micellar chromatography
2001
The predictive and interpretative capability of quantitative chromatographic retention-biological activity models is supported by the fact that in adequate experimental conditions the solute partitioning into the chromatographic system can emulate the solute partitioning into lipid bilayers of biological membranes, which is the basis of drug and metabolite uptake, passive transport across membranes and bioaccumulation. The use of retention data obtained in biopartitioning micellar chromatography (BMC) has been demonstrated to be helpful in describing the biological behaviour of different kinds of drugs. In this chromatographic system, polioxyethylene 23 lauryl ether Brij35 micellar mobile p…
Quinol sulphate, a new conjugate of phenol in goldfish.
1983
1. Metabolism of phenol in goldfish yielded the known phenyl conjugates in fish--phenyl sulphate and phenyl glucuronide. Additionally, quinol sulphate, a new conjugate of phenol in fish, was detected.
Cardiovascular effects induced by rolipram, a selective cAMP phosphodiesterase inhibitor: Interaction with adrenergic and calcium affecting drugs
1990
H2-antihistaminics. 20. Structure-activity relationships in H2-receptor antagonists containing a 4-pyrimidone moiety.
1984
In a series of 5,6-substituted 4- pyrimidones 1 a-v the H2-antihistaminic activity was determined (guinea-pig atrium) and lipophilicity data are given in form of Rmo -values. The influence of different substituents at position 5 or 6 of a pyrimidone moiety has been studied. Quantitative structure-activity analyses showed the importance of lipophilicity for drug activity. Additionally other physicochemical substituent-properties may play a major role.